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ORY-1001 (RG-6016) is the only dual KDM1A/LSD1 inhibitor currently being moved forward to Phase I studies, and it is also the only KDM1A inhibitor in development for the treatment of neurodegenerative disease. In THP-1 (MLL-AF9) cells, ORY-1001 results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers. ORY-1001 also induces apoptosis in THP-1 and inhibits proliferation and colony formation of MV(4;11) (MLL-AF4) cells.
ORY-1001 activated the NOTCH pathway, resulting in the suppression of the transcription factor ASCL1 and the repression of SCLC tumorigenesis. ORY-1001 (<0.020mg/kg, p.o.) leads to significantly reduced tumor growth in rodent MV(4;11) xenografts.
| Molecular Weight | 303.27 |
| Formula | C15H22N2.2HCl |
| CAS Number | 1431326-61-2 |
| Solubility (25°C) | Water 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histone demethylase Products |
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| PFI-90
PFI-90 is a selective inhibitor of histone demethylase (KDM3B) that inhibits PAX3-FOXO1 action. |
| CPI-4203
CPI-4203 is a potent KDM5A inhibitor with an IC50 of 250 nM. |
| KDM2B-IN-4
KDM2B-IN-4 is a histone demethylase KDM2B inhibitor. |
| Zavondemstat
Zavondemstat (QC8222; TACH 101) is an inhibitor of histone lysine demethylase 4D (KDM4D) with antineoplastic activity. |
| Zavondemstat L-lysine
Zavondemstat (QC8222; TACH 101) (L-lysine) is an inhibitor of histone lysine demethylase 4D (KDM4D) with antineoplastic activity. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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