You are here:Home-Inhibitors & Agonists-Epigenetics-Histone Demethylase

Request The Product List ofHistone Demethylase Histone Demethylase

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-61739

QC-6352

1851373-36-8

QC-6352 is a potent and selective KDM4 family inhibitor with IC50 of 104, 56, 35, and 104 nM for KDM4A, KDM4B, KDM4C, and KDM4D, respectively; displays high selectivity over other KDM family members, with the exception of KDM5B (IC50=750 nM); shows a promising cellular potency (KYSE-150 EC50=3.5 nM, H3K36 MOA=1.5 nM); has excellent physical properties and drug-like characteristics, exhibits favorable in vivo efficacy in a breast cancer PDX model and reduces the tumor initiating cell populations which are associated with resistance to chemotherapy treatments.

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-35903

T-448 free base

1597426-52-2 T-448 free base (T448) is a specific inhibitor of LSD1 enzyme activity, enhances H3K4 methylation in primary cultured rat neurons but has little impact on LSD1-GFI1B complex in human TF-1a erythroblasts; increases brain H3K4 methylation and partially restored learning function in mice with NMDA receptor hypofunction, shows unique therapeutic approaches for central nervous system disorders associated with epigenetic dysregulation.
PC-35902

T-448

1597426-53-3 T-448 (T448) is a specific inhibitor of LSD1 enzyme activity, enhances H3K4 methylation in primary cultured rat neurons but has little impact on LSD1-GFI1B complex in human TF-1a erythroblasts; increases brain H3K4 methylation and partially restored learning function in mice with NMDA receptor hypofunction, shows unique therapeutic approaches for central nervous system disorders associated with epigenetic dysregulation.
PC-35801

KDM5A covalent inhibitor N73

KDM5A covalent inhibitor N73 is the the isopropyl ester derivative of N71, an irreversible KDM5A inhibitor (IC50=0.22 uM) that covalently interacts with Cys481, >20-fold selectivity over KDM4A.

Request The Product List

* Indicates a Required FieldYour information is safe with us.

  • *Product List:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Country:
  • Additional Information:
Contact Us sales@probechem.com