推荐产品
product name
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.
品質等級
化驗
≥98% (HPLC)
形狀
solid
製造商/商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
white to off-white
溶解度
DMSO: 25 mg/mL
運輸包裝
ambient
儲存溫度
−20°C
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 密鑰
QDLHCMPXEPAAMD-QAIWCSMKSA-N
一般說明
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
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
包裝
用惰性气体包装
警告
毒性:高毒性(H)
重構
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。
其他說明
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.
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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法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
訊號詞
Danger
危險分類
Acute Tox. 1 Inhalation - Acute Tox. 1 Oral - Acute Tox. 2 Dermal
儲存類別代碼
6.1A - Combustible acute toxic Cat. 1 and 2 / very toxic hazardous materials
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
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