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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
119 Results for "
BRD4-degrading PROTAC
" in MedChemExpress (MCE) Product Catalog:
Products (119)
119 Results for "BRD4-degrading PROTAC" in MCE Product Catalog:
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2 Cited Publications
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BRD4 degrader AT1 is a selective PROTAC BRD4 degrader. BRD4 degrader AT1 induces depletion of Brd4 protein in cells. BRD4 degrader AT1 exhibits highly selective depletion of Brd4 over Brd2 and Brd3 in cells .
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2 Cited Publications
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MZP-54 is a PROTAC degrader that selectively targets BRD3/BRD4, with a DC50 of < 0.05 μM in AML cells. MZP-54 recruits VHL to form a ternary complex, induces BRD3/BRD4 degradation via the ubiquitin-proteasome pathway, inhibits c-Myc expression, and exerts antiproliferative activity. MZP-54 can be used for the research of acute myeloid leukemia .
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1 Cited Publications
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GNE-987 is a VHL-dependent BRD4 PROTAC degrader. 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 can be used for the research of cancer .
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PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader (MZ 1 (HY-107425) analog) 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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. PROTAC BRD4 Degrader-5-CO-PEG3-N3 can be used for the research of HER2-positive breast cancer .
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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 .
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PROTAC BET Degrader-10 (dBET37) is a potent BET protein BRD4 degrader, connected by ligands for Cereblon and BRD4, with a DC50 of 49 nM .
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(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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PROTAC BRD4 Degrader linker conjugate is a linker-payload conjugate as well as a bifunctional degrader of BRD4 that binds to VHL, consisting of PROTAC and a linker. PROTAC BRD4 Degrader linker conjugate can be conjugated with STEAP1 and CLL1 antibodies to degrade BRD4 protein, with DC50 values of 0.86 nM and 7.6 nM, respectively. PROTAC BRD4 Degrader linker conjugate can be used in research related to prostate cancer and acute myeloid leukemia (BRD4 ligand: (HY-129939); VHL ligand: (HY-125845)) .\n
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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 .
Cat. No.: HY-133136
CAS No.: 2185795-53-1
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PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 14.2 nM against BRD4 BD1 .
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TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation .
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 .
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Pomalidomide-PEG1-azide is an E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-PEG1-azide can be used to synthesis PROTAC BRD4 Degrader-1 (HY-133131) . 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.
Cat. No.: HY-147046
CAS No.: 2421153-77-5
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ET-JQ1-OH is an allele-specific BET inhibitor. ET-JQ1-OH can serve as a Ligand for Target Protein for PROTAC, and is used for the development and design of PROTAC Brd4 degraders, such as AB3145 (HY-180923).
Cat. No.: HY-161651A
CAS No.: 2763548-61-2
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BRD4 ligand 6 TFA is the TFA salt form of BRD4 ligand 6 (HY-161651). BRD4 ligand 6 TFA is a BRD4 ligand and can be used for synthesis of BRD4 PROTACs, such as PROTAC BRD4 Degrader-26 (HY-161650) .
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-143328
CAS No.: 2585561-49-3
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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 .
Cat. No.: HY-131203
CAS No.: 2410947-56-5
PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4PROTAC 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 .
Cat. No.: HY-174210
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PROTAC BRD4 Degrader-3 is a potent BRD4 PROTAC degrader with DC50 values of 164 nM and 80 nM at 4 h and 24 h, respectively. PROTAC BRD4 Degrader-3 induces the ubiquitination and subsequent proteasomal degradation of BRD4 by recruiting the ubiquitin E3 ligase KLHDC2. PROTAC BRD4 Degrader-3 can be used in breast cancer research .
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 .
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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
