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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
93 Results for "
BRD4 BD1 inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (93)
93 Results for "BRD4 BD1 inhibitor" in MCE Product Catalog:
13
13 Publications Verification
Research Areas:
CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP .
5
5 Cited Publications
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dBET57 is a potent and selective BRD4BD1 PROTAC degrader with a DC50 of approximately 500 nM. dBET57 forms a ternary complex with CRL4 CRBN and BRD4BD1, induces the ubiquitination and degradation of BRD4, and indirectly inhibits the transcription of MYCN, c-Myc and PD-L1, ultimately leading to cell cycle arrest and apoptosis. dBET57 can be used in related research on neuroblastoma, non-small cell lung cancer and colorectal cancer .
4
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MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM).
4
4 Cited Publications
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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).
3
3 Cited Publications
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ZXH-3-26 is a CRBN-recruiting BRD4 PROTAC degrader with a DC50/5h of approximately 5 nM. ZXH-3-26 drives the ubiquitination and degradation of BRD4 by recruiting BRD4BD1 to the CRL4 CRBN E3 ubiquitin ligase complex, thereby inhibiting the dynamic distribution of super-enhancers. ZXH-3-26 reverses TNF-α-induced impairment of the immunosuppressive function of mesenchymal stem cells, and affects RNA synthesis and the transcriptional elongation process of Pol II. ZXH-3-26 can be used in studies related to inflammatory arthritis, malignant tumors, and HIV latency .
3
3 Cited Publications
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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 .
2
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GSK778 (iBET-BD1), a chemical probe, 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 .
2
2 Cited Publications
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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 .
2
2 Cited Publications
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HJB97 is a high-affinity BET inhibitor with Ki values 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), and 1.0 nM (BRD4 BD2) . HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity . HJB97 can be used for the synthesis of BETd-260 (HY-101519).
2
2 Cited Publications
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ZL0454 is a potent and selective Bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of 49 and 32 nM for BD1 and BD2.
1
1 Cited Publications
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GSK8814 is a potent and selective ATAD2 bromodomain chemical probe and inhibitor (IC50 = 0.059 μM), 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. GSK8814 can be researched for cancer associated with ATAD2 bromodomain .
1
1 Cited Publications
Cat. No.: HY-162514
CAS No.: 2644662-83-7
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BBC0403 is a selective BRD2 inhibitor with Kds of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. BBC0403 exhibitS higher binding specificity for BRD2 compared to BRD3 and BRD4. BBC0403 has the potential for osteoarthritis (OA) research .
1
1 Cited Publications
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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 .
1
1 Cited Publications
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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 .
1
1 Cited Publications
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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 .
Synonyms: CPI-0610
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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 .
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iBRD4-BD1 is selective BRD4 bromodomain inhibitor. iBRD4-BD1 has inhibition activity for BRD4 bromodomain with an IC50 value of 12 nM. iBRD4-BD1 can be used for the research of inflammation and oncology .
Research Areas:
BRD4 degrader-3 is a molecular glue degrader targeting BRD4, with binding activity towards the BD1 and BD2 domains of BRD4. BRD4 degrader-3 regulates the activity of BRD4. BRD4 degrader-3 inhibits MYC expression in cancer cells. BRD4 degrader-3 suppresses cell proliferation. BRD4 degrader-3 can be used in research related to acute myeloid leukemia and prostate cancer .
Synonyms: BI894999
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Amredobresib (BI894999) is an orally active BET inhibitor. Amredobresib inhibits the binding of BRD4-BD1 and BRD4-BD2 bromodomains to acetylated histones with IC50 values of 5 nM and 41 nM, respectively. Amredobresib exhibits anticancer activity against acute myeloid leukemia (AML) and NUT cancer .
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BD-9136 is a selective BRD4 PROTAC degrader with a DC50 of 1.2 nM, and exhibits a selectivity of ≥1000-fold over BRD2 and BRD3. BD-9136 preferentially forms a ternary complex with the BD1 domain of BRD4, and downregulates the expression of B7-H4 by disrupting the PR-P300-BRD4 axis. BD-9136 depletes BRD4 protein in tumor tissues, inhibits tumor growth, reduces B7-H4 protein expression, increases CD8+ T cell infiltration, and enhances tumor sensitivity to anti-PD-L1. Degradation of BRD4 by BD-9136 rescues the erythroid differentiation block induced by LSD1 inhibition, and transient administration restores erythroid output while retaining HbF induction. BD-9136 causes no adverse effects in mice at effective doses. BD-9136 can be used in studies related to acute myeloid leukemia, acute lymphoblastic leukemia and breast cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
