FB23 Chemical Structure
CAS No. : 2243736-35-6
FB23 是一(yī)種有(yǒu)效的(de),選擇性的(de) FTO 去(qù)甲基化酶抑制劑,IC50 為(wèi) 60 nM。FB23 直接與 FTO 結合并選擇性抑制 FTO 的(de) mRNA N6-甲基腺嘌呤脫甲基酶活性。
規格 | 10 mg/支 |
貨号 | GM-2022132 |
生物活性 | FB23 is a potent and selective FTO demethylase inhibitor with an IC50 of 60 nM. FB23 directly binds to FTO and selectively inhibits FTO's mRNA N6-methyladenosine (m6A) demethylase activity[1]. |
IC50 & Target | IC50: 60 nM (FTO)[1] |
體外研究 (In Vitro) | 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]. | |
We has not independently confirmed the accuracy of these methods. They are for reference only. | |
體內(nèi)研究 (In Vitro) | 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]. |
We has not independently confirmed the accuracy of these methods. They are for reference only. | |
分子(zǐ)量 | 377.22 |
Formula | C₁₈H₁₄Cl₂N₂O₃ |
CAS 号 | 2243736-35-6 |
運輸條件 | Room temperature in continental US; may vary elsewhere. |
儲存方式 | Powder -20°C 3 years |
4°C 2 years | |
In solvent -80°C 6 months | |
-20°C 1 month |
參考文獻
[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. |
說明書下載:FB23.pdf