Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DCH36_06 ((5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione) as a bona fide is a potent p300/CBP inhibitor
説明 | DCH36_06 ((5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione) as a bona fide is a potent p300/CBP inhibitor |
ターゲット&IC50 | CBP:3.2 μM, p300:0.6 μM |
In vitro | DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. The suppression of p300/CBP activity retarded cell proliferation in several leukemic cell lines.In addition, DCH36_06 arrested cell cycle at G1 phase and induced apoptosis via activation of capase3, caspase9 and PARP that elucidated the molecular mechanism of its anti-proliferation activity. In transcriptome analysis, DCH36_06 altered downstream gene expression and apoptotic pathways-related genes verified by real-time PCR[1]. |
In vivo | DCH36_06 blocked the leukemic xenograft growth in mice supporting its potential for?in vivo?use that underlies the therapeutic potential for p300/CBP inhibitors in clinical translation[1]. |
別名 | (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione |
分子量 | 372.83 |
分子式 | C18H13ClN2O3S |
CAS No. | 593273-05-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 120 mg/mL (321.86 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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DCH36_06 593273-05-3 Apoptosis Chromatin/Epigenetic Epigenetic Reader Domain Histone Acetyltransferase HATs hypoacetylation DCH-36_06 inhibit antiproliferative p300 HAT Inhibitor (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione anti-tumor CBP inhibitor