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 |
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 |
1063 | Kalata B1 | GLPVCGETCVGGTCNTPGCTCSWPVCTRN | 29 | L | None | None | Three cystine knot Disulfide connectivity (CI-CIV, CII-CV and CIII-CVI) | Cyclic | Natural | From Oldenlandia affinis Plant Extract | NA | Inhibits the growth of the Lymphocytes in a cytostatic fashion | In vitro | Human Peripheral Blood Mononuclear Cells | 3.9±0.5 micromolar for antiproliferative effect on PBMC | NA | Cell Proliferation assay, Cell division assay | 14 micromolar of the peptide are cytotoxic to the cells | NA | 22272797 | 2012 |
1125 | Iberiotoxin (Venom peptide) | XFTDVDCSVSKECWSVCKDLFGVDRGKCMGKKCRCYQ | 37 | L | None | None | X=Pyroglutamic acid and disulfile linkage at Disulfide bridges: Cys7 - Cys28, Cys13 - Cys33, Cys17 - Cys35 | Linear | Natural | Buthus tamulus (scorpion) | Blocker of several BK channels | Bloackion channels | Both | NA | NA | NA | NA | NA | NA | 24333193 | 2014 |
1126 | Kalata B1 (Cyclotide) | GLPVCGETCVGGTCNTPGCTCSWPVCTRN | 29 | L | None | None | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic | Natural | Oldenlandia affinis (plant) | IL-2 | Antiproliferative, IL2-dependent mechanism | Both | NA | NA | NA | NA | NA | NA | 24333193 | 2014 |
1128 | Magatoxin (Venom peptide) | IINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | disulfide bridges between Cys 7-Cys29, Cys13-Cys34 and Cys17-Cys36 | Linear | Natural | Centruroides margaritatus (scorpion) | K+ channel | Potassium channel blocker | In vivo | NA | NA | NA | NA | NA | NA | 24333193 | 2014 |