219491

Cdk/Crk Inhibitor

The Cdk/Crk Inhibitor, also referenced under CAS 784211-09-2, controls the biological activity of Cdk/Crk. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(e): Cdk/Crk Inhibitor, 1-(2,6-Dichlorophenyl)-1,5-dihydro-6-((4-(2-hydroxyethoxy)phenyl)methyl)-3-(1-methylethyl)-4H-pyrazolo[3,4-d]pyrimidin-4-one, RGB-286147, Cdk7 Inhibitor IV
• Empirische Formel (Hill-System): C₂₃H₂₂Cl₂N₄O₃
• CAS-Nummer: 784211-09-2
• Molekulargewicht: 473.35
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥95% (HPLC)
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: white
• Löslichkeit: DMSO: 5 mg/mL
• Versandbedingung: ambient
• Lagertemp.: −20°C

Beschreibung

Allgemeine Beschreibung

A cell-permeable pyrazolo-pyrimidinone compound that acts as a potent, selective, and ATP-competitive inhibitor of Cdks (IC₅₀ = 48 nM, 15 nM, 9 nM, 10 nM, 71 nM, and 9 nM for Cdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9, respectively). It inhibits Cdk4/D1, Cdk6/D3, and GSK-3β only at much higher concentrations (IC₅₀ = 839 nM, 282 nM, and 754 nM, respectively) and exhibits little activity towards a panel of 60 other kinases. A broad-spectrum growth inhibitor toward tumor cells, but not non-transformed quiescent fibroblasts.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
Cdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9

Product competes with ATP.

Reversible: no

Target IC₅₀: 48 nM, 15 nM, 9 nM, 10 nM, 71 nM, and 9 nM for Cdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9, respectively

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

Caligiuri, M., et al. 2005. Chem. Biol.12, 1103.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 1
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable