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Merck

238806

Cdk2/9 Inhibitor

The Cdk2/9 Inhibitor, also referenced under CAS 507487-89-0, controls the biological activity of Cdk2/9. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

Cdk2/9 Inhibitor, (4-(2-Amino-4-methylthiazol-5-yl)pyrimidin-2-yl)-(3-nitrophenyl)amine, Cdk7 Inhibitor III

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About This Item

Empirical Formula (Hill Notation):
C14H12N6O2S
CAS Number:
507487-89-0
Molecular Weight:
328.35
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, protect from light

Key Documents

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InChI key

DYTKVFHLKPDNRW-UHFFFAOYSA-N

InChI

1S/C14H12N6O2S/c1-8-12(23-13(15)17-8)11-5-6-16-14(19-11)18-9-3-2-4-10(7-9)20(21)22/h2-7H,1H3,(H2,15,17)(H,16,18,19)

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

yellow

solubility

DMSO: 25 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

General description

A cell-permeable aminopyrimidinyl compound that acts as a potent and ATP-competitive inhibitor of Cdk2/E and Cdk9/T1 (Ki = 2 nM and 4 nM, respectively). It also inhibits GSK-3β, Cdk4/D1, Cdk7/H, Cdk1/B, and Abl at higher concentrations (Ki = 20, 53, 70, 80, and 160 nM, respectively), but exhibits little activity towards 9 other kinases (Ki >1.0 µM). Shown to inhibit phosphorylation of cellular Cdk substrates, pRb and RNA polymerase II, and Cdk2-mediated S-phase transition.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Cdk2/E and Cdk9/T1
Product competes with ATP.
Reversible: no
Target Ki: 2 nM and 4 nM against Cdk2/E and Cdk9/T1, respectively

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Kontopidis, G., et al. 2006. Chem. Biol.13, 201.
Wang, S., et al. 2004. J. Med. Chem.47, 1662.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

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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