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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
18 Results for "
BD1 domains
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "BD1 domains" in MCE Product Catalog:
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 .
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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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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 .
Cat. No.: HY-163729
CAS No.: 2201082-98-4
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I-BET787 is a orally active BET bromine domain inhibitor with pIC50s of 7.1 and 5.9 for BRD4 BD1 and BRD4 BD2, respectively. I-BET787 has anti-inflammatory activity in mice .
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Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of <2.5 nM (CDK4), 3.3 nM (CDK6), 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ) , respectively. SRX3177 blocks the interaction between the SARS-CoV-2 E protein and the BRD2/4 BD1 domain, restores E protein-attenuated NF-κB activity. SRX3177 exerts broad cytotoxic activity against cancer cells. SRX3177 can be used for the study of anti-SARS-CoV-2 and cancer .
Cat. No.: HY-138623
CAS No.: 2540591-06-6
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GSK789 is a selective inhibitor of BET BD1. GSK789 inhibits the growth of leukemia cell lines. GSK789 inhibits LPS-stimulated production of MCP-1, TNFα and IL-6 in human whole blood. GSK789 exhibits antiproliferative, anti-inflammatory and immunomodulatory activities. GSK789 can be used in research related to cancers such as leukemia, as well as inflammatory and immune diseases .
Cat. No.: HY-136794
CAS No.: 219769-23-0
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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) .
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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 .
Cat. No.: HY-170380
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XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC50 of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity .
Cat. No.: HY-149761
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GSK023 (compound 31) is a selective chemical probe targeting the BET BD1 domain .
Cat. No.: HY-132232
CAS No.: 2159137-02-5
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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 .
Cat. No.: HY-170226
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BET-IN-28 (Compound 44) is a highly potent inhibitor of bromodomain and extra-terminal domain (BET), with an IC50 value of 4.47 nM against BRD4-BD1. BET-IN-28 blocks the interaction between BET proteins and N-acetylated lysine residues on histone tails, down-regulates certain genes. BET-IN-28 can be used for hematological malignancies and solid tumors study .
Cat. No.: HY-151972
CAS No.: 2976403-41-3
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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.
Cat. No.: HY-186267
CAS No.: 3037514-35-2
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BD-7148 is a potent, highly selective BRD4 PROTAC degrader with a DC50 of 0.9 nM. BD-7148 binds to recombinant human BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1 and BRD4-BD2 domain proteins, with Kd values ranging from 26 nM to 240 nM, and shows no binding preference for BRD4 domains over BRD2 or BRD3 domains. BD-7148 inhibits the growth of leukemia and breast cancer cells. BD-7148 can be used in the research of leukemia and breast cancer .
Cat. No.: HY-182362
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TK-285 is a potent TSLP inhibitor that suppresses the production of TSLP and inhibits the expression of interleukin-33 mRNA. TK-285 exhibits a selective binding preference for the BD1 domains of BRD2, BRD3, BRD4 and BRDT. TK-285 can be used in research related to atopic dermatitis .
Cat. No.: HY-182371
CAS No.: 3076613-24-3
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BRD4 ligand 15 (compound 5) is a BRD4 ligand and alkyne-modified chalcone derivative, which serves as a building block for the synthesis of BRD4-targeting PROTAC TKP-5 (HY-182370) .
Cat. No.: HY-186268
CAS No.: 3034180-15-6
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BRD4 ligand-Linker Conjugate 8 is a Target Protein Ligand-Linker Conjugate that can be used in studies related to PROTAC synthesis. BRD4 ligand-Linker Conjugate 8 is applicable for the synthesis of BD-7148 (HY-186267) .
Cat. No.: HY-184339
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BRD4-IN-42 is a BRD4 BD1 inhibitor with an IC50 of 108.50 nM. BRD4-IN-42 can be used for the synthesis of PROTACs and serves as the target protein moiety of PROTAC BET Degrader-18 (HY-184335). BRD4-IN-42 inhibits the proliferation of wild-type and SHP099-resistant acute myeloid leukemia cells. BRD4-IN-42 is applicable to research related to acute myeloid leukemia .
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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
