SML0694
BX-795 盐酸盐
≥98% (HPLC)
别名:
N-[3-[[5-碘-4-[[3-[(2-噻吩羰基)氨基]丙基]氨基]-2-嘧啶基]氨基]苯基]-1-吡咯烷甲酰胺 盐酸盐
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关于此项目
经验公式（希尔记法）:
C23H26IN7O2S · xHCl
化学文摘社编号:
分子量:
591.47 (free base basis)
NACRES:
NA.77
UNSPSC Code:
12352200
产品名称
BX-795 盐酸盐, ≥98% (HPLC)
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
SMILES string
Cl.Ic1cnc(Nc2cccc(NC(=O)N3CCCC3)c2)nc1NCCCNC(=O)c4cccs4
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to light brown
solubility
DMSO: 15 mg/mL, clear
storage temp.
2-8°C
Quality Level
相关类别
Application
BX-795盐酸盐已被用于研究激酶抑制对人内源性逆转录病毒（HERV）转录激活的影响。
Biochem/physiol Actions
BX-795会与3-磷酸肌醇依赖性激酶-1（PDK1）的底物ATP竞争它的ATP（三磷酸腺苷）结合口袋。体外检测表明BX-795可能会抑制Unc-51（丝氨酸/苏氨酸蛋白激酶）样自噬激活激酶（ULK1）。
BX-795是TANK结合激酶（TBK1）和IKB激酶ε（IKKε）′的一种抑制剂。
BX-795最初被定性为3-磷酸肌醇依赖性激酶-1的一种有效抑制剂。利用BX-795进行的更多研究表明该分子也是IKKe和TBK1一种有效双重抑制剂，并已知其可通过干扰素调节因子3（IRF3）的磷酸化来调节干扰素的表达。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Discovery and structure of a new inhibitor scaffold of the autophagy initiating kinase ULK1.
Lazarus M B and Kevan M S
Bioorganic & Medicinal Chemistry, 23(17), 5483-5488 (2015)
Richard I Feldman et al.
The Journal of biological chemistry, 280(20), 19867-19874 (2005-03-18)
The phosphoinositide 3-kinase/3-phosphoinositide-dependent kinase 1 (PDK1)/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumor angiogenesis and represents a promising target for anticancer drugs. Here, we describe three potent PDK1 inhibitors, BX-795, BX-912, and BX-320 (IC(50)
Nagarjuna R Cheemarla et al.
medRxiv : the preprint server for health sciences (2021-02-04)
The interferon response is a potent antiviral defense mechanism, but its effectiveness depends on its timing relative to viral replication. Here, we report viral replication and host response kinetics in patients at the start of SARS-CoV-2 infection and explore the
Qingyuan Zhu et al.
Antiviral research, 183, 104933-104933 (2020-09-20)
Stimulator of interferon genes (STING), as a signaling hub in innate immunity, plays a central role for the effective initiation of host defense mechanisms against microbial infections. Upon binding of its ligand cyclic dinucleotides (CDNs) produced by the cyclic GMP-AMP
Compound signaling activates endogenous retroviruses by inducing enhancer and gene-neighborhood transcription.
Azebi S, et al.
bioRxiv, 284695-284695 (2018)
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