ORY-1001 free base

TargetMol
Product Code: TAR-T28269
Supplier: TargetMol
CodeSizePrice
TAR-T28269-5mg5mg£850.00
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TAR-T28269-50mg50mg£1,661.00
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Quantity:
TAR-T28269-100mg100mg£2,079.00
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Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

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Further Information

Bioactivity:
ORY-1001 is a KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A/B, IL4I1, KDM1B >100uM, SMOX 7uM). Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers (EC50 me2H3K4 and FACS CD11b <1nM). ORY-1001 induces apoptosis in THP-1 and inhibits proliferation and colony formation of MV(4;11) (MLL-AF4) cells (EC50 <1nM). ORY-1001 does not inhibit non-related histone modifiers.
CAS:
1431304-21-0
Formula:
C15H22N2
Molecular Weight:
230.355
Purity:
0.98
SMILES:
NC1CCC(CC1)N[C@@H]1C[C@H]1c1ccccc1

References

1. Hosseini A, Minucci S. A comprehensive review of lysine-specific demethylase 1 and its roles in cancer. Epigenomics. 2017 Aug;9(8):1123-1142. doi: 10.2217/epi-2017-0022. Epub 2017 Jul 12. PubMed PMID: 28699367. 2. Zheng YC, Yu B, Jiang GZ, Feng XJ, He PX, Chu XY, Zhao W, Liu HM. Irreversible LSD1 Inhibitors: Application of Tranylcypromine and Its Derivatives in Cancer Treatment. Curr Top Med Chem. 2016;16(19):2179-88. Review. PubMed PMID: 26881714. 3. Maes T, Mascar? C, Ortega A, Lunardi S, Ciceri F, Somervaille TC, Buesa C. KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease. Epigenomics. 2015;7(4):609-26. doi: 10.2217/epi.15.9. Review. PubMed PMID: 26111032.