| 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 |
| 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 |
| 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 |
| 1047 | CLA analogue2 | LVPPffLII | 9 | Mix | 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 |
| 1049 | CLA analogue4 | LVPPffLII | 9 | Mix | 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 |
| 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 |
| 1058 | 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-6 | 0.5 nM anti-CD3 mediated redirected cytolysis of CD8(+) T cells | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
| 1059 | 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-7 | 0.5 nM anti-CD3 mediated redirected cytolysis of T cells | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
| 1065 | Cyclolinopeptide A (CLA) | VPPFFLIIL | 9 | L | None | None | None | Cyclic | Synthetic | NA | NA | Inhibition of the action of interleukin-1 and interleukin-2 | Both | SRBC (sheep red blood cells) | NA | CBA/Iiw mice 8-10 weeks | Humoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) test | NA | NA | 8441706 | 1992 |
| 1068 | [D-Phe3]CyA A | VFfAGP | 6 | Mix | None | None | None | Cyclic | Synthetic | NA | NA | Not investigated | Both | SRBC (sheep red blood cells) | NA | CBA/Iiw mice 8-10 weeks | Humoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) test | NA | NA | 8441706 | 1992 |
| 1070 | [D-Ser]CyA B | FFFPIPs | 7 | Mix | None | None | None | Cyclic | Synthetic | NA | NA | Not investigated | Both | SRBC (sheep red blood cells) | NA | CBA/Iiw mice 8-10 weeks | Humoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) test | NA | NA | 8441706 | 1992 |
| 1073 | Retro-[D-Phe3]CyA A | fFVPGA | 6 | Mix | None | None | None | Cyclic | Synthetic | NA | NA | Not investigated | Both | SRBC (sheep red blood cells) | NA | CBA/Iiw mice 8-10 weeks | Humoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) test | NA | NA | 8441706 | 1992 |
| 1074 | Retro-[D-Phe3]CyA A | fFVPGA | 6 | Mix | None | None | None | Linear | Synthetic | NA | NA | Not investigated | Both | SRBC (sheep red blood cells) | NA | CBA/Iiw mice 8-10 weeks | Humoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) test | NA | NA | 8441706 | 1992 |
| 1075 | CKS-17 | LQNRRGLDLLFLKEGGL | 17 | L | None | Conjugated to HSA (human serum albumin) | None | Linear | Synthetic | Homologous region found in the transmembrane envelope proteins of murine, feline, and human retro- viruses HTLV-1 and HTLV-2, and an endogenous C-type human retrovirus | Lymphocyte | Inhibits the Proliferation of Purified Lymphocytes | In vitro | Mononuclear Cells, Lymphocytes, Human Neutrophils, Lymphoblastoid cell line-Jurkat cell, | 10 micromolar in Lymphocyte proliferation assays | None | Lymphocyte Proliferation assay | NA | NA | 1921761 | 1991 |
| 1076 | CKS-17 | LQNRRGLDLLFLKEGGL | 17 | L | None | Conjugated to HSA (human serum albumin) | None | Linear | Synthetic | Homologous region found in the transmembrane envelope proteins of murine, feline, and human retro- viruses HTLV-1 and HTLV-2, and an endogenous C-type human retrovirus | Protein Kinase C | Inhibits Protein Kinase C activity | In vitro | Human Neutrophils, Lymphoblastoid cell line-Jurkat cell | 3 micromolar in the in vitro protein kinase C assay | None | Protein kinase assay | NA | NA | 1921761 | 1991 |
| 1077 | CKS-17 | LQNRRGLDLLFLKEGGL | 17 | L | None | Conjugated to BSA (bovine serum albumin) | None | Linear | Synthetic | Homologous region found in the transmembrane envelope proteins of murine, feline, and human retro- viruses HTLV-1 and HTLV-2, and an endogenous C-type human retrovirus | Protein Kinase C | inhibition of IL-1-mediated responses, due to inactivation of PKC. inactivates PKC directly without competing with its cofactors. | In vitro | Human Neutrophils, Lymphoblastoid cell line-Jurkat cell | 3 micromolar in the in vitro protein kinase C assay | None | Protein kinase assay | NA | NA | 1921761 | 1991 |
| 1078 | CSK-17 | LQNRRGLDLLFLKEGGL | 18 | L | None | None | None | Linear | Synthetic | NA | NA | Inhibition of human Lymphocyte | NA | NA | NA | NA | NA | NA | NA | 2421920 | 1986 |
| 1087 | MHC-binding analog (Ac1-9[4Y]) | ASQYRPSQR | 9 | L | Acetylation | None | None | Linear | Synthetic | Analog of Ac1-9 | IL-10 and IL-3 | peptide-induced regulatory cells suppress the response of naive T cells and leads to the generation of IL-10-secreting regulatory cells | Both | purified T cells | NA | Tg4 transgenic mouse | CD4 T cell Proliferation assays, Cytokine protein levels assays | NA | NA | 12538682 | 2003 |
| 1107 | HAP-1 | SFHQFARATLAS | 12 | L | Addition of Cysteine | None | None | Linear | Synthetic | M13 peptide phage library of a rabbit synovial fibroblast cell line | NA | Not Available | In vivo | NA | NA | Female Wistar rat | NA | NA | NA | 245138095 | 2014 |
