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Merck
CN

218826

Caspase-3/7 Inhibitor I

The Caspase-3/7 Inhibitor I, also referenced under CAS 220509-74-0, controls the biological activity of Caspase-3/7. This small molecule/inhibitor is primarily used for Cancer applications.

别名:

Caspase-3/7 Inhibitor I, 5-[(S)-(+)-2-(Methoxymethyl)pyrrolidino]sulfonylisatin

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关于此项目

经验公式(希尔记法):
C14H16N2O5S
化学文摘社编号:
分子量:
324.35
UNSPSC Code:
12352200
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产品名称

Caspase-3/7 Inhibitor I, The Caspase-3/7 Inhibitor I, also referenced under CAS 220509-74-0, controls the biological activity of Caspase-3/7. This small molecule/inhibitor is primarily used for Cancer applications.

InChI key

SLQMNVJNDYLJSF-VIFPVBQESA-N

InChI

1S/C14H16N2O5S/c1-21-8-9-3-2-6-16(9)22(19,20)10-4-5-12-11(7-10)13(17)14(18)15-12/h4-5,7,9H,2-3,6,8H2,1H3,(H,15,17,18)/t9-/m0/s1

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

methanol: 10 mg/mL
DMSO: 200 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

Biochem/physiol Actions

Target Ki: 60 nM, 170 nM, against caspase-3 and caspase-7, respectively
Cell permeable: yes
Primary Target
caspase-3
Product does not compete with ATP.
Reversible: yes

Disclaimer

Toxicity: Standard Handling (A)

General description

A potent, cell-permeable, and specific, reversible inhibitor of caspase-3 (Ki = 60 nM) and caspase-7 (Ki = 170 nM).
A potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (KI(app) = 60 nM) and caspase-7 (KI(app) = 170 nM). Inhibits caspase-9 to a lesser extent (Ki(app) = 3.1 µM). Has only a trivial effect (Ki(app) >25 mM) on the activities of caspase-1, caspase-2, caspase-4, caspase-6, and caspase-8. Reported to inhibit apoptosis in camptothecin treated Jurkat cells (IC50 ~50 µM). Also 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.

Other Notes

5-[(S)-(+)-2-(Methoxymethyl)pyrrolidino]sulfonylisatin
Lee, D., et al. 2001. J. Med. Chem.44, 2015.
Lee, D., et al. 2000. J. Biol. Chem. 275, 16007.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

存储类别

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable


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