2018300-62-2
中文名稱
2018300-62-2
英文名稱
TPOP146
CAS
2018300-62-2
分子式
C27H35N3O5
分子量
481.58
MOL 文件
2018300-62-2.mol
更新日期
2024/12/03 15:40:34
2018300-62-2 結(jié)構(gòu)式
基本信息
中文別名
CBP/P300苯并西泮溴結(jié)構(gòu)域抑制劑(TPOP146) 英文別名
TPOP146TPOP-146
TPOP 146
7-(3,5-dimethoxyphenyl)-N-[(3S)-1-methylpiperidin-3-yl]-4-propanoyl-3,5-dihydro-2H-1,4-benzoxazepine-9-carboxamide
1,4-Benzoxazepine-9-carboxamide, 7-(3,5-dimethoxyphenyl)-2,3,4,5-tetrahydro-N-[(3S)-1-methyl-3-piperidinyl]-4-(1-oxopropyl)-
物理化學(xué)性質(zhì)
沸點(diǎn)641.8±55.0 °C(Predicted)
密度1.24±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : ≥ 100 mg/mL (207.65 mM)
酸度系數(shù)(pKa)10.68±0.20(Predicted)
形態(tài)Solid
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
TPOP146是選擇性的CBP/P300苯并西泮溴結(jié)構(gòu)域抑制劑；對(duì)CBP和BRD4的Kd值分別為134 nM和5.02 μM。靶點(diǎn)
IC50: 134 nM (CBP); 5.02 μM (BRD4)
體外研究
Exposure to 1 μM TPOP146 results in a significant decrease of recovery half-life that is comparable to the construct that contained the bromodomain inactivating mutation N1168F, demonstrating that TPOP146 targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediated interactions of the CBP bromodomain in cellular environments.