Signaling Pathway

Epigenetic Reader Domain

Epigenetic Reader Domain

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Epigenetic Reader Domain Inhibitors & Modulators (47)

Product Name Catalog No. Brief Description
(+)-JQ-1

HY-13030

(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2).

(R)-(-)-JQ1 Enantiomer

HY-13030A

(R)-(-)-JQ1 Enantiomer,  the stereoisomer (+)-JQ1,  showed no significant interaction with any bromodomain; (+)-JQ1 is an inhibitor for the BET.

3-Deazaneplanocin A

HY-10442

3-Deazaneplanocin A (DZNep) is an attractive epigenetic anticancer agent through the inhibition of the cellular enhancer of zeste homolog 2 (EZH2) protein.

3-Deazaneplanocin A hydrochloride

HY-12186

3-Deazaneplanocin A hydrochloride(DZNep hydrochloride) is an attractive epigenetic anticancer agent through the inhibition of the cellular enhancer of zeste homolog 2 (EZH2) protein.

ARV-825

HY-16954

ARV-825 is a BRD4 inhibitor with DC50 (50% of maximum degradation) <1nM for Burkitt's lymphoma (BL) cell lines.

BET-BAY 002

HY-12421

BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model.

BET-BAY 002 S enantiomer

HY-12421B

BET-BAY 002 S enantiomer is the S-enantiomer of BET-BAY 002.

BET-IN-1

HY-19760

BET-IN-1 is a bromodomain inhibitor extracted from patent WO/2013024104A1, compound example 2, has a plC50 in the range 6.0 - 7.0.

BI 2536

HY-50698

BI2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM, BI2536 shows 4- and 11-fold greater selectivity against Plk2 and Plk3; BI2536 also is a BRD4 inhibitor(IC50= 25 nM).

BI-7273

HY-100351

BI-7273 is a selective, and cell-permeable BRD9 BD inhibitor.

BI-9564

HY-100352

BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family.

Bromosporine

HY-15815

Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.

CPI-169

HY-15956A

CPI-169 R-enantiomer is the R enantiomer of CPI-169, which is a novel and potent EZH2 inhibitor with IC50 <1 nM(inhibition of the catalytic activity of PRC2); decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines.

CPI-169 racemate

HY-15956

CPI-169 racemate is the racemate form of CPI-169, which is a novel and potent EZH2 inhibitor with IC50 <1 nM(inhibition of the catalytic activity of PRC2); decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines.

CPI-203

HY-15846

CPI 203 is a novel potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay).

CPI-360

HY-15955

CPI-360 is a potent, selectiveEZH2inhibitor with IC50 of 0.5 nM and 2.5 nM nM for wt EZH2 and Y641N EZH2, respectively.

CPI-637

HY-100482

CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.

EI1

HY-15573

EI1 is a potent and selective small molecule inhibitor of EZH2 with IC50 values of 15 nM and 13 nM for wild type EZH2 and EZH2 Y641F mutant, respectively.

EPZ-6438

HY-13803

EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity with Ki value of 2.5±0.5 nM.

EPZ005687

HY-15555

EPZ-005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.