HKMTI-1-005

Chemical Structure : HKMTI-1-005

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货号: PC-20645Not For Human Use, Lab Use Only.

HKMTI-1-005 is a potent, substrate-competitive dual inhibitor of EZH2 and the closely related G9a/GLP H3K9 methyltransferases with IC50 of 0.1 uM (EHMT2).

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生物&药学活性

HKMTI-1-005 is a potent, substrate-competitive dual inhibitor of EZH2 and the closely related G9a/GLP H3K9 methyltransferases with IC50 of 0.1 uM (EHMT2).
HKMTI-1-005 inhibits MDA-MB-231 cell growth with IC50 of 4.3 uM in MTT assays, induces apoptosis in MDA-MB-231 cells in a dose-dependent manner, as measured by Caspase 3/7 activity.
HKMTI-1-005 induces chromatin changes that resulted in the transcriptional activation of immunostimulatory gene networks, including the re-expression of elements of the ERV-K endogenous retroviral family.
HKMTI-1-005 improved the survival of mice bearing Trp53-/- null ID8 ovarian tumors and resulted in tumor burden reduction.
HKMTI-1-005 phenocopied EZH2 knockdown and was more effective in inducing differentiation than GSK-343.

物理化学性质&存储条件

分子量	476.63
分子式	C27H36N6O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methylpiperazin-1-yl)quinazolin-4-amine

参考文献

1. Spiliopoulou P, et al. Mol Cancer Ther. 2022 Apr 1;21(4):522-534.

2. Curry E, et al. Clin Epigenetics 2015;7:84.

3. Y Sbirkov, et al. Front Cell Dev Biol. 2023 Mar 23;11:1076458.

4. Srimongkolpithak N, et al. Med Chem Commun. 2014.

HKMTI-1-005

生物&药学活性

物理化学性质&存储条件

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HKMTI-1-005

生物&药学活性

物理化学性质&存储条件

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