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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C11H6F3NO2S
CAS Number:
Molecular Weight:
273.23
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
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Quality Level

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

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)


Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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