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.

• Synonym(s): Caspase-3/7 Inhibitor I, 5-[(S)-(+)-2-(Methoxymethyl)pyrrolidino]sulfonylisatin
• Empirical Formula (Hill Notation): C₁₄H₁₆N₂O₅S
• CAS Number: 220509-74-0
• Molecular Weight: 324.35
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• 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

Description

General description

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

A potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (K_I(app) = 60 nM) and caspase-7 (K_I(app) = 170 nM). Inhibits caspase-9 to a lesser extent (K_i(app) = 3.1 µM). Has only a trivial effect (K_i(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

Product does not compete with ATP.

Reversible: yes

Target K_i: 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.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable