LLY-283 - 98%, high purity , CAS No.2040291-27-6, Inhibitor of protein arginine methyltransferase 5

Item Number

L414243

• Synonyms: (2R,3R,4S,5R)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(R)-hydroxy(phenyl)methyl]oxolane-3,4-diol
• Specifications & Purity: Moligand™, ≥98%
• Biochemical and Physiological Mechanisms: LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of protein arginine methyltransferase 5

Product Description

Information

LLY-283 LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) . LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity.

Targets

PRMT5 (Cell-free assay); PRMT5 (Cell-based assay) 22 nM; 25 nM

In vitro

LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 ± 3 and 25 ± 1 nM, respectively. LLY-283 directly binds to and occupies the SAM pocket. LLY-283 is a low nanomolar enzymatic inhibitor of the PRMT5:MEP50 complex in biochemical assays and is selective for PRMT5 over other methyltransferases including related family members.

In vivo

LLY-283 shows antitumor activity in mouse xenografts when dosed orally and can serves as an excellent probe molecule for understanding the biological function of PRMT5 in normal and cancer cells. LLY-283 can be used as an in vivo tool compound to evaluate the pharmacology of PRMT5 inhibition.

Cell Research(from reference)

Cell lines：Sf9 cells, A375 tumor cells, MCF7 cells 

Concentrations：1 µM, 10 µM 

Incubation Time：48 h