MMV390048 是疟原虫 PI4K 抑制剂 (Kdapp=0.3 µM)。MMV390048 与疟原虫 PI4K 的 ATP 结合位点结合，除人 PIP4K2C 外不与其他恶性疟原虫和激酶结合，从而减轻潜在的激酶介导的安全性问题。MMV390048 是一种抗疟剂。
货号:ajcx33070
CAS:1314883-11-8
分子式:C18H14F3N3O2S
分子量：393.38
溶解度:DMSO : 100 mg/mL (254.21 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kdapp=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent[1].

MMV390048 against intraerythrocytic life cycle stages of P. falciparum (NF54 drug-sensitive strain) showed a steep inhibition curve with IC50 and IC90 values of 28 and 40 nM, respectively.

[1]. Paquet T, et al. Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase. Sci Transl Med. 2017 Apr 26;9(387). pii: eaad9735.