ORY-1001 trans and cis isomers( RG 6016 | RG6016 | RG-6016 | ORY1001 | ORY 1001 )

Catalog No. M11827 CAS No. 1431326-61-2

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Product Name

ORY-1001 trans and cis isomers
Note

Research use only, not for human use.
Brief Description

ORY-1001 (RG-6016) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM.
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.
In Vitro

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In Vivo

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Synonyms

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

Chromatin/Epigenetic
Target

Histone Demethylase
Recptor

LSD1/KDM1A
Research Area

Cancer
Indication

Blood cancer

CAS Number

1431326-61-2
Formula Weight

303.2704
Molecular Formula

C15H24Cl2N2
Purity

>98% (HPLC)
Solubility

DMSO: < 6.8 mg/mL
SMILES

NC1CCC(N[C@@H]2C[C@H]2C3=CC=CC=C3)CC1.Cl.Cl
Chemical Name

1,4-Cyclohexanediamine, N1-[(1R,2S)-2-phenylcyclopropyl]-, hydrochloride (1:2), rel-

1. Maes T, et al. Cancer Cell. 2018 Mar 12;33(3):495-511.e12.

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