208725

Calphostin C, Cladosporium cladosporioides

A cell permeable, highly specific inhibitor of protein kinase C (IC₅₀ = 50 nM) that interacts with the protein′s regulatory domain by competing at the binding site of diacylglycerol and phorbol esters.

• Sinônimo(s): Calphostin C, Cladosporium cladosporioides, UCN-1028c
• Fórmula empírica (Notação de Hill): C₄₄H₃₈O₁₄
• Número CAS: 121263-19-2
• Peso molecular: 790.76
• Número MDL: MFCD00133155
• Código UNSPSC: 12352200

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• Formulário: lyophilized solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: light brown
• solubilidade: DMSO: 1 mg/mL; ethanol: soluble
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C
• InChI: 1S/C44H38O14/c1-20(56-43(50)22-10-8-7-9-11-22)16-25-31-32-26(17-21(2)57-44(51)58-24-14-12-23(45)13-15-24)42(55-6)40(49)34-28(47)19-30(53-4)36(38(32)34)35-29(52-3)18-27(46)33(37(31)35)39(48)41(25)54-5/h7-15,18-21,45,48-49H,16-17H2,1-6H3
• chave InChI: LSUTUUOITDQYNO-UHFFFAOYSA-N

Descrição

Descrição geral

A cell permeable, highly specific inhibitor of protein kinase C (IC₅₀ = 50 nM) that interacts with the protein’s regulatory domain by competing at the binding site of diacylglycerol and phorbol esters. Does not compete with Ca²⁺ or phospholipids. At higher concentrations inhibits myosin light chain kinase (IC₅₀ >5 µM), protein kinase A (IC₅₀ >50 µM), protein kinase G (IC₅₀ >25 µM), and p60^v-src (IC₅₀ >50 µM). Induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells. Requires brief exposure to light for activation.

Cell-permeable, highly specific inhibitor of protein kinase C (IC₅₀ = 50 nM) that interacts with the protein′s regulatory domain by competing at the binding site of diacylglycerol and phorbol esters. At higher concentrations inhibits myosin light chain kinase (IC₅₀ >5 µM), protein kinase A (IC₅₀ >50 µM), protein kinase G (IC₅₀ >25 µM), and p60^v-src protein tyrosine kinase (IC₅₀ >50 µM). Does not compete with Ca²⁺ or phospholipids. Also induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells. Inhibition of PKC is dependent on exposure to light in cell-free systems. Ordinary fluorescent light is sufficient for full activation.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
PKC

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 50 nM against protein kinase C

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

Jarvis, W.D., et al. 1994. Cancer Res.54, 1707.
Svetlov, S., and Nigami, S. 1993. Biochim. Biophys. Acta 1177, 75.
Gopalakrishna, R., et al. 1992. FEBS Lett. 314, 149.
Shimamato, H., et al. 1992. Br. J. Pharmacol.107, 282.
Bruns, R.F., et al. 1991. Biochem. Biophys. Res. Commun.176, 288.
Tamaoki, T., et al. 1990. Biotechnology8, 732.
Kobayashi, E., et al. 1989. Biochem. Biophys. Res. Commun.159, 548.

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