204001
BX-795
BX-795, also referenced under CAS 702675-74-9, modulates the biological activity of multiple kinases. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
BX-795, AMPK相关激酶5抑制剂I,ARK5抑制剂I,NUAK激酶抑制剂I,NUAK1抑制剂I,SnF1类激酶-1抑制剂I,N-(3-((5-碘-4-((3-(2-噻吩基羰基)氨基)丙基)氨基)-2-嘧啶基)氨基)苯基)-1-吡咯烷甲酰胺,极光激酶
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About This Item
推荐产品
质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
pale yellow
溶解性
DMSO: 50 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
Ic1c(nc(nc1)Nc3cc(ccc3)NC(=O)N4CCCC4)NCCCNC(=O)c2[s]ccc2
InChI
1S/C23H26IN7O2S/c24-18-15-27-22(30-20(18)25-9-5-10-26-21(32)19-8-4-13-34-19)28-16-6-3-7-17(14-16)29-23(33)31-11-1-2-12-31/h3-4,6-8,13-15H,1-2,5,9-12H2,(H,26,32)(H,29,33)(H2,25,27,28,30)
InChI key
VAVXGGRQQJZYBL-UHFFFAOYSA-N
一般描述
一种可渗透细胞的氨基嘧啶化合物,可作为有效的,ATP竞争性和可逆的多激酶抑制剂(在≤ 10 µM ATP下,PDK1的IC50=11 nM;对于NUAK1,TBK1,MARK4,Aurora B,IKKε和PDK1,在100 µM ATP下,IC50=5、6、19、31、41和111 nM),并且显示出比Cdk2/E、EGFR、GSK-3β、IR、c-Kit、PKA、PKC、TAK1和VEGFR高50倍的选择性。显示可阻断PDK1/Akt信号传导,诱导PC-3和MDA-468细胞的生长停滞和凋亡(IC50分别为0.25和0.75 µM);此外,抑制IRF3的磷酸化(pSer396),核转位和转录活性,并减少刺激的巨噬细胞中IFN-β的产生。
包装
用惰性气体包装
警告
毒性:标准处理(A)
重悬
复溶后,等分并冷冻保存(-20°C)。储备液在-20°C条件下可稳定保存3个月。
其他说明
Clark, K., et al. 2009.J. Biol. Chem.284, 14136.
Tamgumcy, T., et al. 2008.Exp.Cell Res.314, 2299.
Feldman, R.I., et al. 2005.J. Biol. Chem.280, 19867.
Tamgumcy, T., et al. 2008.Exp.Cell Res.314, 2299.
Feldman, R.I., et al. 2005.J. Biol. Chem.280, 19867.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Oncology research, 28(7), 779-790 (2021-03-21)
Glioma are common malignant brain tumors, among which glioblastoma multiforme (GBM) has the worst prognosis. Different studies of GBM revealed that targeting nuclear factor B (NF-B) induced an attenuation tumor proliferation and prolonged cell survival. TBK1 {TANK [TRAF (TNF (tumor-necrosis-factor)
Cancer discovery, 10(3), 460-475 (2019-12-08)
TANK binding kinase 1 (TBK1) is an important kinase involved in the innate immune response. Here we discover that TBK1 is hyperactivated by von Hippel-Lindau (VHL) loss or hypoxia in cancer cells. Tumors from patients with kidney cancer with VHL
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