PROTAC-O4I2 是一种靶向剪接因子 3B1 (SF3B1) 的 PROTAC。PROTAC-O4I2 在 K562 细胞中诱导 FLAG-SF3B1 降解，IC50 值为 0.244 μM。PROTAC-O4I2 还诱导 K562 WT 细胞凋亡 (apoptosis)。
货号:ajcx36612
CAS:N/A
分子式:C29H29ClN6O5S
分子量：609.1
溶解度:DMSO : 250 mg/mL (410.44 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells[1].

PROTAC-O4I2 introduces Thalidomide to ubiquitin E3 ligase cereblon (CRBN), which selectively degrades SF3B1 and inhibits tumor growth in cells[1].PROTAC-O4I2 degrades and inhibits SF3B1 in K562 cells. PROTAC-O4I2 exhibits anti-proliferation effects on SF3B1 WT, SF3B1 OE, and SF3B1 K700E cells with IC50s of 228, 63, and 90 nM, respectively[1].PROTAC-O4I2 induces FLAG-SF3B1 degradation in a concentration-dependent manner with a half maximal inhibitory concentration (IC50) value of 0.244 μM in K562 cells[1].

PROTAC-O4I2 significantly increases survival by interference with the maintenance and proliferation of tumor in a Drosophila intestinal tumor model[1].

[1]. Rodrigo A Gama-Brambila, et al. A PROTAC targets splicing factor 3B1. Cell Chem Biol. 2021 Nov 18;28(11):1616-1627.e8.