LLY-283

SKU: orb1707062

Description

LLY-283 is a potent, selective, and orally bioavailable inhibitor of the PRMT5:MEP50 complex, demonstrating high affinity with a Kd of 6 nM. It exhibits robust antitumor activity and is a valuable chemical probe for investigating PRMT5 biology in cancer research, both in cellular and animal models.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 2040291-27-6
• MW: 342.35
• Purity: 99.49% (May vary between batches)
• Formula: C₁₇H₁₈N₄O₄
• SMILES: [H][C@@]1(O[C@H]([C@H](O)[C@@H]1O)n1ccc2c(N)ncnc12)[C@H](O)c1ccccc1
• Target: Histone Methyltransferase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (11.68 mM);H2O:3.57 mg/mL (10.43 mM);DMSO:112.5 mg/mL (328.61 mM)

Bioactivity

• Target IC50:
  PRMT5:(ki)6 nM|PRMT5:22 nM|MEP50:(ki)6 nM|MEP50:22 nM
• In Vivo:
  LLY-283 administered orally at a dose of 20 mg/kg daily significantly inhibits tumor growth in A375 cell-bearing mice over a 28-day treatment period.
• 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, and a Kd of 6 nM for the PRMT5:MEP50 complex in vitro; LLY-283 inhibits A375 cell proliferation with an IC50 of 46 nM.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Histone Methyltransferase, HistoneMethyltransferase, MEP50, LLY283, LLY-283, LLY 283, PRMT5

Compound Identifiers

PubChem CID

122669401