[CAS NO. 2040291-27-6]  LLY-283

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PRODUCTS SPECIFICATIONS [2040291-27-6]

Catalog
SLK-S8883
Brand
Selleck
CAS
2040291-27-6

DESCRIPTION [2040291-27-6]

Overview

MDL-
Molecular Weight342.35
Molecular FormulaC17H18N4O4
SMILESNC1=C2C(N([C@H]3[C@@H]([C@@H]([C@@H]([C@@H](C4=CC=CC=C4)O)O3)O)O)C=C2)=NC=N1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.9210 mL14.6049 mL29.2099 mL
5 mM0.5842 mL2.9210 mL5.8420 mL
10 mM0.2921 mL1.4605 mL2.9210 mL
50 mM0.0584 mL0.2921 mL0.5842 mL

Description

LLY-283 is a novel and selective inhibitor of . 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 [1]
(Cell-free assay)
PRMT5 [1]
(Cell-based assay)
22 nM25 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.