质量水平
检测方案
≥97% (HPLC)
形式
solid
效能
660 nM IC50
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
颜色
light yellow to yellow
溶解性
water: 1 mg/mL
DMSO: 10 mg/mL
运输
ambient
储存温度
−20°C
InChI
1S/C21H18NO4.ClH/c1-22-10-16-13(6-7-17(23-2)21(16)24-3)14-5-4-12-8-18-19(26-11-25-18)9-15(12)20(14)22;/h4-10H,11H2,1-3H3;1H/q+1;/p-1
InChI key
WEEFNMFMNMASJY-UHFFFAOYSA-M
一般描述
Naturally occurring alkaloid. Cell-permeable, selective inhibitor of protein kinase C (IC50 = 660 nM). Acts on the catalytic domain irrespective of the attachment of the regulatory domain. Material is a competitive inhibitor with respect to the phosphate acceptor and a non-competitive inhibitor with respect to ATP. Over ten-fold more potent than H-7, HCl (Cat. No. 371955). Inhibits thromboxane formation and phosphoinositide metabolism in platelets. Also induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells.
Naturally-occurring alkaloid. Potent, selective, and cell-permeable inhibitor of protein kinase C (IC50 = 660 nM). Acts on the catalytic domain of PKC. A competitive inhibitor with respect to the phosphate acceptor and a non-competitive inhibitor with respect to ATP. Over ten-fold more potent than H-7, HCl (Cat. No. 371955). Inhibits thromboxane formation and phosphoinositide metabolism in platelets. Also induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells.
生化/生理作用
Cell permeable: yes
Primary Target
PKC
PKC
Product does not compete with ATP.
Reversible: no
警告
Toxicity: Harmful (C)
制备说明
Heating to 40-50°C with gentle agitation may be necessary to achieve complete solubilization. Further dilute with buffer just prior to use.
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
其他说明
Kandasamy, R.A., et al. 1995. J. Biol. Chem.270 29209.
Jarvis, W.D., et al. 1994. Cancer Res.54, 1707.
Barg, J., et al. 1992. J. Neurochem.59, 1145.
Herbert, J.M., et al. 1990. Biochem. Biophys. Res. Commun.172, 993.
Ko, F., et al. 1990. Biochim. Biophys. Acta1052, 360.
Walterova, D., et al. J. Med. Chem.24, 1100.
Jarvis, W.D., et al. 1994. Cancer Res.54, 1707.
Barg, J., et al. 1992. J. Neurochem.59, 1145.
Herbert, J.M., et al. 1990. Biochem. Biophys. Res. Commun.172, 993.
Ko, F., et al. 1990. Biochim. Biophys. Acta1052, 360.
Walterova, D., et al. J. Med. Chem.24, 1100.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
警示用语:
Warning
危险分类
Acute Tox. 4 Dermal - Acute Tox. 4 Inhalation - Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官
Respiratory system
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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