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Histone Acetyltransferases

Histone acetyltransferase (HAT) inhibitors target the writers of lysine acetylation on histones and other proteins. Acetylation neutralizes the positive charge of histone tails and favors transcription. In 1996 a Tetrahymena HAT was found to be related to a yeast transcriptional regulator, which linked histone acetylation to gene activation. In the same year the coactivators p300 and CREB-binding protein (CBP) were shown to be histone acetyltransferases. C646, found in 2010 by virtual ligand screening, is a selective inhibitor of the p300/CBP HAT domain. MG149 and NU 9056 target lysine acetyltransferase 5 (KAT5, Tip60), and garcinol is a natural product with broad HAT inhibition. SGC-CBP30 and I-CBP112 bind the CBP/p300 bromodomain rather than the catalytic site.

Cat. No.

A17089

CAS No.

1799824-08-0

E-7386

E-7386 is an orally active CBP/beta-catenin modulator.

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1 mg

$80.00

5 mg

$260.00

All 7 sizes
Cat. No.

A23926

CAS No.

2417097-18-6

JQAD1

JQAD1 is a CRBN-dependent PROTAC selectively targeting EP300 for degradation. It effectively reduces EP300 protein levels and H3K27ac histone acetylation, resulting in apoptosis. JQAD1 is a valuable tool for investigating EP300 function and epigenetic regulation in cellular processes.

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5 mg

$288.00

10 mg

$496.00

All 4 sizes
Cat. No.

A23945

CAS No.

3033714-58-5

JET-209

JET-209 is a potent PROTAC degrader targeting CBP and p300, with DC₅₀ values of 0.05 nM and 0.2 nM, respectively. It is composed of lenalidomide, a linker, and the bromodomain inhibitor GNE-207. JET-209 is a valuable tool for cancer research involving epigenetic regulation.

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1 mg

$486.00

5 mg

$1,458.00

All 4 sizes
Cat. No.

A23966

CAS No.

3037549-86-0

CBPD-409

CBPD-409 is an orally active PROTAC degrader targeting CBP/p300, with a DC₅₀ of 0.2–0.4 nM. It shows potent antiproliferative activity in AR⁺ prostate cancer cell lines (VCaP, LNCaP, 22Rv1) with IC₅₀ values of 1.2–2.0 nM and demonstrates significant antitumor efficacy.

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1 mg

$495.00

5 mg

$1,380.00

All 4 sizes

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