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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
41 Results for "
BRD4-IN-4
" in MedChemExpress (MCE) Product Catalog:
Products (41)
41 Results for "BRD4-IN-4" in MCE Product Catalog:
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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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5 Cited Publications
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AZD5153 is a bivalent, selective, and orally active BET/BRD4 bromodomain inhibitor with an IC50 of value of 5 nM for full-length BRD4 (FL-BRD4). AZD5153 ligates two bromodomains in BRD4 simultaneously. AZD5153 can be used for the study of cancer, such as acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma .
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2 Cited Publications
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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 .
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MMH2 is a novel BRD4 molecular glue degrader that functions by recruiting the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2) .
Cat. No.: HY-107425A
CAS No.: 1797406-72-4
Synonyms: MZP-42
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cis-MZ 1 (MZP-42) serves as a negative control for BRD4-targeted PROTAC MZ 1 (HY-107425). cis-MZ 1 can be used in colorectal cancer-related research .
Synonyms: PROTAC BRD4 Degrader-5
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GAL-02-221 is a BRD4 PROTAC degrader with blood-brain barrier permeability, with a DC50 of 0.009 μM (Jurkat BRD4-HiBiT). GAL-02-221 induces proteasome-catalyzed BRD4 degradation, binds to VHL to trigger BRD4 ubiquitination, and recruits the VHL E3 ligase complex to participate in protein degradation. GAL-02-221 degrades BRD4 in breast cancer cells as well as mouse liver and brain tissues. GAL-02-221 is applicable to research related to breast cancer .
MMH1 is a novel BRD4 molecular glue degrader. MMH1 functions by recruiting the CUL4 DCAF16 ligase to the second bromodomain of BRD4 (BRD4 BD2). MMH1 binds to the JQ1-binding site of BRD4 BD2, acts as a template to covalently modify Cys58 of DCAF16, stabilizes the BRD4-DCAF16 ternary complex, and thereby promotes BRD4 degradation via the CRL4DCAF16 ubiquitin ligase pathway. Using BRD4 BD2 as a structural template, MMH1 covalently modifies Cys87 of GAK and induces the GAK-BRD4 BD2 interaction. Through its covalent mechanism, MMH1 exhibits sustained BRD4 degradation activity, and shows selective degradation activity for BRD4 BD2 over BRD4 BD1 .
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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.
Cat. No.: HY-164995
CAS No.: 2417370-68-2
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L1BC8 (compound 13a) is a BRD4 PROTAC degrader with anticancer effects. L1BC8 is also a drug-linker conjugate for ADC that can be used for the synthesis of ADCs. The resulting BRD4-degrader antibody conjugates exhibit potent and antigen-dependent BRD4 degradation and antiproliferation activities in cell-based experiments .
Cat. No.: HY-44103
CAS No.: 2126819-55-2
Synonyms: PROTAC BRD4-bINdINg moiety 4
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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.
Cat. No.: HY-160267
CAS No.: 950403-60-8
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iPAF1C is a inhibitor of the polymerase-associated factor 1 complex (PAF1C) with specific targeting to the PAF1 binding groove of CTR9 (a key subunit of PAF1C). iPAF1C disrupts PAF1C assembly by interfering with the PAF1-CTR9 interaction. iPAF1C selectively impairs BRD4-mediated recruitment of PAF1 to chromatin at hypoxia-responsive genes and inhibits RNA polymerase II (RNAPII) pause release. iPAF1C increases the population of HIV-1 NL4.3 Nef-IRES-GFP infected primary human CD4 +T cells in a dose-dependent manner. PAF1C can be used for the study of infection and diseases associated with abnormal hypoxic adaptation (e.g., cancers, neurological disorders) .
Cat. No.: HY-160694
CAS No.: 2417369-73-2
Synonyms: cBu-Cit-PROTAC BRD4 Degrader-5
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cBu-Cit-GAL-02-221 (cBu-Cit-PROTAC BRD4 Degrader-5) is a BRD4 PROTAC-linker conjugate with a protease-cleavable cBu-Cit linker. cBu-Cit-GAL-02-221 can be conjugated with antibodies to form PACs, and releases a VHL-recruiting BRD4 degrader inside cells. cBu-Cit-GAL-02-221 is applicable to studies on BRD4-targeted degradation, antibody-mediated PROTAC delivery and PAC construction .
Cat. No.: HY-156566
CAS No.: 2503036-46-0
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PROTAC BRD4 Degrader-21 is a BRD4-targeting PROTAC degrader with an IC50 value of 59 nM. PROTAC BRD4 Degrader-21 induces ubiquitination of BRD4, leading to its degradation via the proteasome. PROTAC BRD4 Degrader-21 binds to recombinant HSP90α protein with moderate affinity, having an IC50 of 100-1000 nM. PROTAC BRD4 Degrader-21 induces cancer cell death. PROTAC BRD4 Degrader-21 inhibits tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-21 can be used for the research of acute myeloid leukemia, diffuse large B-cell lymphoma .
Cat. No.: HY-173450
CAS No.: 2230496-93-0
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ZL0516 is a potent, selective, and orally active BRD4 BD1 inhibitor. ZL0516 suppresses inflammatory bowel disease (IBD) by inhibiting BRD4/NF-κB signaling .
Cat. No.: HY-107425B
Purity: ≥99.0%
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cis-MZ 1 hydrate serves as a negative control for BRD4-targeted PROTAC MZ 1 (HY-107425). cis-MZ 1 hydrate can be used in colorectal cancer-related research .
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Cat. No.: HY-175242
CAS No.: 2954925-72-3
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PROTAC BRD4 ligand-4 is a BRD4 ligand, which can be used to synthesize PROTAC BRD4 Degrader-37 (HY-175225) .
Cat. No.: HY-176449
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PROTAC BRD4 Degrader-32 (Compound 22) is a BRD4 PROTAC degrader (DC50: 0.20 nM). PROTAC BRD4 Degrader-32 connects the BRD4-binding domain and CRBN-binding domain through a unique carbon-carbon linked linker to form a ternary complex, inducing ubiquitination of BRD4 for proteasomal degradation. PROTAC BRD4 Degrader-32 is promising for research of BRD4-related cancers (such as hematological malignancies) .
Cat. No.: HY-174920
CAS No.: 1797406-70-2
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PROTAC BRD4 Degrader-34 (1797406-70-2) is a VHL-recruiting PROTAC BRD4 degrader. PROTAC BRD4 Degrader-34 induces degradation of the short isoform of BRD4 and can be used in studies of BRD4-related diseases and targeted protein degradation .
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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
