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.
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Synonym(s):
Caspase-3/7 Inhibitor I, 5-[(S)-(+)-2-(Methoxymethyl)pyrrolidino]sulfonylisatin
Empirical Formula (Hill Notation):
C14H16N2O5S
Recommended Products
Quality Level
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
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
InChI key
SLQMNVJNDYLJSF-VIFPVBQESA-N
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
caspase-3
caspase-3
Product does not compete with ATP.
Reversible: yes
Target Ki: 60 nM, 170 nM, against caspase-3 and caspase-7, respectively
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Sequence
5-[(S)-(+)-2-(Methoxymethyl)pyrrolidino]sulfonylisatin
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Lee, D., et al. 2001. J. Med. Chem.44, 2015.
Lee, D., et al. 2000. J. Biol. Chem. 275, 16007.
Lee, D., et al. 2000. J. Biol. Chem. 275, 16007.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
wgk_germany
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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