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.

• Synonyme(s) : Caspase-3/7 Inhibitor I, 5-[(S)-(+)-2-(Methoxymethyl)pyrrolidino]sulfonylisatin
• Formule empirique (notation de Hill): C₁₄H₁₆N₂O₅S
• Numéro CAS: 220509-74-0
• Poids moléculaire : 324.35
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow
• Solubilité: methanol: 10 mg/mL; DMSO: 200 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −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
• Clé InChI: SLQMNVJNDYLJSF-VIFPVBQESA-N

Description

Description générale

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.

Actions biochimiques/physiologiques

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

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Séquence

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.

Autres remarques

Lee, D., et al. 2001. J. Med. Chem.44, 2015.
Lee, D., et al. 2000. J. Biol. Chem. 275, 16007.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable