| Identification | Back Directory | [Name]
Caspase-3/7 Inhibitor I | [CAS]
220509-74-0 | [Synonyms]
abs814634
(S)-Caspase-3/7 Inhibitor I
MMPSI, Caspase-3/7 Inhibitor I
5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl-1H-indole-2
5-[(2S)-2-(METHOXYMETHYL)PYRROLIDIN-1-YL]SULFONYL-1H-INDOLE-2;3-DIONE
1H-Indole-2,3-dione, 5-[[(2S)-2-(methoxymethyl)-1-pyrrolidinyl]sulfonyl]-
Pyrrolidine,1-[(2,3-dihydro-2,3-dioxo-1H-indol-5-yl)sulfonyl]-2-(MethoxyMethyl)-,(2S)- | [Molecular Formula]
C14 H16 N2 O5 S | [MDL Number]
MFCD22581511 | [MOL File]
220509-74-0.mol | [Molecular Weight]
324.35 |
| Chemical Properties | Back Directory | [density ]
1.415±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥16.2 mg/mL in DMSO; ≥2.17 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid | [pka]
8.66±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
MMPSI is a potent and selective small molecule caspase 3 and caspase 7 inhibitor with an IC50 of 1.7 μM for human caspase-3. MMPSI can significantly reduce ischemia-reperfusion-induced infarct size in the isolated rabbit heart, and reduce apoptosis in both the ischemic myocardium and isolated cardiomyocytes. MMPSI can be used for researching cardioprotection[1]. | [Biological Activity]
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. [1] [2] in some systems inhibition of caspases-3 and -7 can prevent apoptosis and may therefore have important therapeutic implications. [3]a potent, cell-permeable, and specific, reversible inhibitor of caspase-3 (ki = 60 nm) and caspase-7 (ki = 170 nm). | [target]
Caspase-3 | [IC 50]
human Caspase-3: 1.7 μM (IC50) | [storage]
Store at -20°C | [References]
1. lee, d., et al. 2001. j. med. chem. 44, 2015. 2. lee, d., et al. 2000. j. biol. chem. 275, 16007. 3. clements, k. m., burton‐wurster, n., nuttall, m. e., & lust, g. (2005). caspase‐3/7 inhibition alters cell morphology in mitomycin?\c treated chondrocytes. journal of cellular physiology, 205(1), 133-140. |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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