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Cat. No. Product Name CAS No. Information
PC-43206

ORY-1001 trans and cis isomers

1431326-61-2

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

PC-61398

Seclidemstat

1423715-37-0

Seclidemstat (SP-2577, SP2577) is a potent, selective LSD1 inhibitor with IC50 of 127 nM, reduces tumor volume in vivo.

PC-60264

T-3775440

1422620-34-5

T-3775440 is a novel potent, selecitve, irreversible LSD1 inhibitor with IC50 of 2.1 nM; displays high selectivity for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B); disrupts the interaction between LSD1 and growth factor-independent 1B (GFI1B) in leukemia cell lines, exhibites significant antitumor efficacy in AEL and AMKL xenograft models.

PC-35471

Vafidemstat

1357362-02-7 Vafidemstat is a novel potent, selective lysine-specific histone demethylase (LSD1) inhibitor.
PC-35458

ORY-1001 dihydrochloride

1431303-72-8 ORY-1001 dihydrochloride (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.

Blood Cancer

Phase 2 Clinical

PC-35457

ORY-1001

1431304-21-0 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.

Blood Cancer

Phase 2 Clinical

PC-35295

CBB3001

1639358-50-1 CBB3001 (CBB-3001) is a novel potent, selective histone demethylase LSD1 inhibitor with IC50 of 21.25 uM; potently inhibits LSD1 activity both in vitro and in vivo; CBB3001 also selectively inhibits the growth of human ovarian teratocarcinoma PA-1 and mouse embryonic carcinoma F9 cells, caused the downregulation of pluripotent stem cell proteins SOX2 and OCT4, does not have significant inhibition on the growth of human colorectal carcinoma HCT116 cells or mouse fibroblast NIH3T3 cells that do not express these stem cell proteins.

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