| 1001 | Vm24 | AAAISCVGSPECPPKCRAQGCKNGKCMNRKCKCYYC | 36 | L | None | Amidation | Cross linked by eight cysteines (between Cys6 and Cys26, Cys12 and Cys31, Cys16 and Cys33, and Cys21 and Cys36) (Disulphide linkage) | Linear | Natural | Venom of the Mexican scorpion Vaejovis mexicanus smithi | Block Kv1.3 channels with high affinity, an estimated Kd of 2.9 pM | Inhibits T Cell Proliferation, CD25 Expression, and Ca2+ Signaling In Vitro and Suppresses DTH Reactions In Vivo | Both | Human peripheral T Cells, COS-7, human embryonic kidney 293, tsA201, L929, and MEL cells | NA | Female Lewis rats (9-10 weeks of age) | T cell Proliferation assays | NA | NA | 22622363 | 2012 |
| 1003 | Native kalata B1 | GLPVCGETCVGGTCNTPGCTCSWPVCTRN | 29 | L | None | None | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Natural cyclotide | A cyclotide isolated from Oldenlandia affinis DC. (Rubiaceae) | Reduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11) | Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression. | In vitro | Human peripheral Lymphocytes | 2.9±1.3 micromolar for Lymphocytes (PBMCs) | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1004 | Native kalata B2 | GLPVCGETCVGGTCNTPGCTCSWPVCTRN | 29 | L | None | None | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Natural cyclotide | A cyclotide isolated from Oldenlandia affinis DC. (Rubiaceae) | Reduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11) | Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression. | In vitro | Purified T cells | 2.4±0.5 micromolar for purified T cells | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1005 | kalata B1 mutants [T20K] | GLPVCGETCVGGTCNTPGCKCSWPVCTRN | 29 | L | Addition of Cysteine | Thioester linker | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Synthetic | NA | Reduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11) | Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression. | In vitro | Human peripheral Lymphocytes | 1.9±0.6 micromolar for Lymphocytes (PBMCs) | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1006 | kalata B1 mutants [T20K] | GLPVCGETCVGGTCNTPGCKCSWPVCTRN | 29 | L | Addition of Cysteine | Thioester linker | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Synthetic | NA | Reduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11) | Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression. | In vitro | Purified T cells | 2.7±0.6 micromolar for purified T cells | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1007 | kalata B1 mutants [N29K] | GLPVCGETCVGGTCNTPGCTCSWPVCTRK | 29 | L | Addition of Cysteine | Thioester linker | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Synthetic | NA | Reduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11) | Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression. | In vitro | Human peripheral Lymphocytes | 3.2±0.6 micromolar for Lymphocytes (PBMCs) | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1008 | kalata B1 mutants [N29K] | GLPVCGETCVGGTCNTPGCTCSWPVCTRK | 29 | L | Addition of Cysteine | Thioester linker | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Synthetic | NA | Reduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11) | Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression. | In vitro | Purified T cells | 2.1±0.9 micromolar for purified T cells | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1009 | kalata B1 mutants [G18K] | GLPVCGETCVGGTCNTPKCTCSWPVCTRN | 29 | L | Addition of Cysteine | Thioester linker | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Synthetic | NA | Reduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11) | Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression. | In vitro | Human peripheral Lymphocytes | 4.4±0.5 micromolar for Lymphocytes (PBMCs) | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1010 | kalata B1 mutants [G18K] | GLPVCGETCVGGTCNTPKCTCSWPVCTRN | 29 | L | Addition of Cysteine | Thioester linker | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Synthetic | NA | Reduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11) | Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression. | In vitro | Purified T cells | 3.2±1.8 micromolar for purified T cells | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1011 | OSK1 (α-KTx3.7) | GVIINVKCKISRQCLEPCKKAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge C1-C4, C2-C5 and C3-C6) | Linear | Natural | Venom of the central Asian scorpion Orthochirus scrobiculosus | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 0.60±0.04 nM for Kv1.1 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 2.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1012 | OSK1 (α-KTx3.7) | GVIINVKCKISRQCLEPCKKAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1C4, C2-C5 and C3-C6) | Linear | Natural | Venom of the central Asian scorpion Orthochirus scrobiculosus | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 5.40±1.89 nM for Kv1.2 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 2.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1013 | OSK1 (α-KTx3.7) | GVIINVKCKISRQCLEPCKKAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C-C4, C2-C5 and C3-C6) | Linear | Natural | Venom of the central Asian scorpion Orthochirus scrobiculosus | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 0.014±0.001 nM for Kv1.3 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 2.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1014 | OSK1 (α-KTx3.7) | GVIINVKCKISRQCLEPCKKAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge C1-C4, C2-C5 and C3-C6) | Linear | Natural | Venom of the central Asian scorpion Orthochirus scrobiculosus | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 225±10 nM for Kca 3.1 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 2.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1015 | [K16 ,D20 ]-OSK1 | GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 0.40± 0.01 nM for Kv1.1 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 2.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1016 | [K16 ,D20 ]-OSK1 | GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 2.96±0.01 nM for Kv1.2 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 2.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1017 | [K16 ,D20 ]-OSK1 | GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 0.003± 0.0011 nM for Kv1.3 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 2.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1018 | [K16 ,D20 ]-OSK1 | GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 228±92 nM for Kca 3.1 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 2.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1019 | [K16 ]-OSK1 | GVIINVKCKISRQCLKPCKKAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 0.63±0.05 nM for Kv1.1 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 3 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1020 | [K16 ]-OSK1 | GVIINVKCKISRQCLKPCKKAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 5.23±0.22 nM for Kv1.2 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 3 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1021 | [K16 ]-OSK1 | GVIINVKCKISRQCLKPCKKAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 0.067±0.006 nM for Kv1.3 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 3 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1022 | [K16 ]-OSK1 | GVIINVKCKISRQCLKPCKKAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 151±21 nM for Kca 3.1 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 3 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1023 | [D20 ]-OSK1 | GVIINVKCKISRQCLEPCKDAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 2.95±0.24 nM for Kv1.1 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 4.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1024 | [D20 ]-OSK1 | GVIINVKCKISRQCLEPCKDAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 77.8± 9.2 nM for Kv1.2 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 4.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1025 | [D20 ]-OSK1 | GVIINVKCKISRQCLEPCKDAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 0.037±0.007 nM for Kv1.3 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 4.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1026 | [D20 ]-OSK1 | GVIINVKCKISRQCLEPCKDAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 716±10 nM for Kca 3.1 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 4.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1027 | [P12 ,K16 , D20]-OSK1 | GVIINVKCKISPQCLKPCKDAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 3.18± 0.11 nM for Kv1.1 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 7.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1028 | [P12 ,K16 , D20]-OSK1 | GVIINVKCKISPQCLKPCKDAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 196±9 nM for Kv1.2 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 7.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1029 | [P12 ,K16 , D20]-OSK1 | GVIINVKCKISPQCLKPCKDAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 0.059±0.003 nM for Kv1.3 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 7.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1030 | [P12 ,K16 , D20]-OSK1 | GVIINVKCKISPQCLKPCKDAGMRFGKCMNGKCHCTPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channel | Potent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 2600±400 nM for Kca 3.1 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 7.5 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1031 | [K16,D20,Y36]-OSK1 | GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCYPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2, Kv 1.3 and Kv 1.7 channel and also Ca2+ -activated KCa 3.1 channel | Blocker of four different Kv channel types and also blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 34.4±0.3 nM for Kv1.1 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 9 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1032 | [K16,D20,Y36]-OSK1 | GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCYPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2, Kv 1.3 and Kv 1.7 channel and also Ca2+ -activated KCa 3.1 channel | Blocker of four different Kv channel types and also blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 232±11 nM for Kv1.2 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 9 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1033 | [K16,D20,Y36]-OSK1 | GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCYPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2, Kv 1.3 and Kv 1.7 channel and also Ca2+ -activated KCa 3.1 channel | Blocker of four different Kv channel types and also blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 0.122± 0.007 nM for Kv1.3 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 9 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1034 | [K16,D20,Y36]-OSK1 | GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCYPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2, Kv 1.3 and Kv 1.7 channel and also Ca2+ -activated KCa 3.1 channel | Blocker of four different Kv channel types and also blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 1500±500 nM for Kv1.7 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 9 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1035 | [K16,D20,Y36]-OSK1 | GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCYPK | 38 | L | None | None | Three- Disulphide-bridge (C1-C4, C2-C5 and C3-C6) | Linear | Synthetic | NA | Kv 1.1, Kv 1.2, Kv 1.3 and Kv 1.7 channel and also Ca2+ -activated KCa 3.1 channel | Blocker of four different Kv channel types and also blocker of Ca2+ -activated KCa 3.1 channel | Both | L929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells | 885±18 nM for Kca 3.1 | C57/BL6 mice | Neurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel | 9 (μg/kg of mice) | NA | 15588251 | 2005 |
| 1037 | Colutellin A | VISIIPV | 7 | L | None | None | None | Cyclic | Natural | Endophytic fungus Colletotrichum dematium | Inhibit IL-2 production by activated CD4+ T-cells | Inhibiting the calcineurin pathway | Both | Peripheral blood mononuclear cells (PBMCs) | 167.3±0.38 nM for CD4+ T cell activation of IL-2 production | C57/B6 mice | MIC assay, Immunosuppression and toxicity test | MIC of 3.6 mg/ml (48 h) against Botrytis cinerea and Sclerotinia sclerotiorum. | NA | 18599825 | 2008 |
| 1039 | Microcolin A | presence of N-methylvaline, cis-4-hydroxyproline, N-methylleucine, and threonine | 0 | L | NA | NA | NA | Linear | Natural | Isolated from a Venezuelan sample of the blue-green alga Lyngbya majwcnh | NA | Inhibitor of murine mixed Lymphocyteresponce and murine murine P-388 leukemia | In vitro | Murine mixed Lymphocyte | 1.5 nM | NA | Murine mixed Lymphocyte reaction | 22.6 nM | NA | 1517734 | 1992 |
| 1040 | Microcolin B | contained threonine, proline, N-methylvaline, and N- methylleucine | 0 | L | NA | NA | NA | Linear | Natural | Isolated from a Venezuelan sample of the blue-green alga Lyngbya majwcnh | NA | Inhibitor of murine mixed Lymphocyteresponce and murine murine P-388 leukemia | In vitro | Murine mixed Lymphocyte | 42.7 nM | NA | Murine mixed Lymphocyte reaction | 191.0 nM | NA | 1517734 | 1992 |
| 1042 | ISP region (Mutant D105) | EVVLQNRRGLDLLTAEQGGICLALQEKCCFYANKS | 35 | L | None | None | None | Linear | Protein Derived | Within the transmembrane (TM) protein of Mason-Pfizer monkey virus | T-cell and B-cell | Immunosuppressive effect on both T-cell and B-cell mitogenic response | In vitro | HeLa, COS-1, CV-1and BHK cells | NA | NA | NA | NA | NA | 1316462 | 1992 |
| 1043 | ISP region (Mutant D33) | LQNRRGLDLLT | 11 | L | None | None | None | Linear | Protein Derived | Within the transmembrane (TM) protein of Mason-Pfizer monkey virus | T-cell and B-cell | Immunosuppressive effect on both T-cell and B-cell mitogenic response | In vitro | HeLa, COS-1, CV-1and BHK cells | NA | NA | NA | NA | NA | 1316462 | 1992 |
| 1045 | Cyclolinopeptide A (CLA) | VPPFFLIIL | 9 | L | None | None | None | Cyclic | Natural | isolated from linseed oil | Cyclophilin A, IL-1α, IL-2 | it binds to cyclophilin A and inhibits the action of Interleukin-1-alpha and Interleukin-2 | Both | SRBC (Sheep red blood cells) | dose combinations: 0.1 mg/ml of CLA and 0.25 mM of MTX exhibited suppressive, synergistic action | 12-week-old BALB/c female mice | Secondary humoral immune response | NA | Methotrexate (MTX) | 21839548 | 2011 |
| 1046 | CLA analogue1 | LVPPFFLII | 9 | L | None | None | Ethylene bridge (-CH2-CH2-) between phenylalanine nitrogens | Cyclic | Synthetic | Analog of cyclolinopeptide A (CLA) | NA | NA | Both | SRBC (Sheep red blood cells) | NA | 12-week-old BALB/c female mice | Secondary humoral immune response | NA | NA | 21839548 | 2011 |
| 1048 | CLA analogue3 | LVPPFFLII | 9 | L | None | None | Ethylene bridge (-CH2-CH2-) between phenylalanine nitrogens | Linear | Synthetic | Analog of cyclolinopeptide A (CLA) | NA | NA | Both | SRBC (Sheep red blood cells) | NA | 12-week-old BALB/c female mice | Secondary humoral immune response | NA | NA | 21839548 | 2011 |
| 1050 | CLA analogue5 | LVPPFFLII | 9 | L | None | None | None | Linear | Synthetic | Analog of cyclolinopeptide A (CLA) | NA | NA | Both | SRBC (Sheep red blood cells) | NA | 12-week-old BALB/c female mice | Secondary humoral immune response | NA | NA | 21839548 | 2011 |
| 1051 | Vm24 | AAAISCVGSPECPPKCRAQGCKNGKCMNRKCKCYYC | 36 | L | None | Amidation | Four Disulfide bridges (between Cys6 and Cys26, Cys12 and Cys31, Cys16 and Cys33, and Cys21 and Cys36) | Linear | Natural | venom of the Mexican scorpion Vaejovis mexicanus smithi | K+ channel | Remarkable blocking potency and selectivity for Kv1.3 channels | Both | Mononuclear cells from human peripheral venous blood | 90% inhibition achieved at 100pM | Mouse model | Lethality test | No toxicity for 50 to 200 μg of protein per mouse (20 g body weight) | NA | 22540187 | 2012 |
| 1052 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Natural | Purified from venom of the scorpion Centruroides margaritatus | Kv1.3 channel | Inhibit both Th1 and Th2 cytokine production | NA | NA | NA | NA | NA | NA | NA | 12747950 | 2003 |
| 1053 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Synthetic | Recombinantnt was made by expressing the synthetic cDNA in Escherichia coli | Kv1.3 channel | Inhibit both Th1 and Th2 cytokine production | Both | Human peripheral blood mononuclear cells (PBMC), Purified T cells, Human monocytes, Human monocytic cell line, THP-1 | 0.013 nM for IL-2 when stimulation with PMA and ionomycin | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
| 1054 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Synthetic | Recombinantnt was made by expressing the synthetic cDNA in Escherichia coli | Kv1.3 channel | Inhibit both Th1 and Th2 cytokine production | Both | Human peripheral blood mononuclear cells (PBMC), Purified T cells, Human monocytes, Human monocytic cell line, THP-2 | 0.016 nM for IL-4 when stimulation with PMA and ionomycin | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
| 1055 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Synthetic | Recombinantnt was made by expressing the synthetic cDNA in Escherichia coli | Kv1.3 channel | Inhibit both Th1 and Th2 cytokine production | Both | Human peripheral blood mononuclear cells (PBMC), Purified T cells, Human monocytes, Human monocytic cell line, THP-3 | 0.5 nM for IL-2 production when stimulated with a-CD3 and VCAM-1 | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
| 1056 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Synthetic | Recombinantnt was made by expressing the synthetic cDNA in Escherichia coli | Kv1.3 channel | Inhibit both Th1 and Th2 cytokine production | Both | Human peripheral blood mononuclear cells (PBMC), Purified T cells, Human monocytes, Human monocytic cell line, THP-4 | 0.13 nM for IL-4 production when stimulated with a-CD3 and VCAM-1 | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
| 1057 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Synthetic | Recombinantnt was made by expressing the synthetic cDNA in Escherichia coli | Kv1.3 channel | Inhibit both Th1 and Th2 cytokine production | Both | Human peripheral blood mononuclear cells (PBMC), Purified T cells, Human monocytes, Human monocytic cell line, THP-5 | 4.9 nM for a-CD3/VCAM-1 induced proliferation | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
