Search Result
Results for "
BRD
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-116830B
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(R)-BRD0705
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GSK-3
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Cancer
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BRD5648 ((R)-BRD0705) is a negative control of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) .
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-
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- HY-100719
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HDAC
HIV
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Infection
Cardiovascular Disease
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BRD-6929 is a potent, selective brain-penetrant inhibitor of class I histone deacetylase HDAC1 and HDAC2 inhibitor with IC50 of 1 nM and 8 nM, respectively. BRD-6929 shows high-affinity to HDAC1 and HDAC2 with Ki of 0.2 and 1.5 nM, respectively. BRD-6929 can be used for mood-related behavioral model research .
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- HY-141715
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Antibiotic
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Infection
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BRD-8000.3, as a specific EfpA inhibitor, is a narrow-spectrum, bactericidal antimycobacterial agent with good wild-type activity. BRD-8000.3 can be used for the research of tuberculosis .
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-
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- HY-13498
-
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STK33
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Cancer
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BRD-8899 is a STK33 inhibitor, with an IC50 of 11 nM .
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-
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- HY-149519
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-28 (Compound 18) is an orally active BRD4 Inhibitor. BRD4 Inhibitor-28 inhibits BRD40-BD1, BRD40-BD2 with IC50s of 15, 55 nM. BRD4 Inhibitor-28 also inhibits BRD2-BD1, BRD3-BD1, BRDT-BD1 with IC50s of 19, 25, 68 nM. BRD4 Inhibitor-28 has anti-melanoma activity .
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-
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- HY-149421
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Epigenetic Reader Domain
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Cancer
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BRD7-IN-3 (compound 1-78) is a dual inhibitor of bromodomain-containing proteins BRD7/BRD9 with IC50s of 1.6 μM and 2.7 μM respectively .
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-
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- HY-161368
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-
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- HY-149420
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Epigenetic Reader Domain
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Others
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BRD7-IN-2 (compound 2-77) is a potent inhibitor of bromodomain-containing protein 7 (BRD7), targeting to prostate cancer cells. BRD7-IN-2 is selective for BRD7 rather than BRD9, with IC50s of 5.4 μM, and >300 μM, respectively.
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- HY-156401
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Epigenetic Reader Domain
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Cancer
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BRD9 Degrader-1 is a BRD9 degrader. BRD9 Degrader-1 exhibits micromolar binding affinity to BRD9 and nanomolar affinity for the ternary complex with BRD9 and VCB .
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-
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- HY-160672
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-
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- HY-104072
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-
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- HY-153751
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Epigenetic Reader Domain
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Cancer
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BRD4-IN-4 (Compound 1) is a BRD4 inhibitor (IC50=6.83 μM). BRD4-IN-4 selectively inhibits MV4-11 cell line proliferation and arrests cell at G1 phase. BRD4-IN-4 can be used for research of MLL leukemia .
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- HY-111905
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Epigenetic Reader Domain
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Cancer
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BRD7-IN-1, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively) .
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-
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- HY-141843
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-
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- HY-148730
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CRISPR/Cas9
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Others
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BRD7586 is a cell-permeable small-molecule inhibitor of SpCas9. BRD7586 is the smallest known anti-CRISPR .
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-
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- HY-160670
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-
-
- HY-160671
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-
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- HY-116785
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DNA/RNA Synthesis
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Cancer
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BRD32048 is a direct binder of ETV1 with a KD of 17.1 μM. BRD32048 modulates both ETV1-mediated transcriptional activity and invasion of ETV1-driven cancer cells. BRD32048 inhibits ETV1 acetylation and promotes its degradation. BRD32048 acts as a top candidate ETV1 perturbagen .
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- HY-155078
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-27 (compound 6) is a BRD4 inhibitor with IC50 of 9.6 and 11.3 μM for BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-27 has the potential to study cancer .
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- HY-160662
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Epigenetic Reader Domain
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Cancer
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BRD4-IN-5 (example 51) is a BRD4 inhibitor. The Ki values of the two BRD4 domains BDI_K57-E168 and BDII_E352-M457 are 9.7 nM and 16.1 nM, respectively. BRD4-IN-5 can be used in cancer research .
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- HY-152209
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-26 is a bromodomain protein 4 (BRD4) inhibitor/nitric oxide-donator. BRD4 Inhibitor-26 inhibits BRD4 (BD1) and BRD4 (BD2) with IC50 values of 0.82 μM and 1.94 μM, respectively. BRD4 Inhibitor-26 can be used for the research of ovarian cancer .
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- HY-123494
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Others
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Cardiovascular Disease
Neurological Disease
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BRD0418 is a diversity-oriented synthesis (DOS) molecule that regulates the expression of tribbles pseudokinase 1. BRD0418 has the effect of causing hot lipoprotein metabolism from fat production to clearance. BRD0418 can be used in the study of coronary artery disease (CAD) .
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- HY-117822
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GSK-3
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Neurological Disease
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BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases .
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- HY-160634
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- HY-146208
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer .
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- HY-122586
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CDK
Interleukin Related
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Inflammation/Immunology
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BRD6989, an analog of the natural product cortistatin A (dCA), inhibits CDK8 and upregulates IL-10. BRD6989 selectively binds a complex of CDK8 with an IC50 of ~200 nM. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes .
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- HY-115926
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Epigenetic Reader Domain
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Cancer
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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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- HY-146739
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-19 is a BET inhibitor with an IC50 of 55 nM for BRD4-BD1. BRD4 Inhibitor-19 can be used for multiple myeloma research .
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- HY-128597
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Epigenetic Reader Domain
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Cancer
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BRD-IN-3 ((R,R)-36n) is a highly potent PCAF bromodomain (BRD) inhibitor, with an IC50 of 7 nM. BRD-IN-3 also exhibits activity against GCN5 and FALZ .
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- HY-111433
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PROTACs
Epigenetic Reader Domain
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Cancer
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BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a Kd of 44 nM for Brd4 BD2 in cells.
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- HY-145413
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Glutathione S-transferase
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Cancer
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BRD2889 is an analog of the alkaloid piperlongumine. BRD2889 is a robust modulator of the GSTP1-ISCU axis in pulmonary hypertension (PH) . BRD2889 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-147573
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-23 is a potent and orally active BRD4 inhibitor with IC50s of 6.21 nM and 1.44 nM for BRD4 BD-1 and BRD4 BD-2, respectively (WO2022033542A1; Example 1) .
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- HY-163413
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- HY-146660
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c-Myc
Epigenetic Reader Domain
Apoptosis
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Cancer
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BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with an IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity .
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- HY-19618
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BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency .
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- HY-116830
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BRD0705
1 Publications Verification
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GSK-3
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Cancer
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BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research .
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- HY-139672
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Parasite
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Infection
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BRD5018 is an antimalarial agent. BRD5018 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-151972
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Epigenetic Reader Domain
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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BRD4 Inhibitor-25 is a BRD4 inhibitor with IC50s of 0.82 μM, 1.94 μM for BD1 and BD2 domains of BRD4. BRD4 Inhibitor-25 induces apoptotic and autophagy cell death in ovarian cancer cells. BRD4 Inhibitor-25 can be used in the research of cancers, cardiovascular, neuromuscular and inflammatory disorders.
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- HY-157460
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-29 (SQ-17) is a BRD4 inhibitor, with an IC50 of <100 nM. BRD4 Inhibitor-29 shows antiproliferative effect against prostate cancer cells .
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- HY-110208
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BRD9876
1 Publications Verification
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Kinesin
Microtubule/Tubulin
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Cancer
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BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research .
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- HY-111905A
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Epigenetic Reader Domain
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Cancer
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BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively) .
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- HY-145909
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Epigenetic Reader Domain
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Cancer
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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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- HY-117709
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HDAC
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Neurological Disease
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BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model .
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- HY-160499
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- HY-143299
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-
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- HY-117491
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC50 of 8 nM .
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- HY-143300
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-
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- HY-145260
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Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
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Cancer
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BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
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- HY-112719
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HDAC
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Cancer
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BRD 4354 is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively.
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- HY-15647
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BRD9539
1 Publications Verification
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Histone Methyltransferase
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Cancer
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BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1 .
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- HY-143235
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Epigenetic Reader Domain
Apoptosis
Bcl-2 Family
Caspase
c-Myc
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Cancer
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BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .
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- HY-111102
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- HY-132309
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BRD0639
1 Publications Verification
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Histone Methyltransferase
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Cancer
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BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities .
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- HY-112719B
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HDAC
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Cancer
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BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively .
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- HY-142704
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Epigenetic Reader Domain
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Cancer
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BRD4 D1-IN-1 is a selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-1 has 18 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC .
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- HY-136251
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CRISPR/Cas9
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Infection
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BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay .
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- HY-125197
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Autophagy
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Inflammation/Immunology
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BRD5631 is an autophagy enhancer, enhances autophagy through an mTOR-independent pathway. BRD5631 affects several cellular disease phenotypes previously linked to autophagy, including protein aggregation, cell survival, bacterial replication, and inflammatory cytokine production .
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- HY-117554
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HDAC
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Cancer
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BRD9757 is a potent, capless and selective HDAC6 inhibitor with an IC50 of 30 nM. BRD9757 shows excellent selectivity toward HDAC6 versus the class I (>20-fold) and class II (>400-fold) HDACs .
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- HY-115497
-
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E1/E2/E3 Enzyme
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Infection
Inflammation/Immunology
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BRD5529 is an effective dose-dependent CARD9-TRIM62 protein–protein interaction (PPI) inhibitor with an IC50 value of 8.6 μM. BRD5529 has potency and complete inhibition of CARD9 ubiquitinylation in vitro, also has favorable solubility. BRD5529 can be used for the research of inflammatory bowel disease (IBD) such as Crohn’s disease (CD) and ulcerative colitis (UC) .
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- HY-142705
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Epigenetic Reader Domain
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Cancer
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BRD4 D1-IN-2 (compound 26) is a potent and selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-2 has 15 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC .
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- HY-142674
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Epigenetic Reader Domain
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Cancer
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BRD4-BD1/2-IN-1 is a potent BRD4 inhibitor with IC50s of <100 nM for BRD4 BD-1 and BRD4 BD-2, respectively (US20150148375A1, compound 5) .
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- HY-124607B
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BRD3731
1 Publications Verification
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GSK-3
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Neurological Disease
Metabolic Disease
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BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. BRD3731 is potentail for the research of post-traumatic stress disorder (PTSD), psychiatric disorder, diabetes, and neurodegenerative disorders .
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- HY-160636
-
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Epigenetic Reader Domain
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Others
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BRD4 Inhibitor-32 (example 15) is a BRD4 inhibitor that can be used in acute kidney disease and chronic kidney disease research .
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- HY-160660
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Epigenetic Reader Domain
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Others
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BRD4 Inhibitor-33 (example 13) is a BRD4 inhibitor that can be used in acute kidney disease and chronic kidney disease research .
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- HY-142675
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Epigenetic Reader Domain
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Cancer
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BRD4-BD1/2-IN-2 is a potent BRD4 BD2 inhibitor with IC50s of <0.5 nM and <300 nM for BRD4 BD2 and BRD4 BD1, respectively (WO2021233371A1, compound 2) .
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- HY-100590
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BRD6125
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FPH1(BRD-6125) increases the number and activity of primary human hepatocytes in vitro and promotes the differentiation of iPS cells towards a hepatic lineage .
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- HY-147202
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Epigenetic Reader Domain
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Cancer
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BRD4 Inhibitor-24 (compound 3U) is a potent BRD4 inhibitor, BRD4 Inhibitor-24 shows antitumor activity against MCF7 and K652 cells, with IC50 values of 33.7 and 45.9 μM, respectively (extracted from patent CN107721975A) .
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- HY-12185
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BRD7389
1 Publications Verification
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Ribosomal S6 Kinase (RSK)
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Metabolic Disease
Cancer
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BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells .
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- HY-16705
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BRD4770
2 Publications Verification
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Histone Methyltransferase
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Cancer
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BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 µM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence .
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- HY-124053
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HDAC
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Cancer
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BRD2492 (compound 6d) is a potent, selective HDAC1 and HDAC2 inhibitor with IC50s of 13.2 nM and 77.2 nM, respecrtively. BRD2492 exhibits >100-fold selectivity for HDAC1/2 over selectivity over HDAC3 and HDAC6. BRD2492 inhibits breast cancer cell lines growth with IC50s of 1.01 μM and 11.13 μM for T-47D and MCF-7 cells, respectively .
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- HY-120711
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ML187
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Apoptosis
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Metabolic Disease
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BRD0476 is an inhibitor of pancreatic β-cell apoptosis with an EC50 value of 0.78 μM and a maximal inhibitory activity of 99%. BRD0476 can be used in diabetes-related research .
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- HY-18700
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HDAC
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Cancer
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BRD73954 is a potent HDAC inhibitor and selectively inhibiting both HDAC6 and HDAC8 with IC50 values of 0.0036, 0.12, 9, 12, 23 µM for HDAC6, HDAC8, HDAC2, HDAC1 and HDAC3, respectively. BRD73954 decreases the levels of HDAC6, associated with upregulation of Ac-Tubulin .
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- HY-19694
-
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Others
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Endocrinology
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BRD7552, a potent PDX1 transcription factor inducer, upregulates PDX1 expression in both primary human islets and ductal cells, and induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. BRD7552 increases insulin expression. PDX1 is a key transcription factor involved in pancreas development and β cell function .
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- HY-18714
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Bacterial
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Others
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BRD7116 competitively binds to bacterial DNA gyrase, exhibits an EC50 of 200 nM for LSCe cells, with cell-non-autonomous anti-leukemia activity.
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- HY-102083
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HDAC
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Neurological Disease
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BRD4884 is a potent HDAC inhibitor with IC50 values of 29 nM, 62 nM, and 1.09 µM for HDAC1, 2, and 3, respectively .
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- HY-114268
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HIV
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Infection
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BRD-K98645985 is a BAF (mammalian SWI/SNF) transcriptional repression inhibitor with an EC50 of ~2.37 µM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1 latency, without T cell activation or toxicity .
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- HY-125191
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Bcl-2 Family
Beclin1
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Cancer
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BRD1991 selectively disrupts Beclin 1/Bcl-2 binding and induces autophagy without triggering apoptosis or other forms of cell death .
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- HY-136350
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Phosphodiesterase (PDE)
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Cancer
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BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity .
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- HY-120924
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-
- HY-RS01596
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Small Interfering RNA (siRNA)
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Others
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BRD1 Human Pre-designed siRNA Set A contains three designed siRNAs for BRD1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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BRD1 Human Pre-designed siRNA Set A
BRD1 Human Pre-designed siRNA Set A
- HY-RS01597
-
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Small Interfering RNA (siRNA)
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Others
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BRD2 Human Pre-designed siRNA Set A contains three designed siRNAs for BRD2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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-
BRD2 Human Pre-designed siRNA Set A
BRD2 Human Pre-designed siRNA Set A
- HY-RS01598
-
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Small Interfering RNA (siRNA)
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Others
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Brd2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Brd2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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-
Brd2 Mouse Pre-designed siRNA Set A
Brd2 Mouse Pre-designed siRNA Set A
- HY-RS01599
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Small Interfering RNA (siRNA)
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Others
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BRD2 Rat Pre-designed siRNA Set A contains three designed siRNAs for BRD2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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-
BRD2 Rat Pre-designed siRNA Set A
BRD2 Rat Pre-designed siRNA Set A
- HY-RS01600
-
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Small Interfering RNA (siRNA)
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Others
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BRD3 Human Pre-designed siRNA Set A contains three designed siRNAs for BRD3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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-
BRD3 Human Pre-designed siRNA Set A
BRD3 Human Pre-designed siRNA Set A
- HY-RS01601
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Small Interfering RNA (siRNA)
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Others
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Brd3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Brd3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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-
Brd3 Mouse Pre-designed siRNA Set A
Brd3 Mouse Pre-designed siRNA Set A
- HY-RS01602
-
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Small Interfering RNA (siRNA)
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Others
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Brd3 Rat Pre-designed siRNA Set A contains three designed siRNAs for Brd3 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Brd3 Rat Pre-designed siRNA Set A
Brd3 Rat Pre-designed siRNA Set A
- HY-RS01603
-
|
Small Interfering RNA (siRNA)
|
Others
|
BRD4 Human Pre-designed siRNA Set A contains three designed siRNAs for BRD4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
BRD4 Human Pre-designed siRNA Set A
BRD4 Human Pre-designed siRNA Set A
- HY-RS01604
-
|
Small Interfering RNA (siRNA)
|
Others
|
Brd4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Brd4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Brd4 Mouse Pre-designed siRNA Set A
Brd4 Mouse Pre-designed siRNA Set A
- HY-RS01605
-
|
Small Interfering RNA (siRNA)
|
Others
|
Brd4 Rat Pre-designed siRNA Set A contains three designed siRNAs for Brd4 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Brd4 Rat Pre-designed siRNA Set A
Brd4 Rat Pre-designed siRNA Set A
- HY-RS01606
-
|
Small Interfering RNA (siRNA)
|
Others
|
BRD7 Human Pre-designed siRNA Set A contains three designed siRNAs for BRD7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
BRD7 Human Pre-designed siRNA Set A
BRD7 Human Pre-designed siRNA Set A
- HY-RS01607
-
|
Small Interfering RNA (siRNA)
|
Others
|
Brd7 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Brd7 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Brd7 Mouse Pre-designed siRNA Set A
Brd7 Mouse Pre-designed siRNA Set A
- HY-RS01608
-
|
Small Interfering RNA (siRNA)
|
Others
|
Brd7 Rat Pre-designed siRNA Set A contains three designed siRNAs for Brd7 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Brd7 Rat Pre-designed siRNA Set A
Brd7 Rat Pre-designed siRNA Set A
- HY-RS01609
-
|
Small Interfering RNA (siRNA)
|
Others
|
BRD8 Human Pre-designed siRNA Set A contains three designed siRNAs for BRD8 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
BRD8 Human Pre-designed siRNA Set A
BRD8 Human Pre-designed siRNA Set A
- HY-RS01610
-
|
Small Interfering RNA (siRNA)
|
Others
|
BRD9 Human Pre-designed siRNA Set A contains three designed siRNAs for BRD9 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
BRD9 Human Pre-designed siRNA Set A
BRD9 Human Pre-designed siRNA Set A
- HY-RS01611
-
|
Small Interfering RNA (siRNA)
|
Others
|
Brd9 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Brd9 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Brd9 Mouse Pre-designed siRNA Set A
Brd9 Mouse Pre-designed siRNA Set A
- HY-RS01612
-
|
Small Interfering RNA (siRNA)
|
Others
|
Brd9 Rat Pre-designed siRNA Set A contains three designed siRNAs for Brd9 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Brd9 Rat Pre-designed siRNA Set A
Brd9 Rat Pre-designed siRNA Set A
- HY-101374A
-
-
- HY-132943
-
-
- HY-132943A
-
-
- HY-12281
-
BRD-9424
|
Others
|
Metabolic Disease
Cancer
|
FPH2 induces of functional proliferation of primary human hepatocytes and may lead to the development of new therapeutics for liver diseases.
|
-
- HY-145939
-
BRD5846
|
Others
|
Cancer
|
BAY-888 exhibits IC50 value of 1.5 nM and 5.5 nM towards CSNK1A1 and CSNK1D, respectively.
|
-
- HY-145940
-
BRD3727
|
Others
|
Cancer
|
BAY-204 is an inhibitor of Casein kinase 1 alpha and delta (CSNK1α and δ) useful for the research of proliferative disorders.
|
-
- HY-12346
-
NSC 12407; BRD-K4477
|
Others
|
Others
|
FH1 (NSC 12407) enhances hepatocyte functions, and promotes the differentiation of induced pluripotent stem (iPS)-derived hepatocytes toward a phenotype more mature and the maturation of well-differentiated cultures of hepatocyte-like cells (iHeps) .
|
-
- HY-130612
-
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
|
-
- HY-149948
-
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
PROTAC BRD3/BRD4-L degrader-2 is a PROTAC molecule and can selectively degrade cellular BRD3 and BRD4-L with Ki values of 16.91 and 2.8 nM, respectively. PROTAC BRD3/BRD4-L degrader-2 also has robust antitumor activity in mouse xenograft models. PROTAC BRD3/BRD4-L degrader-2 can be used for the research of cancer .
|
-
- HY-117865
-
|
Epigenetic Reader Domain
|
Cancer
|
GNE-886 (Compound 21) is a potent and selective inhibitor of Cat eye syndrome chromosome region candidate 2 bromodomain (CECR2) (BRD) with an IC50 value of 0.016 µM and an EC50 value of 370 nM. GNE-886 also inhibits BRD9 with an IC50 value of 1.6 µM .
|
-
- HY-18975
-
I-BRD9
4 Publications Verification
|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
I-BRD9 is a selective cellular chemical probe of bromodomain-containing protein 9 (BRD9) with pIC50 value of 7.3 μM. I-BRD9 has high selectivity for bromodomain and extra terminal domain (BET) family and highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 can be used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways .
|
-
- HY-116830A
-
|
GSK-3
|
Cancer
|
(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) .
|
-
- HY-133131
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression .
|
-
- HY-144338
-
|
Epigenetic Reader Domain
PARP
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
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 .
|
-
- HY-111875
-
|
SNIPERs
Epigenetic Reader Domain
|
Cancer
|
SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a BET inhibitor, (+)-JQ-1, connected by a linker. SNIPER(BRD)-1 induces the degradation of BRD4 via the ubiquitin-proteasome pathway. SNIPER(BRD)-1 also degrades cIAP1 , cIAP2 and XIAP with IC50s of 6.8 nM, 17 nM, and 49nM, respectively .
|
-
- HY-136857
-
|
PROTACs
Epigenetic Reader Domain
Ligands for Target Protein for PROTAC
|
Cancer
|
PROTAC BRD4 Degrader-7 is a potent bromodomain BRD4 degrader extracted from patent WO2020055976A1, example 1a, has IC50s of 15.5 and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively . PROTAC BRD4 Degrader-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-131203
-
|
Epigenetic Reader Domain
Apoptosis
c-Myc
Caspase
|
Cancer
|
PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4 degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research .
|
-
- HY-133136
-
-
- HY-136350B
-
|
Others
|
Cancer
|
(S)-BRD9500 is the isomer of BRD9500 (HY-136350), and can be used as an experimental control. BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity .
|
-
- HY-143327
-
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
PROTAC BRD4 Degrader-16 is a potent PROTAC BRD4 Degrader, with IC50 values of 34.58 nM (BRD4 (BD1)) and 40.23 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-16 ignificantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-16 significantly induces apoptosis in MV-4-11 cells .
|
-
- HY-133737
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD4 Degrader-5 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-5 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines .
|
-
- HY-138555
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells .
|
-
- HY-138637
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD4 Degrader-14 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.8 nM and 1.7 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-14 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells .
|
-
- HY-139294
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD4 Degrader-15 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells .
|
-
- HY-145947
-
|
PROTACs
|
Cancer
|
PROTAC BRD9 Degrader-5 is a PROTAC for targeted degradation of BRD9.
|
-
- HY-143328
-
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells .
|
-
- HY-150613
-
|
Epigenetic Reader Domain
PARP
Apoptosis
|
Cancer
|
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
|
-
- HY-158031
-
|
Apoptosis
Polo-like Kinase (PLK)
Epigenetic Reader Domain
|
Cancer
|
PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3 nM and 60.8 nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research .
|
-
- HY-145403
-
|
PROTACs
|
Cancer
|
PROTAC BRD9 Degrader-4 is a BRD9 bifunctional degrader for researching cancer.
|
-
- HY-145395
-
|
PROTACs
|
Cancer
|
PROTAC BRD9 Degrader-2 is a BRD9 bifunctional degrader for researching cancer.
|
-
- HY-145400
-
|
PROTACs
|
Cancer
|
PROTAC BRD9 Degrader-3 is a BRD9 bifunctional degrader for researching cancer.
|
-
- HY-153459
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD4 Degrader-19 (compound 176) is a PROTAC that targets BRD4 protein for degradation. PROTAC BRD4 Degrader-19 can be used in cancer research .
|
-
- HY-143471
-
|
Polo-like Kinase (PLK)
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
PLK1/BRD4-IN-1 (9b) is an orally active dual PLK1 and BRD4 inhibitor with IC50 values of 22 nM and 109 nM against PLK1 and BRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest and apoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity .
|
-
- HY-153820
-
-
- HY-107445
-
-
- HY-107445A
-
-
- HY-160527
-
|
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD4 Degrader-25 (Compound 1-f) is a BRD4 degrader. PROTAC BRD4 Degrader-25 can be used for the research of cancer and other bromodomain related diseases .
|
-
- HY-132942
-
-
- HY-132942A
-
-
- HY-107442
-
|
Epigenetic Reader Domain
Ligands for Target Protein for PROTAC
|
Cancer
|
PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136) . PROTAC BRD4-binding moiety 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-155361
-
|
PROTACs
|
Cancer
|
PROTAC BRD9 Degrader-7 is an orally active and selective degrader of BRD9 with a DC50 of 1.02 nM. PROTAC BRD9 Degrader-7 has superior oral activity with a Cmax of 3436.95 ng/mL .
|
-
- HY-138633
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD4 Degrader-10 (compound 8b) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-10 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 1.3 nM and 18 nM, respectively .
|
-
- HY-138636
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD4 Degrader-13 (compound 9d) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-13 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.025 nM and 6.0 nM, respectively .
|
-
- HY-138632
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD4 Degrader-9 (compound 8a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-9 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.86 nM and 7.6 nM, respectively .
|
-
- HY-138634
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD4 Degrader-11 (compound 9a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-11 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.23 nM and 0.38 nM, respectively .
|
-
- HY-138635
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-12 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.39 nM and 0.24 nM, respectively .
|
-
- HY-156566
-
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research .
|
-
- HY-143270
-
-
- HY-135558
-
-
- HY-129939
-
-
- HY-153632
-
-
- HY-155393
-
-
- HY-156273
-
|
Apoptosis
HDAC
Epigenetic Reader Domain
JAK
|
Cancer
|
HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo .
|
-
- HY-103632
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD9 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD9 (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology .
|
-
- HY-161093
-
|
PROTACs
|
Cancer
|
PROTAC BRD4 Degrader-23 (compound 17) is an
effective visible-light-controlled degrader. PROTAC BRD4 Degrader-23 can
inhibit tumor cell proliferation under 405 nm light irradiation .
|
-
- HY-124607
-
|
GSK-3
|
Neurological Disease
|
(R)-BRD3731 is a GSK3 inhibitor extracted from patent US20160375006A1, compound example 273, has IC50s of 1.05 and 6.7 μM for GSK3β and GSK3α, respectively .
|
-
- HY-129938
-
|
PROTAC-Linker Conjugates for PAC
|
Cancer
|
PROTAC BRD4 Degrader-24 (compound 5), a PROTAC-linker Conjugate for PAC, comprises the chimeric BET degrader GNE-987 and disulfide-containing linker .
|
-
- HY-15826
-
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Inflammation/Immunology
Cancer
|
SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects .
|
-
- HY-133736
-
|
PROTAC-Linker Conjugates for PAC
ADC Cytotoxin
|
Cancer
|
PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader GNE-987 and PEG-based linker . PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-44103
-
PROTAC BRD4-binding moiety 4
|
Ligands for Target Protein for PROTAC
|
Cancer
|
Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM . Desmethyl-QCA276 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-110374
-
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism .
|
-
- HY-107443
-
Molibresib carboxylic acid; GSK525762A carboxylic acid; PROTAC BRD4-binding moiety 2
|
Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
|
Cancer
|
I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1 .
|
-
- HY-100972
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively .
|
-
- HY-130813
-
-
- HY-120000
-
MS402
1 Publications Verification
|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice .
|
-
- HY-19553
-
|
|
|
LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells .
|
-
- HY-130814
-
|
E3 Ligase Ligand-Linker Conjugates
Autophagy
Apoptosis
|
Cancer
|
Thalidomide-NH-C4-NH2 TFA (compound 29c) is an E3 ligase ligand-linker conjugate, and incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-NH-C4-NH2 TFA is used in PROTAC BRD2/BRD4 degrader-1 (HY-130612). PROTAC BRD2/BRD4 degrader-1 is a potent and selective BET protein BRD4 and BRD2 degrader .
|
-
- HY-130842
-
β-NF-CH2-Br
|
Ligands for E3 Ligase
|
Cancer
|
β-Naphthoflavone-CH2-Br (β-NF-CH2-Br) is an arylhydrocarbon receptor (AhR) ligand. β-Naphthoflavone-CH2-Br can be used to synthesize the PROTAC β-NF-JQ1(HY-130256) .
|
-
- HY-121738
-
-
- HY-131061
-
|
Epigenetic Reader Domain
|
Cancer
|
BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity .
|
-
- HY-125232
-
|
Epigenetic Reader Domain
|
Cancer
|
MS645 is a bivalent BET bromodomains (BrD) inhibitor with a Ki of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells .
|
-
- HY-111139
-
-
- HY-111977
-
|
Epigenetic Reader Domain
|
Cancer
|
ZEN-3219 is a BET inhibitor with IC50s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4 .
|
-
- HY-111979
-
|
Epigenetic Reader Domain
|
Cancer
|
ZEN-3411 is a BET inhibitor with IC50s of 0.05, 0.05 and 0.06 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTACs to induce degradation of BRD4 .
|
-
- HY-100517
-
|
|
|
TP-472 is a selective BRD9/7 inhibitor, with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7 . TP-472 induces apoptosis of melanoma cells .
|
-
- HY-107425
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. Kds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively .
|
-
- HY-129201
-
|
Epigenetic Reader Domain
|
Cancer
|
ZEN-2759 is a potent BET (Bromodomain and Extra-Terminal Domain) inhibitor, with IC50 values of 0.23, 0.08 and 0.28 μM for BRD4(BD1), BRD4(BD2), and BRD4(BD1BD2), respectively .
|
-
- HY-103297
-
-
- HY-112376
-
-
- HY-112377
-
-
- HY-116227
-
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
(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 .
|
-
- HY-111978
-
|
Epigenetic Reader Domain
|
Cancer
|
ZEN-3862 is a BET inhibitor with IC50s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively. ZEN-3862 can be used to form PROTACs to induce degradation of BRD4 .
|
-
- HY-110215
-
|
Epigenetic Reader Domain
|
Cancer
|
XD14 is a potent BET inhibitor with antitumor effect. It binds to BRD2, BRD3, and BRD4 with Kds of 170, 380, and 160 nM, respectively .
|
-
- HY-103633
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
|
-
- HY-153414
-
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
GXF-111, a PROTAC molecule, can promote selective degradation of cellular BRD3 and BRD4-L. GXF-111 has binding affinities for BRD3 BD1 and BRD3 BD2 with Ki values of 11.97 nM and 2.35 nM, respectively. GXF-111 can be used for the research of cancer .
|
-
- HY-112429
-
HJB97
2 Publications Verification
|
Epigenetic Reader Domain
|
Cancer
|
HJB97 is a high-affinity BET inhibitor with Kis of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively. HJB97 is employed for the design of potential PROTAC BET degrader and has antitumor activity .
|
-
- HY-147375
-
|
Epigenetic Reader Domain
|
Cancer
|
Bromodomain inhibitor-10 (compound 128) is a potent bromodomain inhibitor with Kds of 15.0, 2500 nM for BRD4-1 and BRD4-2, respectively. Bromodomain inhibitor-10 inhibits the production of IL12p40 .
|
-
- HY-148116
-
|
Epigenetic Reader Domain
|
Cancer
|
DN02 is a potent, selective BRD8 bromodomain probe. DN02 has exhibits high affinity for the BRD8(1) (Ki=32 nM), which is 30-fold more affinity than BRD8 (2) (Ki>1000 nM) .
|
-
- HY-153385
-
-
- HY-156828
-
|
Others
|
Others
|
MMH2 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2) .
|
-
- HY-156827
-
|
Others
|
Others
|
MMH1 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2) .
|
-
- HY-100352
-
BI-9564
1 Publications Verification
|
Epigenetic Reader Domain
|
Cancer
|
BI-9564 is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC50s of 75 nM and 3.4 μM and Kds of 14 nM and 239 nM, respectively. BI-9564 has an IC50 of > 100 μM for BET family .
|
-
- HY-123621
-
|
Epigenetic Reader Domain
|
Cancer
|
GNE-375 is a potent and highly selective BRD9 inhibitor with an IC50 of 5 nM. GNE-375 shows >100-fold selective for BRD9 over BRD4, TAF1, and CECR2. GNE-375 decreases BRD9 binding to chromatin .
|
-
- HY-13959
-
MS436
1 Publications Verification
|
Epigenetic Reader Domain
|
Cancer
|
MS436 is a new class of bromodomain inhibitor, exhibits potent affinity of an estimated Ki=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2.
|
-
- HY-112149
-
-
- HY-153945
-
|
Epigenetic Reader Domain
|
Cancer
|
BET-IN-15 (compound 1) is a potent and orally active BET inhibitor with IC50 values of 0.64, 0.25 nM for BRD4-BD1, BRD4-BD2, respectively. BET-IN-15 shows antiproliferative activity .
|
-
- HY-149098
-
|
Epigenetic Reader Domain
|
Cancer
|
SJ1461 is a potent and orally active BET inhibitor. SJ1461 inhibits BRD2 (BD1), and BRD2 (BD2), BRD4 (BD1), and BRD4 (BD2) with IC50 values of 1.6 nM, 0.1 nM, 6.5 nM, and 0.2 nM, respectively .
|
-
- HY-149806
-
|
Epigenetic Reader Domain
|
Cancer
|
BD-IN-1 is a pan bromodomain (BD) inhibitor with KD values of 250, 420, 130, 430, 67, 240, 970 nM for BRD4(1), CBP, BRPF1B, BRD7, BRD9, BRDT(1), CECR2 respectively. BD-IN-1 shows antiproliferative activity .
|
-
- HY-114504
-
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models .
|
-
- HY-150684
-
|
Epigenetic Reader Domain
|
Cancer
|
GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc .
|
-
- HY-102044
-
-
- HY-13235
-
GSK1210151A
|
Epigenetic Reader Domain
|
Cancer
|
I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively .
|
-
- HY-13960
-
I-BET726
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).
|
-
- HY-110106
-
GSK1210151A dihydrochloride
|
Epigenetic Reader Domain
|
Cancer
|
I-BET151 dihydrochloride (GSK1210151A dihydrochloride) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively .
|
-
- HY-101460
-
|
PROTACs
Molecular Glues
Epigenetic Reader Domain
|
Cancer
|
Tz-Thalidomide is a tetrazine tagged Thalidomide (HY-14658) (Ligands for E3 Ligase). Tz-Thalidomide has binding affinity for BRD4, with IC50s of 46.25 μM (BRD4-1) and 62.55 μM (BRD4-2). Tz-Thalidomide is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups .
|
-
- HY-114305
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
A1874 is a nutlin-based (MDM2 ligand) and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation .
|
-
- HY-145264
-
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively .
|
-
- HY-111976
-
-
- HY-139620
-
|
PROTACs
|
Cancer
|
MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.
|
-
- HY-150683
-
|
Epigenetic Reader Domain
|
Cancer
|
NC-III-49-1 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. NC-III-49-1 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 0.095, 0.32, 0.29, 0.089, 5.5, 0.058 nM, respectively. NC-III-49-1 shows antiproliferative activity. NC-III-49-1 decreases the expression of c-Myc .
|
-
- HY-157290
-
|
Epigenetic Reader Domain
Src
|
Cancer
|
HL403 is a potent and dual BRD4/Src inhibitor. HL403 has IC50 values of 133 nM for BRD4 inhibition and 4.5 nM for Src inhibition. HL403 shows anti-cancer activity .
|
-
- HY-132941
-
|
PROTACs
|
Cancer
|
CFT-2718 is a new BRD4-targeting degrader (PROTAC) with enhanced catalytic activity and in vivo properties.
|
-
- HY-19549
-
|
|
|
RX-37 is a selective BET inhibitor. RX-37 binds to BET bromodomain proteins (BRD2, BRD3, and BRD4) with Ki values of 3.2-24.7 nM. RX-37 can be used for research of cancers .
|
-
- HY-150516S
-
-
- HY-107425B
-
|
Epigenetic Reader Domain
|
Cancer
|
cis-MZ 1 hydrate is a negative control for BRD4-targeted PROTAC MZ 1 (HY-107425). cis-MZ 1 or MZ 1 is a combination of the von Hippel-Lindau ligand (red part in the structural formula) and the BRD4 ligand (blue part in the structural formula). The Kd of MZ 1 for BRD4 BD1/2 was 382 nM and 120 nM, respectively .
|
-
- HY-100670
-
-
- HY-126325
-
|
Epigenetic Reader Domain
|
Cancer
|
BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. Anti-cancer activity .
|
-
- HY-15743
-
OTX-015; MK-8628
|
Epigenetic Reader Domain
|
Cancer
|
Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.
|
-
- HY-111502
-
|
Epigenetic Reader Domain
|
Cancer
|
Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM . Antitumor activity .
|
-
- HY-112375
-
|
PROTACs
|
Cancer
|
AT6 is a PROTAC AT1 analogue, which is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 with highly selectivity to bromodomain (Brd4).
|
-
- HY-138563
-
|
Epigenetic Reader Domain
|
Cancer
|
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5) .
|
-
- HY-153519
-
|
Epigenetic Reader Domain
|
Cancer
|
WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 .
|
-
- HY-136570A
-
-
- HY-110378
-
-
- HY-112610
-
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo .
|
-
- HY-111503
-
|
Epigenetic Reader Domain
|
Cancer
|
Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM .
|
-
- HY-N3213
-
|
Epigenetic Reader Domain
|
Cancer
|
Naringenin triacetate is a flavonoid isolated from plant, exhibits a good binding affinity with multiple crystal structures of first bromodomain BRD4 (BRD4 BD1) .
|
-
- HY-136192
-
-
- HY-123911
-
-
- HY-132991
-
|
PROTAC Linkers
|
Cancer
|
ML 2-14 is a PROTAC for degrading BRD4, with C4 alkyl linker. ML 2-14 exerts degradation of BRD4 in 231MFP breast cancer cells .
|
-
- HY-123844
-
dBET57
2 Publications Verification
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4 Cereblon E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2 .
|
-
- HY-16954
-
-
- HY-100351
-
|
Epigenetic Reader Domain
|
Cancer
|
BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.
|
-
- HY-100696
-
|
|
|
PNZ5 is a potent and isoxazole-based pan-BET inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a KD of 5.43 nM for BRD4(1) .
|
-
- HY-114406
-
|
Ligands for E3 Ligase
|
Cancer
|
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation .
|
-
- HY-144236
-
|
Epigenetic Reader Domain
|
Others
|
Considerable studies confirmed that BRD4 inhibition ameliorated kidney injury and fibrosis ,and ZLD2218 exhibited the most potent inhibitory activity against BRD4, with the IC50 value of 107 nM
|
-
- HY-136794
-
|
p38 MAPK
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
SB-284851-BT is an inhibitor of BRD4/p38α/BRDT. SB-284851-BT inhibits BRD4-BD1 (IC50=1.7 µM), p38α (Kd=0.47 nM), BRDT (1) (IC50=18 µM) and BRD4 (1)(IC50=3.7 µM). SB-284851-BT reduces IL-8 production by inhibiting p38α, as well as inhibiting BRD4 to down-regulates c-Myc and NF-κB gene pathways in cancer. SB-284851-BT can combined with the bromine domain and extra terminal (BET) .
|
-
- HY-19760
-
|
|
|
I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD) .
|
-
- HY-111422
-
|
Epigenetic Reader Domain
|
Cancer
|
PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
|
-
- HY-136571
-
GSK046
2 Publications Verification
iBET-BD2
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity .
|
-
- HY-112090
-
|
Epigenetic Reader Domain
HIV
|
Infection
Inflammation/Immunology
Cancer
|
ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability .
|
-
- HY-112149A
-
|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
(E/Z)-ZL0420 is a racemic compound of (Z)-ZL0420 and (E)-ZL0420 isomers. (E)-ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 .
|
-
- HY-151593
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1 .
|
-
- HY-19760B
-
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
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) .
|
-
- HY-143317
-
|
Epigenetic Reader Domain
|
Cancer
|
XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .
|
-
- HY-139620A
-
|
PROTACs
|
Others
|
MS83 epimer 1 is the epimer of MS83 (HY-139620). MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder .
|
-
- HY-136570
-
iBET-BD1
|
Epigenetic Reader Domain
Apoptosis
|
Inflammation/Immunology
Cancer
|
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 .
|
-
- HY-134463
-
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .
|
-
- HY-112718
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BET Degrader-10 is a potent BET protein BRD4 degrader extracted from patent WO2017007612A1, example 37, connected by ligands for Cereblon and BRD4, with a DC50 of 49 nM .
|
-
- HY-145310
-
-
- HY-117997
-
|
Epigenetic Reader Domain
|
Cancer
|
UMB-32, a potent, selective BRD4 inhibitor, binds BRD4 with the Kd of 550 nM, and IC50 of 637 nM. UMB-32 also shows potency against TAF1, a bromodomain-containing transcription factor .
|
-
- HY-153948
-
|
Epigenetic Reader Domain
|
Cancer
|
CBP-IN-1 (compound 12) is a potent CBP inhibitor, with an IC50 of 1.5 nM. CBP-IN-1 also inhibits CBP BRET and BRD4(1), with IC50 values of 690 and 3100 nM, respectively .
|
-
- HY-156744
-
-
- HY-129917
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1 .
|
-
- HY-15743A
-
(R)-OTX-015; (R)-MK-8628
|
Others
|
Cancer
|
(R)-Birabresib is the isomer of Birabresib (HY-15743), and can be used as an experimental control. Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.
|
-
- HY-12863
-
CPI-0610
|
Epigenetic Reader Domain
|
Cancer
|
Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active BET inhibitor. Pelabresib inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC .
|
-
- HY-108435
-
-
- HY-114416
-
|
Epigenetic Reader Domain
|
Cancer
|
GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively .
|
-
- HY-13030
-
-
- HY-146741
-
|
Epigenetic Reader Domain
|
Cancer
|
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 .
|
-
- HY-147374
-
|
Epigenetic Reader Domain
|
Metabolic Disease
Inflammation/Immunology
|
Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases .
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- HY-157561
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- HY-124859
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- HY-100653A
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Epigenetic Reader Domain
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Cancer
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AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.
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- HY-160528
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Epigenetic Reader Domain
Molecular Glues
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Cancer
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IBG3 is a dual-JQ1-containing BET degrader that targets protein degradation via intramolecular bivalent glues. IBG3 is a BRD2 and BRD4 bifunctional degrader with DC50 values of 8.6 pM and 6.7 pM, respectively .
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- HY-120196
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- HY-161167
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PROTACs
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Cancer
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MM-02-08 is the potent BRD4 degrader and binds to DDB1 .
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- HY-145925C
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Epigenetic Reader Domain
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Cancer
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(S,R)-CFT8634 is a selective and orally active BRD9 protein degrader. (S,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 176) .
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- HY-162352
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Epigenetic Reader Domain
Apoptosis
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Cancer
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SDU-071 is a potent and orally active inhibitor of BRD4-p53 inhibitor. SDU-071 inhibits MDA-MB-231 cells proliferation with an IC50 of 10.5 μM. SDU-071 induces cell cycle arrest and apoptosis .
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- HY-14443
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ERK
Epigenetic Reader Domain
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Cancer
|
XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity .
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- HY-124596
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NKR-P1A
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Epigenetic Reader Domain
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Cancer
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CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity .
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- HY-114322
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PROTACs
Epigenetic Reader Domain
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Cancer
|
VZ185 is a potent, fast, and selective von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively .
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- HY-151594
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-
- HY-153894
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CDK
Epigenetic Reader Domain
PI3K
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Cancer
|
SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ), <2.5 nM (CDK4), 3.3 nM (CDK6), respectively. SRX3177 exerts broad cytotoxic activity against cancer cells, but acts friendly with normal epithelial cells .
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- HY-112398
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- HY-112609
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- HY-161125
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Others
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Others
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(+)-JQ1-OH is the major metabolite of (+)-JQ1(HY-13030). (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy .
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- HY-156743
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Others
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Others
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DCAF1 binder 2, a ligands for E3 Ligase, involves in BRD9, kinase and selective BTK degration.
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- HY-117690A
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- HY-151594A
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Epigenetic Reader Domain
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Inflammation/Immunology
Cancer
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iBRD4-BD1 diTFA is selective BRD4 bromodomain inhibitor. iBRD4-BD1 diTFA has inhibition activity for BRD4 bromodomain with an IC50 value of 12 nM. iBRD4-BD1 diTFA can be used for the research of inflammation and oncology .
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- HY-112316B
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- HY-149328
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PROTACs
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Cancer
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phoBET1 is a photocaged-PROTAC. phoBET1 can achieve BRD4 degradation and effectively suppress tumor growth .
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- HY-108696
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GNE-781
2 Publications Verification
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Epigenetic Reader Domain
Histone Acetyltransferase
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Cancer
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GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model .
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- HY-101121
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NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins .
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- HY-111916
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-
- HY-150211
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- HY-130256
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PROTACs
Epigenetic Reader Domain
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Cancer
|
β-NF-JQ1 is a PROTAC that recruits Aryl Hydrocarbon Receptor E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity .
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- HY-130622
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Epigenetic Reader Domain
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Inflammation/Immunology
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LT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC50=12.130 μM). LT052 has anti-inflammatory activity and can be used for acute gout arthritis research .
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- HY-145226
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PROTACs
Epigenetic Reader Domain
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Cancer
|
XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4BD1L94V degrader. XY-06-007 shows a DC50, 6 h of 10 nM against BRD4BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies .
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- HY-129937A
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PROTACs
Epigenetic Reader Domain
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Cancer
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GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC) .
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- HY-16586
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-
- HY-112150
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- HY-107425A
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- HY-114407
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PROTACs
Epigenetic Reader Domain
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Cancer
|
TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM . TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation .
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- HY-129937
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PROTACs
Epigenetic Reader Domain
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Cancer
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(S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to von Hippel-Lindau and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC) .
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- HY-100697
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- HY-100015
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ABBV-075
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Epigenetic Reader Domain
Apoptosis
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Cancer
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Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM .
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- HY-114902
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Epigenetic Reader Domain
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Cancer
|
Y02224 is a potent BRD4 inhibitor and exhibits reasonable antiproliferative effect on leukemia cells.Y02224 has the potential for? CRPC research .
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- HY-157426
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- HY-160260
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Epigenetic Reader Domain
Histone Acetyltransferase
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Cancer
|
EP300/CBP-IN-1 (compound 172) is a potent EP300/CBP inhibitor with IC50s of 2.3 nM and 2.1 nM for CBP BRD and EP300 BRD, respectively. EP300/CBP-IN-1 has the inhibitory effect on the proliferation of prostate cancer CWR22RV1 cells .
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- HY-15846
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- HY-163019
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- HY-114204
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Epigenetic Reader Domain
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Cancer
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GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1 .
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- HY-115568
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PROTACs
Epigenetic Reader Domain
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Cancer
|
BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity .
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- HY-162240
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- HY-12518
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OF-1
3 Publications Verification
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Epigenetic Reader Domain
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Cancer
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OF-1 is a potent pan-BRPF bromodomain (BRD) inhibitor, with IC50 values of 270 nM, 1.2 μM for TRIM24 and BRPF1B, respectively .
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- HY-111445
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- HY-119053
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MDM-2/p53
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Cancer
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MS7972 is a small molecule that blocks human p53 and CREB binding protein association. MS7972 can almost completely block this BRD interaction at 50 μM .
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- HY-13030A
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Epigenetic Reader Domain
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Cancer
|
(R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (R)-(-)-JQ1 Enantiomer has no effect.
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- HY-117690
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PROTACs
Epigenetic Reader Domain
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Cancer
|
dBRD9,a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family .
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- HY-101125A
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L-45 dihydrochloride
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Epigenetic Reader Domain
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Cancer
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L-Moses (L-45) dihydrochloride is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM .
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- HY-101125
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L-Moses
2 Publications Verification
L-45
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L-Moses (L-45) is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126 nM .
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- HY-148739
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PROTACs
Epigenetic Reader Domain
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Cancer
|
dBRD 9-A is a PROTAC which can selective degrade BRD9. dBRD 9-A improves the bromine domain binding profile and reduces the binding activity of the whole BET family .
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- HY-50698
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- HY-101838
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PROTACs
Epigenetic Reader Domain
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Cancer
|
dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker .
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- HY-138553A
-
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Others
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Cancer
|
(S,R,S)-AHPC-isobutyl acetate-methanesulfonothioate-Me-C10-NH2 TFA is a part of
PROTAC BRD4 Degrader-12 (HY-138635) .
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- HY-153241
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Epigenetic Reader Domain
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Cancer
|
GSK737 is a BRD4 BD1 and BD2 inhibitor, with pIC50 values of 5.3 and 7.3 respectively. GSK737 has low clearance and good solubility and permeability in rat .
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- HY-155370
-
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PROTACs
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Cancer
|
IR808-TZ?is a potent BRD4 BT-PROTAC?degrader.?IR808-TZ?has the potential for?application in the design of BT-PROTAC targeting other proteins .
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- HY-19537
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NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF) famlily of proteins, with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively.
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- HY-135236
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Epigenetic Reader Domain
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Cancer
|
OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity .
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- HY-141844
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HDAC
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Cancer
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HDAC/BET-IN-1 displays submicromolar inhibitory activity against HDAC1 and 6 (IC50 = 0.163 μM and 0.067 μM), and BRD4 (Ki = 0.076 μM), and possess potent antileukemia activity.
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- HY-78695
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Epigenetic Reader Domain
PD-1/PD-L1
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Cancer
|
JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4.
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- HY-157592
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Epigenetic Reader Domain
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Cancer
|
MMH2-NR a negtive control of MMH2. MMH2 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader .
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- HY-131387
-
|
E3 Ligase Ligand-Linker Conjugates
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Cancer
|
(S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the a VHL ligand and a linker. (S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 can be used in PROTAC BRD4 Degrader-5 (HY-133737) and PROTAC BRD4 Degrader-5-CO-PEG3-N3 (HY-133736) .
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- HY-145925B
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Epigenetic Reader Domain
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Cancer
|
CFT8634 is an oral activity degrader targeting BRD9 extracted from patent WO2021178920A1 compound 174. CFT8634 can be used for the research of synovial sarcoma and SMARCB1-deleted solid tumors .
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- HY-122826
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PROTACs
Epigenetic Reader Domain
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Cancer
|
ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM .
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- HY-101146
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SF2523
2 Publications Verification
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PI3K
Epigenetic Reader Domain
DNA-PK
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Cancer
|
SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
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- HY-157591
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Others
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Others
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MMH1-NR, containing a non-reactive (ethyl) group is a negative control of MMH1. MMH1 is a CUL4-associated factor (DCAF16)-based bromodomain protein 4 (BRD4) degrader .
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- HY-100653
-
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Others
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Cancer
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AZD5153 (Compound 13) is a trivalent triazolpyrazine bromide domain (BRD), bromodomain and
extraterminal (BET) inhibitor. AZD5153 has down-regulated c-Myc gene and tumor growth inhibition activity. AZD5153 can be used in the study of BET small molecule inhibitors .
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- HY-114205
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Epigenetic Reader Domain
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Cancer
|
TP-238 is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases .
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- HY-114205A
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Epigenetic Reader Domain
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Cancer
|
TP-238 hydrochloride is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 hydrochloride also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases .
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- HY-141438
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SIM1
1 Publications Verification
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PROTACs
Epigenetic Reader Domain
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Cancer
|
SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC50=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity .
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- HY-132232
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Epigenetic Reader Domain
|
Cancer
|
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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- HY-146999
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Histone Methyltransferase
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer .
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-
- HY-15658
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GSK2801
2 Publications Verification
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Epigenetic Reader Domain
Apoptosis
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Cancer
|
GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4 .
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- HY-142520
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|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
I-BET567 is a potent and orally 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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-
- HY-145667
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Biotin-JQ1
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Epigenetic Reader Domain
|
Cancer
|
Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for the bromodomain of BRD4. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC50 of 0.4 μM .
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-
- HY-100482
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-
- HY-100726
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-
- HY-126428
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|
HIV
Epigenetic Reader Domain
|
Infection
Inflammation/Immunology
|
ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter .
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-
- HY-163282
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HDAC
Epigenetic Reader Domain
|
Cancer
|
NB512 (compound 39a) is a dual inhibitor for BET and HDAC, which exhibits a efficient binding affinity with BRD4 bromodomains and HDAC1/2, with EC50s of 100-400 nM. NB512 exhibits an anti-proliferative activity towards cancer cells PaTu8988T and NMC .
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-
- HY-101519
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ZBC 260
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PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line . BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells .
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-
- HY-120028
-
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Epigenetic Reader Domain
Histone Acetyltransferase
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Cancer
|
GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells .
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-
- HY-136920
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|
Epigenetic Reader Domain
|
Cancer
|
CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 family of bromodomains. CBP/p300-IN-8 inhibits CBP (IC50=0.01-0.1 µΜ) and BRD4 (IC50=1-1000 µΜ) activity .
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-
- HY-145431
-
|
Epigenetic Reader Domain
Parasite
|
Infection
|
(S)-GSK1379725A (compound AU1) is a selective bromodomain and PHD finger containing transcription factor (BPTF) bromodomain inhibitor with a Kd of 2.8 μM. (S)-GSK1379725A shows to be selective for BPTF over BRD4 bromodomain. (S)-GSK1379725A shows antimalarial activity .
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-
- HY-153367
-
|
Epigenetic Reader Domain
|
Cancer
|
FHD-609 is an inhibitor and a degrader of BRD9 (bromodomain-containing protein 9). FHD-609 targets to ncBAF, can be used for research of wide range of cancers that contain a mutation in a BAF complex subunit. FHD-609 in combination with Telomelysin or INO5401, may play a role in adrenocortical carcinoma (ACC) treatment .
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-
- HY-10220
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|
PI3K
Apoptosis
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Cancer
|
SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 proagent, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis .
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-
- HY-130853
-
|
E3 Ligase Ligand-Linker Conjugates
Autophagy
Apoptosis
|
Cancer
|
Thalidomide-NH-PEG2-C2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a PEG linker used for dBRD9 (compound 6) synthesis. dBRD9 is a selective BRD9 probe PROTAC degrader for the study of BAF complex biology .
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-
- HY-151894
-
|
Epigenetic Reader Domain
|
Cancer
|
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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-
- HY-157491
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-
- HY-149878
-
|
Epigenetic Reader Domain
|
Cancer
|
BD-9136 is a highly selective BRD4 degrader. BD-9136 can inhibit tumor growth without adverse effects on mice. BD-9136 can be used for the research of cancer . BD-9136 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-107477
-
|
Epigenetic Reader Domain
|
Cancer
|
GSK8573 is an inactive control compound for GSK2801 (acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains). GSK8573 has binding activity to BRD9 with a Kd value of 1.04 μM and is inactive against BAZ2A/B and other bromodomain familiy. GSK8573 can be used as a structurally related negative control compound in biological experiments .
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-
- HY-156214
-
AP1867-PEG2-JQ1; AP-PEG2-JQ1
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Others
|
Others
|
NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound that bind to proteins in separate cellular compartments that can induce nuclear import of cytosolic cargoes, using nuclear-localized bromodomain-containing protein 4 (BRD4) as a “carrier” for co-import and nuclear trapping of cytosolic proteins .
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-
- HY-125236
-
|
Epigenetic Reader Domain
|
Cancer
|
BET-IN-19 (Compound 146) is a BET inhibitor. BET-IN-19 inhibits hlL-6 mRNA transcription (IC50 ≤ 0.3 uM), and c-myc activity in human AML MV4-11 cell (IC50 ≤ 0.3 uM)。BET-IN-19 inhibits tetra-acetylated histone H4 binding to BRD4 bromodomain 1 (IC50 ≤ 0.3 uM) .
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-
- HY-149735
-
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
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BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC50=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage .
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- HY-111784
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CCS1477
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Epigenetic Reader Domain
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Cancer
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Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression .
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- HY-128341
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ERK
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Cardiovascular Disease
Cancer
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ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis .
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- HY-123941
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dTAG-7
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PROTACs
FKBP
Epigenetic Reader Domain
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Cancer
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FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12 F36V with expression of FKBP12 F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN .
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- HY-150797
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QA-68-ZU81
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Epigenetic Reader Domain
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Inflammation/Immunology
Cancer
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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 . QA-68 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-19999A
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Epigenetic Reader Domain
Histone Acetyltransferase
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Neurological Disease
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PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with IC50 of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1β, IL-6 and IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates RGS4 expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al .
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- HY-133138
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Pomalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker.?Pomalidomide-PEG1-azide?can be used to design a?PROTAC BRD4 Degrader-1 (HY-133131) . Pomalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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- HY-133139
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Lenalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Lenalidomide-PEG1-azide incorporates the Lenalidomide based cereblon ligand and a linker.?Lenalidomide-PEG1-azide?can be used to design a PROTAC BRD4 Degrader-2 (HY-133136) . Lenalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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- HY-130984
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PROTAC Linkers
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Cancer
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Azido-PEG1-CH2COO-Cl (compound 43a) is an alkyl/ether-based PROTAC linker. Azido-PEG1-CH2COO-Cl can be used in the synthesis of PROTAC BRD4 Degrader-1 (HY-133131) . Azido-PEG1-CH2COO-Cl is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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- HY-108369
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PROTAC Linkers
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Cancer
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Azido-PEG1-CH2CO2H is a PROTAC linker, which refers to the alkyl/ether composition. Azido-PEG1-CH2CO2H can be used in the synthesis of PROTAC BRD4 Degrader-1 . Azido-PEG1-CH2CO2H is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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* This product has been "discontinued".
Optimized version of product available:
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-150516S
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BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4[1].
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Cat. No. |
Product Name |
Application |
Reactivity |
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- HY-P80976
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BRD4; CAP; HUNK1; MCAP; Bromodomain containing 4; chromosome associated protein
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WB, IHC-P, ICC/IF, IP
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Human, Mouse, Rat |
BRD4 Antibody is an antibody about 152 kDa, targeting to BRD4.
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- HY-P80037
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WB, ICC, IHC-P, FC
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Human |
BRD2 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 88 kDa, targeting to BRD2. It can be used for WB,ICC,IHC-P,FC assays with tag free, in the background of Human.
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Product Name |
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Classification |
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- HY-107442
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Alkynes
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PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136) . PROTAC BRD4-binding moiety 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-133736
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Azide
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PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader GNE-987 and PEG-based linker . PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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- HY-101460
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Tetrazine
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Tz-Thalidomide is a tetrazine tagged Thalidomide (HY-14658) (Ligands for E3 Ligase). Tz-Thalidomide has binding affinity for BRD4, with IC50s of 46.25 μM (BRD4-1) and 62.55 μM (BRD4-2). Tz-Thalidomide is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups .
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- HY-133138
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Azide
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Pomalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker.?Pomalidomide-PEG1-azide?can be used to design a?PROTAC BRD4 Degrader-1 (HY-133131) . Pomalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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- HY-133139
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Azide
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Lenalidomide-PEG1-azide is a E3 ligase lgand-linker conjugate. Lenalidomide-PEG1-azide incorporates the Lenalidomide based cereblon ligand and a linker.?Lenalidomide-PEG1-azide?can be used to design a PROTAC BRD4 Degrader-2 (HY-133136) . Lenalidomide-PEG1-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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- HY-130984
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Azide
PROTAC Synthesis
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Azido-PEG1-CH2COO-Cl (compound 43a) is an alkyl/ether-based PROTAC linker. Azido-PEG1-CH2COO-Cl can be used in the synthesis of PROTAC BRD4 Degrader-1 (HY-133131) . Azido-PEG1-CH2COO-Cl is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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- HY-108369
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PROTAC Synthesis
Azide
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Azido-PEG1-CH2CO2H is a PROTAC linker, which refers to the alkyl/ether composition. Azido-PEG1-CH2CO2H can be used in the synthesis of PROTAC BRD4 Degrader-1 . Azido-PEG1-CH2CO2H is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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