LLY-283是一种有效的，选择性的，可口服的蛋白精氨酸甲基转移酶5(PRMT5)抑制剂，对PRMT5:MEP50复合物的作用很强，IC50和Kd值分别为22nM和6nM，具有抗肿瘤活性。
货号:ajcx12890
CAS:2040291-27-6
分子式:C17H18N4O4
分子量：342.35
溶解度:DMSO: 250 mg/mL (730.25 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.

LLY-283 is a potent, oral and selective arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM in vitro and 25 nM in cells, as well as a Kd of 6 nM for PRMT5:MEP50 complex in vitro; LLY-283 inhibits the proliferation of A375 cell with an IC50 of 46 nM[1].

LLY-283 (20 mg/kg; p.o., QD (once a day)) causes a significant inhibition on tumor growth in mice bearing A375 cells after treatment for 28 days[1].

[1]. Zahid Q. Bonday, et al. LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity. ACS Med. Chem. Lett., 2018, 9 (7), pp 612-617.