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产品描述:

产品名称:Caspase-3/7 Inhibitor I

参考文献: 1.Lee, D.,Long, S.A.,Adams, J.L., et al. Potent and selective nonpeptide inhibitors of caspases 3 and 7 inhibit apoptosis and maintain cell functionality. The Journal of Biological Chemisty 275, 16007-16014 (2000).
2.Lee, D.,Long, S.A.,Murray, J.H., et al. Potent and selective nonpeptide inhibitors of caspases 3 and 7. Journal of Medicinal Chemistry 44, 2015-2026 (2001).

靶点: Caspase-3,Caspase-7

CAS号: 1110670-49-9

描述:

Caspase-3/7 inhibitor I is a potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (K_i(app) = 60 nM; IC₅₀ = 120 nM) and caspase-7 (K_i(app) = 170 nM). It is a weaker inhibitor of caspase-9 (K_i(app) = 3.1 μM) and caspase-1, caspase-2, caspase-4, caspase-6, and caspase-8 (K_i(app)s ≥25 μM). Caspase-3/7 inhibitor I inhibits apoptosis in camptothecin-treated Jurkat cells (IC₅₀ = ~50 µM) and in chondrocytes (44% inhibition at 10 µM and 98% inhibition at 50 µM). The basis for the unique selectivity of this compound for caspases 3 and 7 involves the recognition of three distinct hydrophobic residues in the S2 pocket surrounding the catalytic cysteine residue.

中文别名: 5-[[2-(methoxymethyl)-1-pyrrolidinyl]sulfonyl]-1H-indole-2,3-dione

外观: solid

分子式: C₁₄H₁₆N₂O₅S

分子量: 324.4

纯度: ≥98%

储存/保存方法: Store at -20℃

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