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.
Sinónimos:
Calphostin C, Cladosporium cladosporioides, UCN-1028c
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About This Item
Fórmula empírica (notación de Hill):
C44H38O14
Número de CAS:
Peso molecular:
790.76
Número MDL:
Código UNSPSC:
12352200
Productos recomendados
Nivel de calidad
Análisis
≥95% (HPLC)
formulario
lyophilized solid
fabricante / nombre comercial
Calbiochem®
condiciones de almacenamiento
OK to freeze
protect from light
color
light brown
solubilidad
DMSO: 1 mg/mL
ethanol: soluble
Condiciones de envío
ambient
temp. de almacenamiento
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
Clave InChI
LSUTUUOITDQYNO-UHFFFAOYSA-N
Descripción general
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 p60v-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 p60v-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.
Acciones bioquímicas o fisiológicas
Cell permeable: yes
Primary Target
PKC
PKC
Product does not compete with ATP.
Reversible: no
Target IC50: 50 nM against protein kinase C
Advertencia
Toxicity: Standard Handling (A)
Reconstitución
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Otras 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.
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.
Información legal
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Código de clase de almacenamiento
11 - Combustible Solids
Clase de riesgo para el agua (WGK)
WGK 3
Punto de inflamabilidad (°F)
Not applicable
Punto de inflamabilidad (°C)
Not applicable
Certificados de análisis (COA)
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