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Chemical Structure : HKMTI-1-005
Catalog No.: 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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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.
| M.Wt | 476.63 | |
| Formula | C27H36N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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.
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