FB23是一种有效的，选择性的脂肪与肥胖相关蛋白(FTO)抑制剂，IC50为60nM。FB23直接与FTO结合并选择性抑制FTO的mRNAN6-甲基腺嘌呤脱甲基酶活性。
货号:ajcx30636
CAS:2243736-35-6
分子式:C18H14Cl2N2O3
分子量：377.22
溶解度:DMSO: 125 mg/mL (331.37 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

FB23 is a potent and selective fat-mass and obesity-associated protein (FTO) inhibitor with an IC50 of 60 nM. FB23directly binds to FTO and selectively inhibits FTO’s mRNA N6-methyladenosine (m6A) demethylase activity[1].

FB23 (72 hours) treatment inhibits acute myeloid leukemia (AML) cells proliferation with IC50 values of 44.8 μM, 23.6 μM for NB4 and MONOMAC6 AML cells[1].FB23 treatment causes the significant suppression of MYC targets, E2F targets, and G2M checkpoint signal cascades, which may contribute to the inhibitory effects of FTO inhibitors and FTO KD on cell cycle and proliferation. FB23 treatments activates apoptosis and p53 pathways[1].

A single dose of 3 mg/kg FB23 is i.p. administrated to Sprague Dawley (SD) rats for the pharmacokinetic profile. The Cmax and Tmax value of FB23 are 142.5 ng/mL and 0.4 hr, respectively[1].

[1]. Yue Huang, et al. Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia. Cancer Cell. 2019 Apr 15;35(4):677-691.e10.