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DCH36_06

SKU: orb1298142

Description

DCH36_06 is a potent and selective small molecule inhibitor of the p300/CBP histone acetyltransferase. This compound is used in research to probe epigenetic mechanisms in vitro and has shown activity in cellular models of oncology and other diseases dependent on transcriptional coactivators.

Research Area

Cell Biology, Epigenetics & Chromatin

Images & Validation

Key Properties

CAS Number593273-05-3
MW372.83
Purity98.32% (May vary between batches)
FormulaC18H13ClN2O3S
SMILESCc1ccc(cc1Cl)N1C(=S)NC(=O)\C(=C/C=C/c2ccco2)C1=O
TargetHistone Acetyltransferase,Apoptosis,Epigenetic Reader Domain
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (10.73 mM);DMSO:120 mg/mL (321.86 mM)

Bioactivity

Target IC50
CBP:3.2 μM|p300:0.6 μM 
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.
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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

p300, EpigeneticReaderDomain, Epigenetic Reader Domain, HATs, HAT, Inhibitor, hypoacetylation, Histone Acetyltransferase, HistoneAcetyltransferase, inhibit, (5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione, Apoptosis, antiproliferative, anti-tumor, DCH36_06, DCH-36_06, CBP
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Key Properties

No computed properties available.

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DCH36_06 (orb1298142)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 1,040.00
5 mg
¥ 1,560.00
1 ml x 10 mM (in DMSO)
¥ 1,820.00
10 mg
¥ 2,210.00
25 mg
¥ 3,900.00
50 mg
¥ 5,850.00
100 mg
¥ 8,970.00
200 mg
¥ 11,830.00
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