LLY-283

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

LLY-283 (LLY283) 是一种有效的、选择性的精氨酸甲基转移酶 5 (PRMT5) 抑制剂，IC50 为 22 nM。

LLY-283 (LLY283) is a potent, selective inhibitor of arginine methyltransferase 5 (PRMT5) with IC50 of 22 nM; displays excellent against other arginine methyltransferases including the closely related PRMT7 and the type II PRMTs such as PRMT4 and 6; decreases SmBB’-Rme2s levels in MCF7 cells with IC50 of 25 nM, also inhibits the PRMT5 mediated regulation of the splicing of MDM4; inhibits proliferation of A375 cells with IC50 of 45.6 nM; inhibits Tumor growth in mouse xenograft (A375, 20 mg/kg; QD).

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.

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.

LLY283

Chromatin/Epigenetic

HMTase

HMTase

Cancer

——

2040291-27-6

342.36

C17H18N4O4

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (365.12 mM)

O[C@H]1[C@H](N2C=CC3=C(N)N=CN=C32)O[C@H]([C@H](O)C4=CC=CC=C4)[C@H]1O

(2R,3R,4S,5R)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(R)-hydroxy(phenyl)methyl]oxolane-3,4-diol

(-20℃)

With Ice Pack

≥ 2 years