217713

Cdk1/2 Inhibitor II, NU6102

The Cdk1/2 Inhibitor II, NU6102, also referenced under CAS 444722-95-6, controls the biological activity of Cdk1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinonimo/i: Cdk1/2 Inhibitor II, NU6102, 6-Cyclohexylmethoxy-2-(4ʹ-sulfamoylanilino)purine
• Formula empirica (notazione di Hill): C₁₈H₂₂N₆O₃S
• Numero CAS: 444722-95-6
• Peso molecolare: 402.47
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: white
• Solubilità: DMSO: 20 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C
• InChI: 1S/C18H22N6O3S/c19-28(25,26)14-8-6-13(7-9-14)22-18-23-16-15(20-11-21-16)17(24-18)27-10-12-4-2-1-3-5-12/h6-9,11-12H,1-5,10H2,(H2,19,25,26)(H2,20,21,22,23,24); OWXORKPNCHJYOF-UHFFFAOYSA-N

Descrizione

Descrizione generale

A cell-permeable 2,6-disubstituted purine compound that displays antiproliferative properties. Acts as a potent and ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A3 (IC₅₀ = 9.5 nM and 5.4 nM). Displays greater selectivity for Cdk1/2 over other kinases tested (IC₅₀ = 600 nM, 800 nM, 900 nM and 1.6 µM for ROCKII, PDK1, DYRK1A and Cdk4/D1, respectively). Shown to inhibit human MCF-7 breast carcinoma cell growth with a GI₅₀ of 8 µM.

A cell-permeable purine analog that displays anti-proliferative properties and acts as a potent and ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A3 (IC₅₀ = 9.5 nM and 5.4 nM, respectively). Displays greater selectivity for Cdk′s over other kinases tested (IC₅₀ = 30 nM, 600 nM, 800 nM, 900 nM, and 1.6 µM for Cdk2/A, ROCKII, PDK1, DYRK1A, and Cdk4/D1, respectively). Shown to inhibit human MCF-7 breast carcinoma cell growth (GI₅₀ of 8 µM).

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
Cdk1/cyclin B, Cdk2/cyclin A3

Product competes with ATP.

Reversible: no

Target IC₅₀: 9.5 nM, 5.4 nM against Cdk1/cyclin B, Cdk2/cyclin A3, respectively

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Carcinogenic / Teratogenic (D)

Ricostituzione

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

Altre note

Hardcastle, I.R., et al. 2004. J. Med. Chem.47, 3710.
Sayle, K.L., et al. 2003. Bioorg. Med. Chem. Lett.13, 3079.
Davies, T.G., et al. 2002. Nat. Struct. Biol.9, 745.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable