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Caspase-3/7 Inhibitor ICaspase-3/7 inhibitor

Caspase-3/7 Inhibitor I

Catalog No. A1925
Size Price Stock Qty
10mM (in 1mL DMSO) $260.00 In stock
Evaluation Sample $28.00 In stock
1mg $85.00 In stock
5mg $225.00 In stock
10mg $375.00 In stock
25mg $600.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

Dang Q, Song W, Xu D, et al. Kaempferol suppresses bladder cancer tumor growth by inhibiting cell proliferation and inducing apoptosis[J]. Molecular carcinogenesis, 2014.

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Related Biological Data

caspase 3/7
Human bladder cancer cells were treated with caspase 3/7 inhibitor 1 (10 μMM) or kaempferol (100 μM) for 48 h; In combination treatment, caspase 3/7 inhibitor 1 was added 1 h prior to kaempferol treatment. At the end of treatment, cell extracts were prepared for caspase-7 activity assay. Error bars represent SEs. *P < 0.05.

Chemical structure

Caspase-3/7 Inhibitor I

Biological Activity

A potent, cell-permeable, and specific, reversible inhibitor of caspase-3 (Ki = 60 nM) and caspase-7 (Ki = 170 nM).
Targets Caspase-3 Caspase-7        
Ki 60nM 170nM        

Protocol

Cell experiment: [1]

Cell lines

Human Jurkat T cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

50 μM

Applications

Cells were treated with camptothecin to induce cell death, and the ability of the compound to inhibit cell death was assessed by FACS analysis. A good correlation exists between relative cell-based activities of the compound with its in vitro isolated caspase 3 or 7 inhibition activites. The compound exhibited 54% inhibition of apoptosis at 50 μM and 22% at 10 μM.

Animal experiment:

Animal models

Dosage form

Applications

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Lee D, Long S A, Murray J H, et al. Potent and selective nonpeptide inhibitors of caspases 3 and 7. Journal of medicinal chemistry, 2001, 44(12): 2015-2026.

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Chemical Properties

Cas No. 220509-74-0 SDF Download SDF
Chemical Name 5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl-1H-indole-2,3-dione
Canonical SMILES COCC1CCCN1S(=O)(=O)C2=CC3=C(C=C2)NC(=O)C3=O
Formula C14H16N2O5S M.Wt 324.4
Solubility >16.2mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Research Update

1. Tissue inhibitor of metalloproteinases-3 moderates the proinflammatory status of macrophages. Am J Respir Cell Mol Biol. 2013 Nov;49(5):768-77. doi: 10.1165/rcmb.2012-0377OC.
Abstract
TIMP-3 is involved in the regulation of inflammation where, in the absence of TIMP3, macrophages are more likely to be differentiated into proinflammatory (M1) cells.
2. [X-linked inhibitor of apoptosis protein (XIAP) and Survivin suppression on human pancreatic cancer cells Panc-1 proliferation and chemosensitivety]. Beijing Da Xue Xue Bao. 2013 Apr 18;45(2):242-9.
Abstract
The effects of inhibition of XIAP, Survivin or both on cell proliferation and chemosensitivity of Panc-1 cells have been investigated and compared.
3. [Effect of aurora kinase B inhibitor AZD1152 in the treatment of cisplatin-resistant ovarian carcinoma]. Zhonghua Fu Chan Ke Za Zhi. 2013 Jan;48(1):46-50.
Abstract
The effect of AZD1152 alone or in combination with cisplatin has been investigated in the treatment of cisplatin-resistant ovarian carcinoma.
4. Targeting X-linked inhibitor of apoptosis protein inhibits pancreatic cancer cell growth through p-Akt depletion. World J Gastroenterol. 2012 Jun 21;18(23):2956-65. doi: 10.3748/wjg.v18.i23.2956.
Abstract
The regulation of XIAP gene by lentivirus-mediated shRNA has been investigated for its effect in the treatment of pancreatic cancer.

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).

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.