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Caspase-3/7 Inhibitor I , CAS 220509-74-0
Caspase-3/7 Inhibitor I , CAS 220509-74-0
Artikelnummer
BPS27741-2
Verpackungseinheit
10 mg
Hersteller
BPS Bioscience
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Background: Selectivity for caspases-3 and 7 involves unique hydrophobic residues in the S2 pocket surrounding the catalytic cysteine residue. Sequence alignments of the active site residues of the caspases strongly suggest that the basis of this selectivity is due to binding in the S2 subsite comprised of residues Tyr204, Trp206, and Phe256 which are unique to caspases 3 and 7. In some systems inhibition of caspases-3 and -7 can prevent apoptosis and may therefore have important therapeutic implications.
Biological Activity: Caspase-3/7 inbibitor I is a potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (Ki = 60 nM, IC50= 120 nM) and caspase-7 (Ki = 170 nM). It is a weaker inhibitor of caspase-9 (Ki = 3.1 µM). It 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). Also it has been reported to inhibit apoptosis in chondrocytes (44% inhibition at 10 µM and 98% inhibition at 50 µM).
CAS Number: 220509-74-0
Description: A potent, cell-permeable, and specific, reversible inhibitor of caspase-3 and caspase-7.
Format: crystalline solid.
Solubility: Soluble in DMSO
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: Caspase3, 7
Biosafety Level: Not applicable (BSL-1)
References: 1. Lee, D., et al. 2000. J. Biol. Chem. 275, 16007.
2. Lee, D., et al. 2001. J. Med. Chem. 44, 2015.
3. Jiang Y., Hansen T.V. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1626-9.
Background: Selectivity for caspases-3 and 7 involves unique hydrophobic residues in the S2 pocket surrounding the catalytic cysteine residue. Sequence alignments of the active site residues of the caspases strongly suggest that the basis of this selectivity is due to binding in the S2 subsite comprised of residues Tyr204, Trp206, and Phe256 which are unique to caspases 3 and 7. In some systems inhibition of caspases-3 and -7 can prevent apoptosis and may therefore have important therapeutic implications.
Biological Activity: Caspase-3/7 inbibitor I is a potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (Ki = 60 nM, IC50= 120 nM) and caspase-7 (Ki = 170 nM). It is a weaker inhibitor of caspase-9 (Ki = 3.1 µM). It 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). Also it has been reported to inhibit apoptosis in chondrocytes (44% inhibition at 10 µM and 98% inhibition at 50 µM).
CAS Number: 220509-74-0
Description: A potent, cell-permeable, and specific, reversible inhibitor of caspase-3 and caspase-7.
Format: crystalline solid.
Solubility: Soluble in DMSO
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: Caspase3, 7
Biosafety Level: Not applicable (BSL-1)
References: 1. Lee, D., et al. 2000. J. Biol. Chem. 275, 16007.
2. Lee, D., et al. 2001. J. Med. Chem. 44, 2015.
3. Jiang Y., Hansen T.V. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1626-9.
| Artikelnummer | BPS27741-2 |
|---|---|
| Hersteller | BPS Bioscience |
| Hersteller Artikelnummer | 27741-2 |
| Green Labware | Nein |
| Verpackungseinheit | 10 mg |
| Mengeneinheit | STK |
| Produktinformation (PDF) |
|
| MSDS (PDF) |
|
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Gernot Ensinger, M.Sc.
Laurent Haze
