C 646

C 646 Basic information
Product Name:C 646
Synonyms:C 646;(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;(Z)-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;4-[4-[[5-(4,5-Dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl]-benzoic acid;Benzoic acid, 4-[4-[[5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl]-;4-[4-[[5-(4,5-Dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl]-benzoic acid C646;C 646 4-[4-[[5-(4,5-Dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl]-benzoic acid;C646, p300/CBP Inhibitor
CAS:328968-36-1
MF:C24H19N3O6
MW:445.42
EINECS:
Product Categories:Inhibitors
Mol File:328968-36-1.mol
C 646 Structure
C 646 Chemical Properties
Melting point 224-226℃
Boiling point 662.6±65.0 °C(Predicted)
density 1.38±0.1 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO: >25mg/mL
form powder
pka4.20±0.10(Predicted)
color red to brown
Stability:Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
InChIKeyHEKJYZZSCQBJGB-XDHOZWIPSA-N
Safety Information
Hazard Codes N
Risk Statements 50
Safety Statements 61
RIDADR UN 3077 9 / PGIII
WGK Germany 3
MSDS Information
C 646 Usage And Synthesis
DescriptionC-646 (328968-36-1) is a potent and selective inhibitor of the histone acetyl transferase p300/CBP (Ki=400 nM ). Induces apoptosis in prostate cancer cells. C-646 enhances fear extinction memory and synaptic plasticity in mice. Promotes tau deacetylation reducing levels of pathogenic p-tau. Cell permeable.
UsesC646 is an inhibitor for histone acetyltransferase p300 and may be a potential candidate for treating AML1-ETO (AE) positive acute myeloid leukemia (AML). It is shown that C646 inhibited cellular proliferation, reduced colony formation, evoked partial cell cycle arrest in the G1 phase, and induced apoptosis in AE-positive AML cell lines and primary blasts isolated from leukemic mice and AML patients.
UsesC646 was used to study the role of p300 in chronic neuropathic pain in rats with chronic constriction injury.
DefinitionChEBI: A pyrazolone that is 5-methyl-4-methylene-2-(p-carboxyphenyl)-2,4-dihydro-3H-pyrazol-3-one in which the exocyclic carbon of the methylene group is attached to a 5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl group by a single bond C646 is a potent, cell permeable and selective competitive inhibitor of p300 and CBP (p300/CBP) histone acetyltransferases.
Biochem/physiol ActionsC646 is a potent, cell permeable and selective inhibitor of p300 and CBP (p300/CBP) histone acetyltransferases. Inhibition of p300/CBP by C646 affects the activity of a variety of transcriptional factors such as NF-κB, p53 and MyoD that are associated with physiology, disease processes, hippocampal synaptic plasticity, spatial memory and contextual fear.
storageStore at +4°C
References1) Bowers et al. (2010), Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor; Chem. Biol., 17 471 2) Santer et al. (2011), Inhibition of the acetyltransferases p300 and CBP reveals a targetable function for p300 in the survival and invasion pathways of prostate cancer cell lines; Mol. Cancer Ther., 10 1644 3) Marek et al. (2011), Paradoxical enhancement of fear extinction memory and synaptic plasticity by inhibition of the histone acetyltransferase p300; J. Neurosci.., 31 7486 4) Min et al. (2010), Acetylation of tau inhibits its degradation and contributes to tauopathy; Neuron, 67 953
C 646 Preparation Products And Raw materials
LY 294002 HYDROCHLORIDE (E)-3-[[[3-[2-(7-CHLORO-2-QUINOLINYL)ETHENYL]PHENYL]-[[(3-DIMETHYLAMINO)-3-OXOPROPYL]THIO]METHYL]THIO]-PROPANOIC ACID, SODIUM SALT (2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol 6-CHLORO-2,3,4,9-TETRAHYDRO-1H-CARBAZOLE-1-CARBOXAMIDE GSK J4 HCl Adapalene MG149 CYCLOPAMINE TCPOBOP TRICHOSTATIN A

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