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.

• Synonim(y): Calphostin C, Cladosporium cladosporioides, UCN-1028c
• Wzór empiryczny (zapis Hilla): C₄₄H₃₈O₁₄
• Numer CAS: 121263-19-2
• Masa cząsteczkowa: 790.76
• Numer MDL: MFCD00133155
• Kod UNSPSC: 12352200

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Postać: lyophilized solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: light brown
• rozpuszczalność: DMSO: 1 mg/mL; ethanol: soluble
• Warunki transportu: ambient
• temp. przechowywania: 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
• Klucz InChI: LSUTUUOITDQYNO-UHFFFAOYSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
PKC

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 50 nM against protein kinase C

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable