C646, p300/CBP Inhibitor

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Blocking Reagent (BR), Inhibition Assay (InhA)
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Purpose A reversible, p300/CBP (CREB-binding protein) histone acetyltransferase (HAT) inhibitor
Characteristics A reversible, p300/CBP (CREB-binding protein) histone acetyltransferase (HAT) inhibitor (Ki = 400 nM). Specific inhibition to p300 (86 %) compared to N-acetyltransferase, PCAF, GCN5, Rtt109, Sas or MOZ histone acetyltransferases (< 10 %). Suppresses histone H3 and H4 acetylation in mouse fibroblast cell lines.
Purity ≥ 98 % by NMR
Chemical Name (E)-4-(4-((5-(4,5-Dimethyl-2-nitrophenyl)furan-2-yl)-methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Formula C₂₄H₁₉N₃O₆
Permeability Cell-permeable
Solubility DMSO (25 mM)
Molecular Weight 445.42 g/mol
CAS-No 328968-36-1
Restrictions For Research Use only
Format Solid
Handling Advice Protect from light and air
Storage -20 °C
Expiry Date 36 months
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Product cited in: Chen, Wang, Uttarwar, vanKrieken, Li, Chen, Gao, Ghayur, Margetts, Krepinsky: "SREBP-1 is a novel mediator of TGFβ1 signaling in mesangial cells." in: Journal of molecular cell biology, Vol. 6, Issue 6, pp. 516-30, 2015 (PubMed).