ORY-1001-trans - Histone Demethylase 抑制劑 - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEORY-1001(trans)Cat. No.: HY-12782TCAS No.: 1431303-72-8分式: CHClN分量: 303.27作靶點: Histone Demethylase作通路: Epigenetics儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 H2O : 57.75 mg/mL (190.42 mM; Need

2、 ultrasonic and warming)DMSO : 0.69 mg/mL (2.28 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.2974 mL 16.4870 mL 32.9739 mL5 mM 0.6595 mL 3.2974 mL 6.5948 mL10 mM 0.3297 mL 1.6487 mL 3.2974 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 OR

3、Y-1001 trans種不可逆的選擇性賴氨酸特異性脫甲基酶 1A (KDM1A/LSD1) 抑制劑。IC50 & Target KDM1A/LSD1 1體外研究ORY-1001 trans is a KDM1A inhibitor that inactivate KDM1A by irreversible binding to the flavin adeninenucleotide (FAD) cofactor. ORY-1001 trans has very high selectivity for KDM1A over the MAO enzymes, high1/2 Master o

4、f Small Molecules 您邊的抑制劑師www.MedChemEselectivity over KDM1B and unrivaled subnanomolar cellular activity in differentiation and colony formationassays on mixed lineage leukemia (MLL)-translocated acute myeloid leukemia (AML) cell lines. ORY-1001provokes a time and dose-dependent induction of the Cd1

5、1b differentiation marker in MLL-AF9 cells, whichinterestingly preceeds changes in H3K4me2 levels. While MLL-translocated cells are especially sensitive,other acute leukemia (AL) cell lines also respond to ORY-1001 trans 1.體內(nèi)研究 ORY-1001 trans reduces AML tumor growth in mice and rat xenografts and i

6、ncreases survival time in adisseminated model of T-ALL 1.REFERENCES1. Maes T, et al. 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.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-8