63388-44-3
中文名稱
SJB2-043
英文名稱
SJB2-043
CAS
63388-44-3
分子式
C17H9NO3
分子量
275.26
MOL 文件
63388-44-3.mol
更新日期
2025/01/14 17:14:45
63388-44-3 結(jié)構(gòu)式
基本信息
中文別名
2-苯基萘并[2,3-D]惡唑-4,9-二酮USP1/UAF1復(fù)合體抑制劑(SJB2-043)
英文別名
SJB2-0432-Phenylnaphth[2,3-d]oxazole-4,9-dione
Naphth[2,3-d]oxazole-4,9-dione, 2-phenyl-
2-phenylbenzo[f][1,3]benzoxazole-4,9-dione
所屬類別
生物化工：蛋白酶抑制劑物理化學(xué)性質(zhì)
熔點(diǎn)>290℃
沸點(diǎn)495.0±48.0 °C(Predicted)
密度1.373±0.06 g/cm3(Predicted)
儲(chǔ)存條件Sealed in dry,Room Temperature
溶解度insoluble in H2O; insoluble in EtOH; ≥4.62 mg/mL in DMSO
酸度系數(shù)(pKa)-3.87±0.20(Predicted)
形態(tài)固體
顏色Green to dark green
常見(jiàn)問(wèn)題列表
用途
SJB2-043是有效的USP1抑制劑，可抑制天然USP1/UAF1的活性，IC50為544 nM。生物活性
SJB2-043 是一種有效的 USP1 的抑制劑，可抑制天然 USP1/UAF1 的活性，對(duì)應(yīng)的IC50值為544 nM。靶點(diǎn)
| Target | Value |
|
USP1-UAF1
(Cell-free assay) | 544 nM |
體外研究
SJB2-043 causes a dose-dependent decrease in ubiquitin-specific protease 1 (USP1) levels and a concomitant degradation of inhibitor of DNA-binding-1 (ID1) protein in the K562 cells at a micromolar drug concentration. SJB2-043 also causes a decrease in the levels of other ID proteins, namely ID2 and ID3 in K562 cells. SJB2-043 causes a dose-dependent decrease in the number of viable K562 cells, with an EC 50 of approximately 1.07 μM. Moreover, SJB2-043 induces apoptosis of K562 cells in a dose-dependent manner.