Name: Caspase-3/7 Inhibitor I
Price: 413.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    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).
    
    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.
- Properties
  - Alternative Name
    
    5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl-1H-indole-2,3-dione
    
    CAS Number
    
    220509-74-0
    
    Molecular Formula
    
    C14H16N2O5S
    
    Molecular Weight
    
    324.4
    
    Appearance
    
    A solid
    
    Purity
    
    99.31%
    
    Solubility
    
    insoluble in H2O; ≥16.2 mg/mL in DMSO; ≥2.17 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Zheng X, Zhong T, et al. "Bnip3 mediates doxorubicin-induced cardiomyocyte pyroptosis via caspase-3/GSDME." Life Sci. 2019 Dec 17;242:117186. PMID:31862454
    2. DXie L, Dai H, et al. "MARCH1 encourages tumour progression of hepatocellular carcinoma via regulation of PI3K-AKT-β-catenin pathways." J Cell Mol Med. 2019 May;23(5):3386-3401. PMID:30793486
    3. Dang Q, Song W, et al. "Kaempferol suppresses bladder cancer tumor growth by inhibiting cell proliferation and inducing apoptosis". Molecular carcinogenesis, 2014.

Caspase-3/7 Inhibitor I

Caspase-3/7 Inhibitor I

Background

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