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关于此项目
经验公式(希尔记法):
C23H26IN7O2S
化学文摘社编号:
分子量:
591.47
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
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.
SMILES string
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
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
pale yellow
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
相关类别
Disclaimer
毒性:标准处理(A)
General description
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。
Other Notes
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.
Packaging
用惰性气体包装
Preparation Note
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。
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Sarah A Scuderi et al.
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)
Lianxin Hu et al.
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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