Caspase-3/7 Inhibitor I is a potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (KI(app)= 60 nM) and caspase-7 (KI(app) = 170 nM). It is a weaker inhibitor of caspase-9 (KI(app) = 3.1 μM). Caspase-3/7 Inhibitor I has only a trivial effect (Ki(app) >25 μM) 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). Caspase-3/7 Inhibitor I has also 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.
1. Lee, D., et al. 2000. J. Biol. Chem. 275: 16007-16014. PMID: 10821855
2. Lee, D., et al. 2001. J. Med. Chem. 44: 2015-2026. PMID: 11384246
3. Lührmann, Anja., et al., 2004. Necrotic death of Rhodococcus equi-infected macrophages is regulated by virulence-associated plasmids. Infection and immunity. 72(2): 853-62. PMID: 14742529
看其他用户如何应用Caspase-3/7 Inhibitor I (CAS 220509-74-0).点击进入浏览PubMed条目 .
PMID: # 24587248 Wang, J. et al. 2014. PLoS ONE. 9: e90146.
PMID: # 23658722 Boehm, D. et al. 2013. PLoS ONE. 8: e62303.
PMID: # 22335196 Wang, J. et al. 2012. J. Pineal Res. 53: 77-90.
PMID: # 32345661 Life Sci Alliance. 3: