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Caspase-3/7 Inhibitor

CAS number:220509-74-0    molecular formula:C14H16N2O5S

overview

compound introduction

MMPSI 是一种有效且具有选择性的 caspase 3 和 caspase 7 小分子抑制剂,对人 caspase-3 的 IC50 为 1.7 μM。MMPSI 能显著减少离体兔心脏缺血再灌注诱导的梗死面积,降低缺血心肌和离体心肌细胞凋亡 (apoptosis)。MMPSI 可用于心脏保护研究。 A potent, cell-permeable, and specific, reversible inhibitor of caspase-3 (Ki = 60 nM) and caspase-7 (Ki = 170 nM). A potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (KI(app) = 60 nM) and caspase-7 (KI(app) = 170 nM). Inhibits caspase-9 to a lesser extent (Ki(app) = 3.1 µM). Has only a trivial effect (Ki(app) >25 mM) on the activities of caspase-1, caspase-2, caspase-4, caspase-6, and caspase-8. Reported to inhibit apoptosis in camptothecin treated Jurkat cells (IC50 ~50 µM). Also 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.

Specs

Chinese alias5-[[((2S)-2-(甲氧甲基)-1-吡咯烷基]磺酰基]-1H-吲哚-2,3-二酮 | Caspase-3/7 抑制剂
English aliasAKOS040744939 | HY-103346 | 5-[(S)-(+)-2-(Methoxymethyl)pyrrolidino]sulfonylisatin | DTXSID50431688 | Isatin Sulfonamide 16 | SLQMNVJNDYLJSF-VIFPVBQESA-N | 5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl-1H-indole-2,3-dione | SCHEMBL3681388 | (S)-5-[1-(
CAS number220509-74-0molecular formulaC14H16N2O5S
molecular weight324.35 g/molExact mass≥97%
PSA101.000 Ųlogp0.300

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