LLY-283

For research use only.

Catalog No.S8883

LLY-283 Chemical Structure

CAS No. 2040291-27-6

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.

Purity & Quality Control

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Biological Activity

Description 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 [1]
(Cell-free assay)
PRMT5 [1]
(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.[1]

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.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: Sf9 cells, A375 tumor cells, MCF7 cells
  • Concentrations: 1 µM, 10 µM
  • Incubation Time: 48 h
  • Method:

    PRMT5 cellular assay. MCF7 cells are grown in DMEM supplemented with 10% FBS, penicillin (100 units/ml) and streptomycin (100 µg/ml). 40% confluent cells are treated with different concentrations of LLY-283 or DMSO control for 48 h. The levels of SmBB' and symmetrically dimethylated SmBB' are analyzed in westernblot.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: SCID mice with A375 derived xenografts
  • Dosages: 20 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 68 mg/mL (198.62 mM)
Water 5 mg/mL (14.6 mM)
Ethanol 3 mg/mL (8.76 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 342.35
Formula

C17H18N4O4

CAS No. 2040291-27-6
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC=C(C=C1)C(C2C(C(C(O2)N3C=CC4=C(N=CN=C43)N)O)O)O

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID