[CAS NO. 328968-36-1] C646

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PRODUCTS SPECIFICATIONS [328968-36-1]

Catalog

HY-13823

Brand

MCE

CAS

328968-36-1

DESCRIPTION [328968-36-1]

Overview

MDL	MFCD01784780
Molecular Weight	445.42
Molecular Formula	C24H19N3O6
SMILES	O=C(O)C1=CC=C(N2N=C(C)/C(C2=O)=C\C3=CC=C(C4=CC(C)=C(C)C=C4[N+]([O-])=O)O3)C=C1

For research use only. We do not sell to patients.

36 Publications Citing Use of MCE

Summary

C646 is a selective and competitive histone acetyltransferase p300 inhibitor with K _i of 400 nM, and is less potent for other acetyltransferases ^[1] .

IC50 & Target

Ki: 400 nM (histone acetyltransferase p300)

In Vitro

C646 is a linear competitive inhibitor of p300 versus acetyl-CoA with a K _i of 400 nM. C646 shows a noncompetitive pattern of p300 inhibition versus H4-15 peptide substrate. C646 treatment reduces histone H3 and H4 acetylation levels and abrogates TSA-induced acetylation in cells. C646 has a more potent effect on cell growth than Lys-CoA-Tat does ^[1] . C646 enhances mitotic catastrophe after IR and suppresses phosphorylation of CHK1 after IRin A549 cells ^[2] . C646 attenuates the increased acetylation of GATA1 and the increased transcriptional activity of GATA1 induced by EDAG ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Suppression of P300 by c646 (intraperitoneally injected, 30 nmol/g/d for 2 weeks) dramatically reduces the level of blood glucose in db/db mice ^[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Fourteen-week-old male db/db mice and normal m/m mice ^[4]
Dosage:	30 nmol/g
Administration:	Intraperitoneally injected; daily; 2 weeks
Result:	The db/db mice showed greater body masses and higher levels of fasting blood glucose than the m/m mice.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 16.67 mg/mL ( 37.43 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2451 mL	11.2254 mL	22.4507 mL
5 mM	0.4490 mL	2.2451 mL	4.4901 mL
10 mM	0.2245 mL	1.1225 mL	2.2451 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: 1.67 mg/mL (3.75 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 1.67 mg/mL (3.75 mM); Suspended solution; Need ultrasonic

* All of the co-solvents are available by MCE.

References

Synonyms

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

C 646