C646

Catalog #

27613-1

$170 *

Size: 10 mg

Qty

Bulk/Custom

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Description

C646, a pyrazolone-containing small molecule, is a cell-permeable histone acetyltransferase (HAT) inhibitor that competitively and selectively inhibits the HAT activity of p300, a transcriptional co-activator involved in a variety of gene regulatory pathways and protein acetylation events, with the Ki value of 400 nM and an IC50 value of 1.6 µM .

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Synonyms

4-[(4Z)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxopyrazol-1-yl]benzoic acid

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Product Data Gallery

Product Info

Storage and Usage

Citations

Target(s)

p300

Formula

C₂₄H₁₉N₃O₆

445.4 Da

Solubility

Soluble in DMSO

CAS Registry #

328968-36-1

Background

C646 binds to p300 as the Z-isomer forming hydrogen bonds between Thr1411, tYR1467, Trp1466 and Arg1410 on the side chains of p300 and oxygen atoms of C646. C646 is also capable of inhibiting a variety of p300 HAT mutants, including T1411A, Y1467F, W1466F and R1410A with IC50 values of 3.4 µM, 7 µM, 5 µM and 2.5 µM respectively.

References

Bowers EM, et al. Chem Biol. 2010 May 28;17(5):471-82.

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