A1925-1mg | Caspase-3/7 Inhibitor I [220509-74-0] Quimigen Portugal

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.

Product Citation

1. Yuhang Miao, Tao Ding, et al. "The Yeast and Hypha Phases ofCandida kruseiInduce the Apoptosis of Bovine Mammary Epithelial Cells via Distinct Signaling Pathways." Animals (Basel). 2023 Oct 15;13(20):3222. PMID: 37893947
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.

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	324.4
Cas No.	220509-74-0
Formula	C₁₄H₁₆N₂O₅S
Solubility	insoluble in H2O; ≥16.2 mg/mL in DMSO; ≥2.17 mg/mL in EtOH with gentle warming and ultrasonic
Chemical Name	5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl-1H-indole-2,3-dione
SDF	Download SDF
Canonical SMILES	COCC1CCCN1S(=O)(=O)C2=CC3=C(C=C2)NC(=O)C3=O
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

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.

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

Quality Control

Purity = 99.31%

Caspase-3/7 Inhibitor I [220509-74-0]

Referencia A1925-1mg

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Marca : APExBIO Technology