539644

UCN-01

A cell-permeable Staurosporine derived anticancer agent that reversibly and ATP-competitively inhibits several protein kinases.

• Sinônimo(s): UCN-01, 7-Hydroxystaurosporine, Staurosporine, 7β-Hydroxy, Streptomyces sp., Chk1 Inhibitor VI, Chk2 Inhibitor V
• Fórmula empírica (Notação de Hill): C₂₈H₂₆N₄O₄
• Número CAS: 112953-11-4
• Peso molecular: 482.53
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: tan; white to beige
• solubilidade: ethanol: 1 mg/mL; DMSO: 5 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C
• InChI: 1S/C28H26N4O4/c1-28-25(35-3)15(29-2)12-18(36-28)31-16-10-6-4-8-13(16)19-21-22(27(34)30-26(21)33)20-14-9-5-7-11-17(14)32(28)24(20)23(19)31/h4-11,15,18,25,27,29,34H,12H2,1-3H3,(H,30,33)/t15-,18-,25-,27-,28+/m1/s1
• chave InChI: PBCZSGKMGDDXIJ-HQCWYSJUSA-N

Descrição

Descrição geral

A cell-permeable Staurosporine (Cat. No. 569397) derived anticancer agent that reversibly and ATP-competitively inhibits several protein kinases (IC₅₀ = 29 nM, 34 nM, 30 nM, 590 nM and 530 nM for PKCα, PKCβ, PKCγ, PKCδ and PKCε; IC₅₀ = 7 nM, 27 nM, 50 nM, 50 nM, 150 nM and 1.04 M for Chk1, Cdc25C-associated protein kinase 1, Cdk1, PAK4, Cdk5/p25 and Chk2; IC₅₀ = 33 nM, 50 nM, 95 nM, 500 nM, 500 nM and 1.0 M for PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA, respectively). At higher concentrations (>15 M), affects the activities of Src, PIM-1, CKII, DNA-PK, ErK1, ILK-1 and MAPKK1). Reported to suppress thymidylate synthase expression, induce apoptosis with caspase activation, and sensitize tumor cells to a range of DNA-damaging agents.

Ações bioquímicas/fisiológicas

Cell permeable: yes

IC50 = 29 nM, 34 nM, 30 nM, 590 nM, 530 nM, 7 nM, 27 nM, 50 nM, 50 nM, 150 nM, 1.04 µM, 33 nM, 50 nM, 95 nM, 500 nM, 500 nM and 1.0 µM, respectively for primary targets in the order listed

Primary Target
PKCα, PKCβ, PKCγ, PKCδ PKCε, Chk1, Cdc25C-associated protein kinase 1, Cdk1, PAK4, Cdk5/p25 and Chk2, PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA

Product competes with ATP.

Reversible: yes

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

Reinhardt, H.C., et al. 2007. Cancer Cell11, 175.
Jiang, X., et al. 2004. Mol. Cancer Ther.3, 1221.
Sato, S., et al. 2002. Oncogene21, 1727.
Patel, V., et al. 2002. Clin. Cancer Res.8, 3549.
Leclerc, S., et al. 2001. J. Biol. Chem.276, 251.
Busby, E.C., et al. 2000. Cancer Res.60, 2108.
Hsueh, C.T., et al. 1998. Clin. Cancer Res.4, 2201.
Akiyama, T., et al. 1997. Cancer Res.57, 1495.
Seynaeve, C.M., et al. 1994. Mol. Pharmacol.45, 1207.
Takahashi, I., et al. 1987, J. Antibiot.40, 1782.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable