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质量水平
方案
≥98% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white to off-white
溶解性
DMSO: 25 mg/mL
warm ethanol: 25 mg/mL
运输
ambient
储存温度
−20°C
SMILES字符串
O1C=C(C=CC1=O)[C@@H]2[C@@]3([C@@](C4C([C@@]5([C@@H](C[C@H](CC5)O)CC4)C)CC3)(CC2)O)C
InChI
1S/C24H34O4/c1-22-10-7-17(25)13-16(22)4-5-20-19(22)8-11-23(2)18(9-12-24(20,23)27)15-3-6-21(26)28-14-15/h3,6,14,16-20,25,27H,4-5,7-13H2,1-2H3/t16-,17+,18-,19?,20?,22+,23-,24+/m1/s1
InChI key
QEEBRPGZBVVINN-ZXRSHIDQSA-N
一般描述
A cardiotonic steroid isolated from Bufo species toads that potently inhibits ouabain-sensitive Na+,K+-ATPase activity. Induces apoptosis in various human cell lines such as leukemia HL60 and U937 cells by altering the expression of apoptosis-related genes. Reported to stimulate the activities of p21 activated kinase (PAK) and c-Jun Kinase (JNK) in leukemic cell lines. Induces a transient increase in the expression of Tiam1 mRNA in U937 cell lines (~100 nM). Bufalin also down-regulates gene expression of the intracellular signaling protein 14-3-3 in rat lens, probably a consequence of Na+-K+-ATPase inhibitors. Reduces the level of topoisomerase II in human leukemia cells.
A cardiotonic steroid isolated from toads of Bufo species that potently inhibits ouabain-sensitive Na+,K+-ATPase activity (IC50 = 1.4 nM). Induces apoptosis in various human cell lines such as leukemia HL-60 and U937 cells by altering the expression of apoptosis-related genes. Reported to stimulate the activities of p21 activated kinase (PAK) and c-Jun Kinase (JNK) in leukemic cell lines. Induces a transient increase in the expression of Tiam1 mRNA in U937 cell lines (~100 nM). Bufalin also down-regulates gene expression of the intracellular signaling protein 14-3-3 in rat lens, probably a consequence of Na+,K+-ATPase inhibition. Reduces the level of topoisomerase II in human leukemia cells.
生化/生理作用
Cell permeable: no
Primary Target
Ouabain-sensitive Na+,K+-ATPase activity
Ouabain-sensitive Na+,K+-ATPase activity
Product does not compete with ATP.
Reversible: no
Target IC50: 1.4 nM against ouabain-sensitive Na+,K+-ATPase activity
包装
Packaged under inert gas
警告
Toxicity: Highly Toxic (H)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.
Kurosawa, M., et al. 2000. Am. J. Physiol.278, C500.
Kawazoe, N., et al. 1999. Oncogene 18, 2413.
McGowan, M.H., et al. 1999. J. Pharmacol. Exp. Ther. 289, 1559.
Watabe, M., et al. 1998. Oncogene 16, 779.
Hashimoto, S., et al. 1997. Leuk. Res. 21, 875.
Morris, J.F., et al. 1997. Comp. Biochem. Physiol. A Physiol. 118, 599.
Brownlee, A.A., et al. 1990. Clin. Sci.78, 169.
Kawazoe, N., et al. 1999. Oncogene 18, 2413.
McGowan, M.H., et al. 1999. J. Pharmacol. Exp. Ther. 289, 1559.
Watabe, M., et al. 1998. Oncogene 16, 779.
Hashimoto, S., et al. 1997. Leuk. Res. 21, 875.
Morris, J.F., et al. 1997. Comp. Biochem. Physiol. A Physiol. 118, 599.
Brownlee, A.A., et al. 1990. Clin. Sci.78, 169.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
警示用语：
Danger
危险声明
危险分类
Acute Tox. 2 Oral
储存分类代码
6.1A - Combustible acute toxic Cat. 1 and 2 / very toxic hazardous materials
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
高风险级别生物产品--毒素类产品
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