2040291-27-6

2040291-27-6 structure

Name: LLY-283
Chemical Name: LLY-283
CAS Number: 2040291-27-6
Molecular Formula: C₁₇H₁₈N₄O₄
Molecular Weight: 342.35
Catalog: Research Areas Cancer
Create Date: 2018-08-13 00:05:05
Modify Date: 2024-01-12 17:01:37
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.

Name	LLY-283

Description	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.
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Cancer
Target	IC50: 22 nM (PRMT5:MEP50)[1] Ki: 6 nM (PRMT5:MEP50)[1]
In Vitro	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].
In Vivo	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].
References	[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.