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.
别名:
Calphostin C, Cladosporium cladosporioides, UCN-1028c
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About This Item
推荐产品
品質等級
化驗
≥95% (HPLC)
形狀
lyophilized solid
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
light brown
溶解度
DMSO: 1 mg/mL
ethanol: soluble
運輸包裝
ambient
儲存溫度
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
InChI 密鑰
LSUTUUOITDQYNO-UHFFFAOYSA-N
一般說明
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.
生化／生理作用
Cell permeable: yes
Primary Target
PKC
PKC
Product does not compete with ATP.
Reversible: no
Target IC50: 50 nM against protein kinase C
警告
Toxicity: Standard Handling (A)
重構
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他說明
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.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
J C Norman et al.
FEBS letters, 484(3), 179-183 (2000-11-18)
Aggregation by immune complexes of receptors specific for the Fc region of IgG results in their internalisation and disposal by trafficking to lysosomes. We show here that internalisation of FcgammaRI by IFN-gamma treated U937 cells following receptor aggregation by cross-linking
Tomoya Sasahara et al.
iScience, 24(9), 102936-102936 (2021-08-31)
Amyloid β-protein (Aβ) may contribute to worsening of Alzheimer's disease (AD) through vascular dysfunction, but the molecular mechanism involved is unknown. Using ex vivo blood vessels and primary endothelial cells from human brain microvessels, we show that patient-derived Aβ assemblies, termed
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