| 1002 | Cyclosporin A (CsA) | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | Fungus | Reduction of the IL-2 surface receptor CD25 expression (76%±11 after 24 hrs and 62%±7.3 after 36 hrs), also reduces TNF-α expression (23%±1.8) | Inhibits the production of IL-2 | In vitro | Human peripheral Lymphocytes and purified T cells | NA | None | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 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 |
| 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 |
| 1036 | Cyclosporin A | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | From fungus Trichoderma polysporum | Inhibit IL-2 production by activated CD4+ T-cells | Inhibiting the calcineurin pathway | Both | Peripheral blood mononuclear cells (PBMCs) | 61.8 nM for CD4+ T cell activation of IL-2 production | C57/B6 mice | MIC assay, Immunosuppression and toxicity test | NA | NA | 18599825 | 2008 |
| 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 |
| 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 |
| 1044 | Cyclosporin A | cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | From fungus Trichoderma polysporum | Ca2+-dependent permeability transition | Inhibit the Ca2+ dependent permeability transition | In vivo | NA | NA | Male Sprague-Dawley rat | NA | NA | NA | 2470734 | 1989 |
| 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 |
| 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 |
| 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 |
| 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 |
| 1060 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Natural | From venom of the new world scorpion Centruroides margaritatus | Kv1.3 channels | Blocks with high affinity and specificity the Kv1.3 channel | In vitro | Human peripheral T-Lymphocytes, rat brain synaptic plasma membrane vesicles, bovine aortic sarcolemmal membrane vesicle | 36 pM | NA | competition binding with Kv1.3 (Potassium channel) | NA | NA | 8360176 | 1993 |
| 1061 | Charybdotoxin (ChTX) | EFTNVSCTTSKECWSVCQRLHNTSRGKCMNKKCRCYS | 37 | L | None | None | None | Linear | Natural | Isolated from venom of the old world scorpion Leiurusguinqwstriutus var. hebraeus | Kv1.3 channels | Inhibit high conductance, Ca2+- activated K+ (Maxi-K) channel | In vitro | Human peripheral T-Lymphocytes, rat brain synaptic plasma membrane vesicles, bovine aortic sarcolemmal membrane vesicle | NA | NA | competition binding with Kv1.4 ((Potassium channel) | NA | NA | 8360176 | 1993 |
| 1062 | Charybdotoxin (ChTX) | EFTNVSCTTSKECWSVCQRLHNTSRGKCMNKKCRCYS | 37 | L | None | None | None | Linear | Natural | Venom of the scorpion Leiurusquin questriatus var. hebraeus | K+ channels | Potent selective block of apamin-insensitive Ca2+- activated K+ channels | In vitro | GH3 pitutary cells and aortic smooth muscle | NA | NA | NA | NA | NA | 2453055 | 1988 |
