所有图片(1)
推荐产品
质量水平
检测方案
≥98% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
off-white
溶解性
DMSO: 20 mg/mL
ethanol: soluble
运输
ambient
储存温度
−20°C
InChI
1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2
InChI key
CZQHHVNHHHRRDU-UHFFFAOYSA-N
一般描述
一种可渗透细胞的，强效的，可逆的和特异性磷脂酰肌醇3-激酶（PI 3-激酶）抑制剂，可作用于酶的ATP结合位点（IC50 = 1.4 µ M）。还抑制460 kDa磷脂酰肌醇3样激酶DNA-PKcs中的非同源DNA末端连接（NHED），DNA-PKcs是DNA激活的蛋白激酶的催化亚基。在50 µM时不影响EGF受体激酶，MAP激酶，PKC，PI 4-激酶，S6激酶和c-src的活性。促进活性GSK-3b的核积累。据报告可抑制鼠胚胎干细胞的增殖。阻断培养的兔主动脉平滑肌细胞增殖，而不诱导凋亡。据报告可抑制RBL-2H3细胞中的组胺分泌（IC50 = 5 µM）。
一种细胞可渗透的、强效的、可逆的和特异性磷脂酰肌醇3-激酶抑制剂（IC50 = 1.4 µM），作用于酶的ATP结合位点。还抑制460 kDa磷脂酰肌醇3样激酶DNA-PKcs的非同源DNA末端连接（NHEJ）活性，DNA-PKcs是DNA激活的蛋白激酶的催化亚基。即使在50 µM时也不影响EGF受体激酶，MAP激酶，PKC，PI 4-激酶，S6激酶和c-Src的活性。促进活性GSK-3b的核积累。据报告可抑制鼠胚胎干细胞的增殖。阻断培养的兔主动脉平滑肌细胞增殖，而不诱导凋亡。显示与I-BET（目录号40101050 ~ 10 µM）结合在同一位点。也可购买10 mM（1 mg/325 µl）LY 294002（目录号440204） 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
产物与ATP竞争。
可逆性：是
细胞可渗透性：具有
靶标IC50：磷脂酰肌醇3-激酶为1.4 µM
警告
毒性：标准处理（A）
制备说明
实现完全溶解可能需要轻微加热。
重悬
复溶后，等分并冷冻保存（-20°C）。贮备液在-20°C下可稳定保存至多6个月。
其他说明
Dittman, A., et al. 2013. ACS Chem. Biol.9, 495.
Bechard, M., and Dalton.S. 2009.Mol.Cell.Biol.29, 2092.
Lianguzova, M.S. et al. 2007.Cell Biol. Int.31, 330.
Baumann, P., and West, S.C.1998.Proc.Natl.Acad.Sci. USA 95, 14066.
Cardone, M.H., et al. 1998.Science282, 1318.
Vlahos, C.J., et al. 1995.J. Immunol.154, 2413.
Yano, H., et al. 1995.Biochem.J.312, 145.
Vlahos, C.J., et al. 1994.J. Biol. Chem.269, 5241.
Selected Citations
Lee, J., et al. 2009.Cell Stem Cell5, 76.
Bechard, M., and Dalton.S. 2009.Mol.Cell.Biol.29, 2092.
Lianguzova, M.S. et al. 2007.Cell Biol. Int.31, 330.
Baumann, P., and West, S.C.1998.Proc.Natl.Acad.Sci. USA 95, 14066.
Cardone, M.H., et al. 1998.Science282, 1318.
Vlahos, C.J., et al. 1995.J. Immunol.154, 2413.
Yano, H., et al. 1995.Biochem.J.312, 145.
Vlahos, C.J., et al. 1994.J. Biol. Chem.269, 5241.
Selected Citations
Lee, J., et al. 2009.Cell Stem Cell5, 76.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
闪点(°F)
487.4 °F
闪点(°C)
253.0 °C
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