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Epigenetic Reader Domain

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Cat. No. Product Name Field of Application Chemical Structure
DC72179 UNC1021 Featured
UNC1021 is a selective L3MBTL3 inhibitor with an IC50 of 0.048 μM.
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DC71321 ET-JQ1-OH Featured
ET-JQ1-OH is an allele-specific BET inhibitor.
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DC42491 GSK778(iBET-BD1 dihydrochloride) Featured
GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.
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DC46835 Ziftomenib Featured
Ziftomenib is a menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151).
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DC48075 SGC-SMARCA-BRDVIII Featured
SGC-SMARCA-BRDVIII is a potent and selective SMARCA2/4 BRD inhibitor.
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DC47977 I-BET567 Featured
I-BET567 is a potent and oral active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.
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DC46500 I-BET282E Featured
I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD).
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DC47894 SR-0813 Featured
SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC50 and EC50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC50 and EC50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia.
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DC41049 Trotabresib (CC-90010) Featured
Trotabresib (CC-90010) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors.
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DC46003 GSK097 Featured
GSK097 is a potent and selective Inhibitor of the second bromodomain (BD2) of the bromodomain and extra-terminal domain (BET) proteins. GSK097 displays 2000-fold selective for BD2 over BD1 (BRD4 data) with >1 mg/mL solubility in FaSSIF media.
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DC48139 NVS-BET-1 Featured
NVS-BET-1 is a BET bromodomain inhibitor that regulates keratinocyte plasticity.
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DC72030 GNE-064 Featured
GNE-064 (compound 5) is a selective, oral and highly soluble inhibitor of the SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of drug synthesis.
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DC72610 Physachenolide C
Physachenolide C is a potent and selective BET inhibitor that induces apoptosis and arrests the cell cycle in the G0-G1 phase, with antitumor activity.
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DC42300 GSK620 Featured
GSK620 is a potent and orally active pan-BD2 with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620
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DC72325 I-BET432
I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases.
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DC71746 QA-68
QA-68 (QA-68-ZU81) is a potent bromodomain-containing protein 9 (BRD9) degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines.
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DC71504 Thalidomide-NH-C4-NH-Boc
Thalidomide-NH-C4-NH-Boc is a novel, potent, and selective class of Bromodomain-containing protein 4 (BRD4) and Bromodomain-containing protein 2 (BRD2) degrader for the development of therapeutics to treat cancers.
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DC71503 PROTAC_ERRα
PROTAC_ERRα is a potent and selective ERRα degrader. PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%.
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DC71320 (2S,3R)-LP99
(2S,3R)-LP99 is a potent and selective BRD7 and BRD9 inhibitor with an KD of 99 nM for BRD9. (2S,3R)-LP99 inhibits the association of BRD7 and BRD9 to acetylated histones in vitro and in cells. (2S,3R)-LP99 demonstrates that BRD7/9 plays a role in regulating pro-inflammatory cytokine secretion.
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DC71319 OXFBD02
OXF BD 02 is a selective inhibitor of BRD4(1) (the first bromodomain of BRD4) with IC50 value of 382 nM.
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DC71230 SDR-04
SDR-04 is a BET inhibitor and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation.
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DC70972 MI-1
MI-1 inhibits Menin-MLL interaction with an IC50 of 1.9 μM.
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DC49605 CREB-IN-1 TFA
CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth.
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DC49603 BRD4 Inhibitor-16
BRD4 Inhibitor-16 (Compound 4) is a potent inhibitor of bromodomain 4 (BRD4). Overexpression of bromodomain 4 (BRD4) is closely correlated with a variety of human cancers by regulating the histone post-translational modifications. BRD4 Inhibitor-16 represents a useful tool for explorative studies of BRD4 inhibition, such as an improved understanding of BRD4 inhibitor release-related information.
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DC49602 BRD4 Inhibitor-17
BRD4 Inhibitor-17 (Compound 5i) is a potent inhibitor of BRD4 with an IC50 of 0.33 μM. BRD4 Inhibitor-17 plays crucial role in regulating transcription of inflammatory, proliferation and cell cycle genes. BRD4 Inhibitor-17 serves as potential antidotes for arsenicals.
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DC49600 PARP1/BRD4-IN-1
PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells.
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DC49599 (R,S)-CFT8634
(R,S)-CFT8634 is a selective and orally active BRD9 protein degrader. (R,S)-CFT8634 has the potential for the research of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation (extracted from patent WO2021178920A1, compound 176).
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DC49598 (R,R)-CFT8634
(R,R)-CFT8634 is a selective and orally active BRD9 protein degrader. (R,R)-CFT8634 has the potential for the research of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation (extracted from patent WO2021178920A1, compound 175).
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DC49597 FHT-1204
FHT-1204 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM (WO2020160180A1; compound 70).
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DC49596 FHT-1015
FHT-1205 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM (WO2020160180A1; compound 67).
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