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.

• Synonym(s): Cdk1/2 Inhibitor II, NU6102, 6-Cyclohexylmethoxy-2-(4ʹ-sulfamoylanilino)purine
• Empirical Formula (Hill Notation): C₁₈H₂₂N₆O₃S
• CAS Number: 444722-95-6
• Molecular Weight: 402.47
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 20 mg/mL
• shipped in: ambient
• storage temp.: 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)
• InChI key: OWXORKPNCHJYOF-UHFFFAOYSA-N

Description

General description

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).

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

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

Other Notes

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.

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable