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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $33 | In Stock | In Stock | |
| 5 mg | $77 | In Stock | In Stock | |
| 10 mg | $125 | In Stock | In Stock | |
| 25 mg | $253 | In Stock | In Stock | |
| 50 mg | $407 | In Stock | In Stock | |
| 100 mg | $648 | In Stock | In Stock | |
| 200 mg | $870 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $91 | In Stock | 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]. |
| Synonyms | (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 |
| Color | Orange |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 120 mg/mL (321.86 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (10.73 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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