1431304-21-0
1431304-21-0 structure
- Name: ORY-1001
- Chemical Name: ORY-1001
- CAS Number: 1431304-21-0
- Molecular Formula: C17H22N2O2
- Molecular Weight: 286.375
- Create Date: 2022-07-02 16:50:08
- Modify Date: 2024-01-08 18:37:09
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ORY-1001 (RG-6016, Ladademstat) 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.
| Name | ORY-1001 |
|---|
| Description | ORY-1001 (RG-6016, Ladademstat) 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. |
|---|---|
| References | 1. Maes T, et al. Cancer Cell. 2018 Mar 12;33(3):495-511.e12. |
| Molecular Formula | C17H22N2O2 |
|---|---|
| Molecular Weight | 286.375 |