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化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
white to light brown
溶解度
DMSO: 15 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
Cl.Ic1cnc(Nc2cccc(NC(=O)N3CCCC3)c2)nc1NCCCNC(=O)c4cccs4
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 密鑰
VAVXGGRQQJZYBL-UHFFFAOYSA-N
應用
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。
生化／生理作用
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。
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
其他客户在看
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)
Discovery and structure of a new inhibitor scaffold of the autophagy initiating kinase ULK1.
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