C646, a histone acetyltransferase inhibitor, inhibits p300, with a Ki of 400 nM in cell-free tests. Compared with other acetyltransferases, C646 acts preferentially on p300. C646 can induce cell cycle arrest, apoptosis and autophagy.

 

Brand: BCM

 

Target: Apoptosis; Epigenetic Reader Domain; Histone Acetyltransferase; Autophagy

Signaling Pathways: Apoptosis; Autophagy; Chromatin/Epigenetic

 

In Vitro: C646 is a histone acetyltransferase inhibitor that inhibits p300 with a Ki of 400 nM and selectively acts on other acetyltransferases. 10 μM C646 inhibited 86% p300 in vitro. C646 is a conventional, reversible p300 inhibitor. C646(25μM) acts on cells, reducing histone H3 and H4 acetylation levels and abolishing TSA-induced acetylation. C646(20μM) acts on androgen-sensitive castrated prostate cancer cell lines, inducing apoptosis by interfering with AR and NF-kB pathways. C646 acts on mouse cells to inhibit the dynamic acetylation of all H3K4me3 and locally across the start sites of promoter and inducer genes, thereby interfering with RNA polymerase II interactions and the activation of these genes.

 

Melting Point: 224-226℃

 

Boiling Point: 662.6±65.0 °C(Predicted)

 

pKa: 4.20±0.10(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; insoluble in Ethanol. 

 

GHS: GHS07

 

Isomeric SMILES: CC1=CC(=C(C=C1C)[N+](=O)[O-])C2=CC=C(O2)/C=C\3/C(=NN(C3=O)C4=CC=C(C=C4)C(=O)O)C  

 

InChIKey: HEKJYZZSCQBJGB-UNOMPAQXSA-N  

 

InChI: InChI=1S/C24H19N3O6/c1-13-10-20(21(27(31)32)11-14(13)2)22-9-8-18(33-22)12-19-15(3)25-26(23(19)28)17-6-4-16(5-7-17)24(29)30/h4-12H,1-3H3,(H,29,30)/b19-12-

 

Attribute
[Chem Name]	4-[(4Z)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxopyrazol-1-yl]benzoic acid
[Synonym]	C646; C-646
[CAS No.]	328968-36-1
[MDL No.]	MFCD01784780
[Formula]	C24H19N3O6
[Molecular]	445.42
[Form]	Red to brown powder
[Storage]	Sealed in dry, 2-8°C

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