PROTAC-O4I2 |
| رقم الكتالوجGC63916 |
PROTAC-O4I2 هو عامل ربط أهداف PROTAC 3B1 (SF3B1)يؤدي PROTAC-O4I2 إلى تدهور FLAG-SF3B1 بقيمة IC50 تبلغ 0.244 ميكرومتر في خلايا K562يحفز PROTAC-O4I2 أيضًا موت الخلايا المبرمج الخلوي في خلايا K562 WT
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Sample solution is provided at 25 µL, 10mM.
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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.
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