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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
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $55 | In Stock | |
5 mg | $129 | In Stock | |
10 mg | $208 | In Stock | |
25 mg | $423 | In Stock | |
50 mg | $678 | In Stock | |
100 mg | $1,080 | In Stock | |
1 mL x 10 mM (in DMSO) | $178 | In Stock |
Description | 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 |
Targets&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]. |
Alias | (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione |
Molecular Weight | 372.83 |
Formula | C18H13ClN2O3S |
Cas No. | 593273-05-3 |
Smiles | Cc1ccc(cc1Cl)N1C(=S)NC(=O)\C(=C/C=C/c2ccco2)C1=O |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 120 mg/mL (321.86 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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