Wortmannin是一种PI3K抑制剂，IC50为3 nM，抑制自噬体的形成，也有效抑制DNA-PK/ATM，IC50分别为16 nM和150 nM。 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。 Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM. A fungal metabolite which inhibits Pl3-kinase A cell-permeable fungal metabolite that acts as a potent, selective and irreversible inhibitor of phosphatidylinositol 3-kinase in purified preparations and cytosolic fractions (IC50=5 nM). Blocks the catalytic activity of PI 3-kinase without affecting upstream signaling events. Preincubation of fibroblasts with wortmannin abolishes PDGF-mediated Ins(3,4,5)P3 formation (IC50=5 nM). Blocks the metabolic effects of insulin in isolated rat adipocytes without affecting insulin receptor tyrosine kinase activity. Inhibits platelet-activating factor-induced MAP kinase activation in guinea pig neutrophils (200-300 nM). Also inhibits other kinases such as myosin light chain kinase (IC50=200 nM) and PI 4-kinase at concentrations higher than those required for inhibition of PI 3-kinase. Also blocks phospholipase D.
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Wortmannin
Dangerous GoodsCAS number：19545-26-7 molecular formula：C23H24O8
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | BRN 0067676 | SCHEMBL4531 | ST-415 | (1S,6bR,9aS,11R,11bR)-1-(methoxymethyl)-9a,11b-dimethyl-3,6,9-trioxo-3,6,6b,7,8,9,9a,10,11,11b-decahydro-1H-furo[4,3,2-de]indeno[4,5-h]isochromen-11-yl acetate. | BDBM15234 | Q27102129 | HMS1792N13 | HY-10197 | NCI60_0 | ||
| CAS number | 19545-26-7 | molecular formula | C23H24O8 |
| molecular weight | 428.43 g/mol | Exact mass | - |
| PSA | 109.000 Ų | logp | 1.200 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
pictogram：
GHS06
Signal word：
Danger
Hazard Statement：
H300: 吞咽致命 H310: 与皮肤接触致命 H330: 吸入致命
Statement of Preventive Measures：
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P284: 如果通风不良，请佩戴呼吸防护装置。 P271: 仅在室外或通风良好的地方使用。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P304+P340: 如误吸入：将人转移到空气新鲜处，保持
WGK Germany：
3
Personal protective equipment：
Eyeshields,Faceshields,full-face particle respirator type N100 (US),Gloves,respirator cartridge type N100 (US),type P1 (EN143) respirator filter,type P3 (EN 143) respirator cartridges
RTECS：
CB9641000
UN Number：
3462
Production methods and uses
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upstream information
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MSDS
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