C 646

Bezeichnung:C 646

CAS-Nr328968-36-1

Englisch Name:C 646

CBNumberCB62535667

SummenformelC24H19N3O6

Molgewicht445.42

MOL-Datei328968-36-1.mol

C 646 physikalisch-chemischer Eigenschaften

Schmelzpunkt	224-226℃
Siedepunkt	662.6±65.0 °C(Predicted)
Dichte	1.38±0.1 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: >25mg/mL
Aggregatzustand	powder
pka	4.20±0.10(Predicted)
Farbe	red to brown
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
InChIKey	HEKJYZZSCQBJGB-XDHOZWIPSA-N

Sicherheit

Kennzeichnung gefährlicher	N
R-Sätze:	50
S-Sätze:	61
RIDADR	UN 3077 9 / PGIII
WGK Germany	3

Gefahreninformationscode (GHS)

C 646 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
C-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.
Verwenden
C646 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.
Verwenden
C646 was used to study the role of p300 in chronic neuropathic pain in rats with chronic constriction injury.
Definition
ChEBI: 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 Actions
C646 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.
Lager
Store at +4°C
Einzelnachweise
1) 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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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