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Merck
CN

681675

渥曼青霉素

≥98% (HPLC), solid, PI3-kinase inhibitor, Calbiochem

别名:

渥曼青霉素

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关于此项目

经验公式（希尔记法）:
C23H24O8
化学文摘社编号:
19545-26-7
分子量:
428.43
MDL编号:
MFCD00133927
UNSPSC代码:
12352200
NACRES:
NA.77

主要文件

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产品名称

渥曼青霉素, Wortmannin, CAS 19545-26-7, is a cell-permeable, potent, selective, and irreversible inhibitor of PI3-Kinase (IC50 = 5 nM). Does not affect any upstream signaling events.

描述

Merck USA index - 14, 10053

质量水平

100

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

运输

ambient

储存温度

−20°C

SMILES字符串

[o]1c2c3c(c1)C(=O)O[C@@H]([C@@]3(C4=C([C@H]5[C@](C[C@H]4OC(=O)C)(C(=O)CC5)C)C2=O)C)COC

InChI

1S/C23H24O8/c1-10(24)30-13-7-22(2)12(5-6-14(22)25)16-18(13)23(3)15(9-28-4)31-21(27)11-8-29-20(17(11)23)19(16)26/h8,12-13,15H,5-7,9H2,1-4H3/t12-,13+,15+,22-,23-/m0/s1

InChI key

QDLHCMPXEPAAMD-QAIWCSMKSA-N

相关类别

一般描述

一种真菌代谢物，在纯化制剂和细胞溶质部分（IC50=5 nM）中，作为磷脂酰肌醇3-激酶（PI 3-激酶）的有效、选择性、细胞渗透性和不可逆抑制剂。成纤维细胞与渥曼青霉素预孵育可消除PDGF介导的Ins（3,4,5）P3形成（IC50=5 nM）。阻断PI 3激酶的催化活性，而不影响上游信号事件。在不影响胰岛素受体酪氨酸激酶活性的情况下，也可阻断胰岛素在离体大鼠脂肪细胞中的代谢作用。抑制血小板活化因子在豚鼠中性粒细胞（0.2-0.3 µM）中诱导的MAP激酶激活。抑制破骨细胞的骨吸收。抑制其他激酶，如肌球蛋白轻链激酶（IC50 = 200 nM）和PI 4激酶，其浓度比抑制PI 3激酶所需浓度高100倍。还阻断磷脂酶D。
一种细胞渗透性真菌代谢物，在纯化制剂和细胞溶质部分（IC50=5 nM）中，作为磷脂酰肌醇3-激酶的有效、选择性和不可逆抑制剂。阻断PI 3激酶的催化活性，而不影响上游信号事件。成纤维细胞与渥曼青霉素预孵育可消除PDGF介导的Ins（3,4,5）P3形成（IC50=5 nM）。在不影响胰岛素受体酪氨酸激酶活性的情况下，也可阻断胰岛素在离体大鼠脂肪细胞中的代谢作用。抑制血小板激活因子诱导的豚鼠中性粒细胞MAP激酶活化活（200-300nm）。也抑制其他激酶，如肌球蛋白轻链激酶（IC50=200 nM）和PI 4激酶，其浓度高于抑制PI 3激酶所需的浓度。还可阻断磷脂酶D。也可提供10 mM（1 mg/233 µl）渥曼青霉素（目录号681676）的DMSO溶液。

生化/生理作用

主要靶标
磷脂酰肌醇-3-激酶
产物不与ATP竞争。
可逆：否
细胞可渗透性：是
靶标IC50：针对磷脂酰肌醇3-激酶，为5 nM；针对PDGF介导的Ins(3,4,5)P3形成，为5 nM；针对肌球蛋白轻链激酶，为200 nM

包装

用惰性气体包装

制备说明

复溶后，等分并冷冻保存（-20°C）。贮备溶液在-20°C下可稳定保存至多2个月。

其他说明

Cross, M.J., et al. 1995.J. Biol. Chem. 270, 25352.
Nakamura, I., et al. 1995.FEBS Lett.361, 79.
Ferby, I.M., et al. 1994.J. Biol. Chem. 269, 30485.
Okada, T., et al. 1994.J. Biol. Chem. 269, 3568.
Wymann, M.P. and Arcaro, A. 1994.Biochem.J.298, 517.
Arcaro, A. and Wymann, M.P. 1993.Biochem.J.296, 297.
Nakanishi, S., et al. 1992.J. Biol. Chem. 267, 2157.
Bonser, R.W., et al. 1991.Br. J. Pharmacol.103, 1237.
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法律信息

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

免责声明

毒性：高毒性（H）

象形图

Skull and crossbones
GHS06

警示用语：

Danger

危险声明

H300 + H310 + H330

危险分类

Acute Tox. 1 Inhalation - Acute Tox. 1 Oral - Acute Tox. 2 Dermal

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

分析证书(COA)

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相关内容

Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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