526523

PIM1/2 Kinase Inhibitor V

The PIM1/2 Kinase Inhibitor V, also referenced under CAS 327033-36-3, controls the biological activity of PIM1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): PIM1/2 Kinase Inhibitor V, (Z)-5-(3-Trifluoromethylbenzylidene)thiazolidine-2,4-dione, SMI-4a, SMI-4a, (Z)-5-(3-Trifluoromethylbenzylidene)thiazolidine-2,4-dione
• Empirical Formula (Hill Notation): C₁₁H₆F₃NO₂S
• CAS Number: 327033-36-3
• Molecular Weight: 273.23
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: light beige
• solubility: DMSO: 25 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C11H6F3NO2S/c12-11(13,14)7-3-1-2-6(4-7)5-8-9(16)15-10(17)18-8/h1-5H,(H,15,16,17)/b8-5+
• InChI key: NGJLOFCOEOHFKQ-VMPITWQZSA-N

Description

General description

A cell-permeable thiazolidinedione compound that acts as a potent, ATP-competitive inhibitor against Pim-1/2 kinases (IC₅₀ = 24 nM and 100 nM against Pim-1 and Pim-2, respectively), while exhibiting little or no activity against a panel of 58 other kinases (≤20% inhibition at 5 µM). One hour inhibitor treatment (0.5 µM) of HEK-293T cultures at the end of a 4 hour ³²PO₄ incubation period results in nearly complete inhibition of the autophosphorylation of overexpressed Pim-1. Comparing to Inhibitor VI (Cat. No. 526524), Inhibitor V is less reactive towards DYRK1α (20% vs. 68% inhibition with respective inhibitor at 5 µM) and more potent in PC3 human prostate cancer cell killing (IC₅₀ = 17 vs. 48 µM with respective inhibitor).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Other Notes

Lin,Y., et al. 2009. Blood In press.
Xia, Z., et al. 2009. J. Med. Chem.52, 74.

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable