513024-M

PD 151746

A cell-permeable, non-peptidic, and highly selective calpain inhibitor directed towards the calcium binding sites of calpain.

• Synonym(s): PD 151746, 3-(5-Fluoro-3-indolyl)-2-mercapto-(Z)-2-propenoic Acid
• Empirical Formula (Hill Notation): C₁₁H₈FNO₂
• CAS Number: 179461-52-0
• Molecular Weight: 205.19
• MDL number: MFCD03453564
• UNSPSC Code: 12352200

Properties

• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: orange
• solubility: DMSO: 200 mg/mL; methanol: 5 mg/mL
• storage temp.: −20°C
• InChI: 1S/C11H8FNO2S/c12-7-1-2-9-8(4-7)6(5-13-9)3-10(16)11(14)15/h1-5,13,16H,(H,14,15)/b10-3-
• InChI key: HWMQHECFXSVZGN-KMKOMSMNSA-N

Description

General description

A cell-permeable, non-peptidic, and highly selective calpain inhibitor directed towards the calcium binding sites of calpain. Displays over 20-fold greater selectivity for µ-calpain (Calpain I) over m-calpain (Calpain II) (K_i values, 260 nM and 5.33 µM, respectively). Has been shown to prevent cycloheximide induced apoptosis.

A cell-permeable, non-peptidic, and highly selective calpain inhibitor directed towards the calcium binding sites of calpain. Displays over 20-fold greater selectivity for calpain-1 (Cat. Nos. 208712 and 208713) over calpain-2 (Cat. Nos. 208715 and 208718) (K_i values: 260 nM and 5.33 µM, respectively). Has been shown to prevent cycloheximide-induced apoptosis.

Biochem/physiol Actions

Primary Target
calpain-1

Target K_i: 260 nM against calpain-1

Warning

Toxicity: Standard Handling (A)

Reconstitution

Unstable in solution; reconstitute just prior to use.

Other Notes

Squier, M.K., et al. 1999. J. Cell Physiol.178, 311.
Wang, K.K., et al. 1996. Proc. Natl. Acad. Sci. USA93, 6687.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable