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产品描述:

产品名称:(S)-Caspase-3/7 Inhibitor I

靶点: Caspase-3,Caspase-7

CAS号: 220509-74-0

描述:

Caspase-3/7 inbibitor I is a potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (KI(app) = 60 nM) and caspase-7 (KI(app) = 170 nM). Is a weaker inhibitor of caspase-9 (Ki(app) = 3.1 mM). It Has only a trivial effect (Ki(app) >25 mM) on the activities of caspase-1, caspase-2, caspase-4, caspase-6, and caspase-8. It has been shown to inhibit apoptosis in camptothecin treated Jurkat cells (IC50 ~50 µM). Also it has been reported to inhibit apoptosis in chondrocytes (44% inhibition at 10 µM and 98% inhibition at 50 µM). Selectivity for caspases-3 and 7 involves unique hydrophobic residues in the S2 pocket surrounding the catalytic cysteine residue. In some systems inhibition of caspases-3 and -7 can prevent apoptosis and may therefore have important therapeutic implications. 

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

外观: Yellow solid

分子式: C₁₄H₁₆N₂O₅S

密度: 1.42 g/cm³ (Predicted)

分子量: 324.4

熔点: 228.25° C (Predicted)

纯度: 98%

沸点: 533.50° C (Predicted)

折射率: n²⁰_D 1.60 (Predicted)

储存/保存方法: Store at -20° C

IC50: caspase-7: IC₅₀ = 170 nM (human); caspase-3: IC₅₀ = 84.9 nM (human); apoptosis: IC₅₀ = ~50 μM (camptothecin treated Jurkat cells)

PK值: pK_a: 8.66 (Predicted)

Ki 数据: Caspase-9: K_i= 1100 nM (human); caspase-7: K_i= 170 nM; caspase-3: K_i= 60 nM

可溶性/溶解性: DMSO :≥16.2mg/mL

MDL: MFCD22581511

PubChem CID: 9840223

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