PROTAC-O4I2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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)。

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.

Cell Proliferation Assay Cell Line:K562 control cells (WT), cells overexpressing SF3B1 (OE), and cells expressing SF3B1K700E (K700E) Concentration:1 pM, 0.1 nM, 10 nM, 1 μM, 100 μMIncubation Time:72 hours Result:In K562 WT cells, the parental compound O4I2 exhibited a marginal anti-proliferation effect (IC50 >10 μM). In contrast, PROTAC-O4I2 showed significantly higher toxicity with an IC50 of 228 nM, nearly 3-fold less potent than pladienolide B (IC50, 76 nM). Cells overexpressing SF3B1 WT was slightly resistant to pladienolide B (IC50, 134 nM), but more sensitive to PROTAC-O4I2 (an IC50 value of 63 nM).Apoptosis Analysis Cell Line:K562 cell Concentration:1 μM Incubation Time:48 h Result:Induced cellular apoptosis s in cells expressing SF3B1WT or SF3B1K700E.

Animal Model:Drosophila melanogasterDosage:10 μM Administration:Flies were fed on a round filter paper loaded with PROTAC-O4I2 in a 5% sucrose solution, maintained at 18℃ and flipped into a freshly prepared vial every 2 days Result:Decreased stem cell activity, blocked the initiation and growth of tumor, and improved the survival of the Drosophila ISC tumor model.

——

Others

Other Targets

PROTACs | Apoptosis

——

——

2785323-62-6

609.1

C29H29ClN6O5S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (410.44 mM; 超声助溶 )

O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2NCCCCCCNC(=O)C=4N=C(NC5=CC=C(Cl)C=C5)SC4

——

(-20℃)

With Ice Pack

≥ 2 years