ORY-1001 trans and cis isomers

SKU: orb1226293

Description

ORY-1001 (RG-6016) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases; exhibits low nanomolar cellular activity (EC50 < 1 nM) in the THP1 differentiation assay and induces the CD11b marker within 6 hr of treatment in FACS based differentiation assay in THP1 cell line; induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML; exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of AML xenograft models.Blood Cancer Phase 2 Clinical.

Key Properties

• CAS Number: 1431326-61-2
• MW: 303.2704
• Purity: >98% (HPLC)
• Formula: C₁₅H₂₄Cl₂N₂
• SMILES: NC1CCC(N[C@@H]2C[C@H]2C3=CC=CC=C3)CC1.Cl.Cl
• Target: Histone Demethylase
• Solubility: DMSO: < 6.8 mg/mL

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RG 6016 | RG6016 | RG-6016 | ORY1001 | ORY 1001

Quick Database Links

Gene Symbol

Histone Demethylase