Search Result
Results for "
brd4+degrader
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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-133736
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PROTAC-Linker Conjugates for PAC
ADC Payload
Epigenetic Reader Domain
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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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- HY-114305
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A1874
2 Publications Verification
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PROTACs
Epigenetic Reader Domain
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Cancer
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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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- HY-136857
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Epigenetic Reader Domain
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Cancer
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BRD4 degrader-3 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.
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- HY-163638
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Epigenetic Reader Domain
Molecular Glues
E1/E2/E3 Enzyme
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Cancer
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BRD4 degrader-1 (Compound mL 1-50) is a relatively selective, monovalent and covalent BRD4 Molecular glue degrader. BRD4 degrader-1 induces degradation of both long and short isoforms of BRD4 by targeting DCAF16 (an E3 ligase). BRD4 degrader-1 can be used in breast cancer research .
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- HY-133131
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PROTACs
Epigenetic Reader Domain
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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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- HY-112718
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- HY-138555
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PROTACs
Epigenetic Reader Domain
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Cancer
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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 .
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- HY-138632
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PROTACs
Epigenetic Reader Domain
PROTAC-Linker Conjugates for PAC
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Cancer
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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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- HY-131387
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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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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- HY-133136
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- HY-133737
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PROTAC brd4 Degrader-5
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PROTACs
Epigenetic Reader Domain
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Cancer
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GAL-02-221 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GAL-02-221 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines .
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- HY-114406
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Ligands for E3 Ligase
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Cancer
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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 .
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- HY-129917
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PROTACs
Epigenetic Reader Domain
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Cancer
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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 .
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- HY-151593
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PROTACs
Epigenetic Reader Domain
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Cancer
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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 .
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- HY-164995
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PROTACs
Epigenetic Reader Domain
Drug-Linker Conjugates for ADC
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Cancer
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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. (Pink: BRD4 ligand (HY-129939); Blue: VHL ligand (HY-125845); Black: linker (HY-171663)) .
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- HY-147046
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- HY-156566
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PROTACs
Epigenetic Reader Domain
HSP
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Cancer
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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 .
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- HY-143328
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PROTACs
Epigenetic Reader Domain
Apoptosis
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Cancer
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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 .
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- HY-131203
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PROTACs
Epigenetic Reader Domain
Apoptosis
c-Myc
Caspase
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Cancer
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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 (Pink:
Mivebresib (HY-100015); Black: linker, Azido-PEG1-CH2CO2H (HY-108369); Blue: Lenalidomide (HY-A0003)) .
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- HY-123911
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- HY-174210
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-31 is a BRD4 PROTAC degrader with DC50 s of 164 and 80 nM at 4 h and 24 h, respectively. PROTAC BRD4 Degrader-31 potently degrades BRD4 in cells with long acting degradation kinetics . Pink: BRD4 ligand (HY-78695); Blue: KLHDC2 ligand (HY-174218)
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- HY-161651A
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Epigenetic Reader Domain
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Cancer
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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) .
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- HY-160694
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cBu-Cit-PROTAC brd4 Degrader-5
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PROTAC-Linker Conjugates for PAC
Epigenetic Reader Domain
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Cancer
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cBu-Cit-GAL-02-221 is a PROTAC that degrades BRD4 by association with cBu-Cit. cBu-Cit-GAL-02-221 can effectively inhibit BRD4 in HER2 positive and negative breast cancer cell lines. cBu-Cit-GAL-02-221 has a single bond and can be conjugated to an ADC antibody to form a PAC .
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- HY-155393
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- HY-175224
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-36 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-36 has a DC50 of 0.649 nM and a Dmax of 71% in PANC-1 cells. PROTAC BRD4 Degrader-36 is cytotoxic to PANC-1 cells (GI50: 0.103 μM). PROTAC BRD4 Degrader-36 can be used in the study of cancer. (Pink: PROTAC BRD4 ligand-1 (HY-129939); Blue + Black: E3 ligase ligand + linker (HY-175241)) .
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- HY-174811
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PROTACs
Epigenetic Reader Domain
PD-1/PD-L1
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Inflammation/Immunology
Cancer
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PROTAC BRD4 Degrader-33 is an enzyme activated clickable BRD4 PROTAC degrader with favorable tumor microenvironment-response. PROTAC BRD4 Degrader-33 has superior tumor tissue penetration capabilities and efficiently inhibits PD-L1 protein expression. PROTAC BRD4 Degrader-33 shows potent anti-tumoral immunomodulation activity in 4T1 tumor-bearing mice model . Pink: BRD4 ligand (HY-174812); Blue: CRBN ligase ligand (HY-10984); Black: linker
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- HY-130612
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Epigenetic Reader Domain
PROTACs
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Cancer
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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 .
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- HY-156774
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PROTACs
Epigenetic Reader Domain
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Others
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CCW 28-3 is a PROTAC-based BRD4 degrader in a proteasome- and RNF4-dependent manner (Pink: JQ-1 (carboxylic acid) (HY-78695); Black: linker (HY-170384); Blue: RNF4 ligand CCW16 (HY-143346)) .
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- HY-163639
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Molecular Glues
Epigenetic Reader Domain
E1/E2/E3 Enzyme
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Cancer
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BRD4 degrader-2 (Compound JP-2-197) is a covalent monovalent molecular glue BRD4degrader that induces a ternary complex formation between BRD4 and RNF126. BRD4 degrader-2 targets RNF126 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells .
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- HY-177730
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-40 is a Bromodomain protein 4 (BRD4) PROTAC degrader. PROTAC BRD4 Degrader-40 can induce BRD4 degradation in cancer cells. PROTAC BRD4 Degrader-40 can be used for the research of cancer, such as leukemia . (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: CRBN ligand (HY-163927))
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- HY-143327
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PROTACs
Epigenetic Reader Domain
Apoptosis
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Cancer
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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 .
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- HY-173327
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PROTACs
Epigenetic Reader Domain
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Cancer
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BRD4 degrader-6 is a dimeric BDR4 PROTAC degrader (DC50: < 0.1 μM). BRD4 degrader-6 promotes the ubiquitination and degradation of BDR4 and has anticancer activity .
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- HY-175225
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-37 (Compound TrimTAC-2) is a PROTAC BRD4 degrader. PROTAC BRD4 Degrader-37 has a DC50 of 36.4 nM and a Dmax of 73% in PANC-1 cells. PROTAC BRD4 Degrader-37 exhibits cytotoxicity against PANC-1 cells (GI50: 0.282 μM). PROTAC BRD4 Degrader-37 can be used in the research of tumors. (Pink: PROTAC BRD4 ligand-4 (HY-175242); Blue + Black: E3 ligase ligand + linker (HY-175241)) .
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- HY-175767
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-39 is a selective targeting Bromodomain protein 4 (BRD4) degrader with an DC50 value of 24.66 nM. PROTAC BRD4 Degrader-39 conjugates BRD PROTAC (ARV-771) (HY-100972) with carbohydrate. PROTAC BRD4 Degrader-39 selectively delivers to tumor cells with high GLUT1 expression, followed by GSH-triggered release of ARV-771 and degrades BRD4. PROTAC BRD4 Degrader-39 can inhibit tumor growth and show no significant toxicity. PROTAC BRD4 Degrader-39 can be used for the research of cancer, such as breast cancer . (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: (HY-42427); BRD4 ligand-Linker: (HY-42429))
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- HY-177041
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-35 (Compound 17) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-35 can be studied in anticancer research. (Pink: BRD4 ligand (HY-78695); Black: linker; Blue: ligase) .
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- HY-174920
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-34 (Compound MZ2) is a selective BRD4 PROTAC degrader (pDC50 = 8.4). PROTAC BRD4 Degrader-34 can induce BD2 degradation mediated by VHL. PROTAC BRD4 Degrader-34 can be used for research on cancer. (Pink: BRD4-BD2 Ligand (HY-78695); Blue: VHL Ligand (HY-125845); Black: Linker (HY-130524)) .
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- HY-163019
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- HY-153820
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- HY-161651
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Epigenetic Reader Domain
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Cancer
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BRD4 ligand 6 is a BRD4 ligand and can be used for synthesis of BRD4 PROTACs, such as PROTAC BRD4 Degrader-26 (HY-161650) .
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- HY-138635
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PROTACs
Epigenetic Reader Domain
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Cancer
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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 .
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- HY-138633
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PROTACs
Epigenetic Reader Domain
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Cancer
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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 .
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- HY-138637
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PROTACs
Epigenetic Reader Domain
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Cancer
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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 .
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- HY-139294
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PROTACs
Epigenetic Reader Domain
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Cancer
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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 .
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- HY-176368
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PROTAC Linkers
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Cancer
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NH2-PEG-phenol-PEG-COOtBu is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs, such as PROTAC BRD4 Degrader-14 (HY-138637) .
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- HY-176449
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PROTACs
Epigenetic Reader Domain
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Cancer
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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). (Pink: GSK1324726A (HY-13960); Black: linker (HY-176450); Blue: Lenalidomide-5-Br (HY-W072954)) .
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- HY-135558
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- HY-161650
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-26 (PROTAC-2) is a photo-regulated PROTAC, which degrades 80% BRD4 at 1 μM by using photocleavable linker. PROTAC BRD4 Degrader-26 will be deactivated by UV light. (Pink: ligand for target protein BRD4 ligand 6 (HY-161651); Black: linker (HY-161653); Blue: E3 ligase ligand Thalidomide 4-fluoride (HY-41547))
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- HY-175240
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-38 is a BRD4 PROTAC degrader with DC50s of 86 and 106 nM for the short and long isoforms of BRD4, respectively. PROTAC BRD4 Degrader-38 significantly induces the degradation of BRD4 by covalently engaging C232 of E3 ligase TRIM28 .Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand (HY-203082); Black: linker (HY-40172)
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- HY-130813
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- HY-176369
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- HY-175610
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PROTACs
FLT3
JAK
Epigenetic Reader Domain
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Cancer
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PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .
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- HY-160527
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Epigenetic Reader Domain
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Cancer
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BRD4 degrader-4 (Compound 1-f) is a BRD4 degrader. BRD4 degrader-4 can be used for the research of cancer and other bromodomain related diseases .
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- HY-161093
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PROTACs
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Cancer
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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 .
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- HY-170989
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HyT
Epigenetic Reader Domain
Autophagy
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Cancer
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BRD4 degrader-5 (Compound 23) is a hydrophobic tag (HyTag)-based protein degrader for BRD4 (DC50 = 24.7 μM) through ER stress and autophagy-lysosome pathway. BRD4 degrader-5 inhibits the proliferation of cancer cell 4T1 with an IC50 of 20.6 μM .
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- HY-174222
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PROTAC Linkers
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Cancer
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4-Piperidineethanol-piperidine-Boc is a PROTAC linker can be used in the synthesis of PROTAC BRD4 Degrader-31 (HY-174210) .
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- HY-175179
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Epigenetic Reader Domain
E1/E2/E3 Enzyme
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Cancer
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LO-3-61, a JQ-1 (HY-13030) analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells .
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- HY-175242
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- HY-174218
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Ligands for E3 Ligase
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Cancer
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KLHDC2 ligand 1 is an E3 ligase ligand. KLHDC2 ligand 1 can be used for synthesis of PROTAC BRD4 Degrader-31 (HY-174210) .
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- HY-172124
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-29 (compound 7a) is a potent PROTACs degrader of BRD4, with the DC50 of 89.4 nM. PROTAC BRD4 Degrader-29 plays an important role in cancer research (Pink: ligand for target protein (HY-13030); Black: linker (HY-172125); Blue: E3 ligase ligand (HY-103597)) .
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- HY-130814
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E3 Ligase Ligand-Linker Conjugates
Autophagy
Apoptosis
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Cancer
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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 .
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- HY-174812
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- HY-157592
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- HY-170808
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD4 Degrader-28 (Compound 4) is a PROTAC degrader targeting BRD4. PROTAC BRD4 Degrader-28 is promising for research of cancers (Pink: target protein ligand JQ-1 (carboxylic acid) (HY-78695); Black+ Blue: E3 ubiquitin ligase ligand-Linker conjugate Thalidomide-O-amido-C3-NH2 (HY-115560)) .
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- HY-176070
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Epigenetic Reader Domain
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Cancer
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HRG038 is a selective covalent BRD4 degrader. HRG038 binds covalently to the E3 ubiquitin ligase CUL4 DCAF16, recruiting it to BRD4, leading to the ubiquitination and subsequent proteasomal degradation of BRD4. HRG038 is promising for research of cancers .
|
-
- HY-174813
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
Pomalidomide-PEG3-Cys is an E3 ligase ligand-linker conjugate that incorporates a CRBN ligand Pomalidomide (HY-10984) and 3-unit PEG linker. Pomalidomide-PEG3-Cys can be used for synthesis of PROTAC BRD4 Degrader-33 (HY-174811) .
|
-
- HY-162875
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-27 (compound 6b) is a PROTAC that selectively targets BRD4 (rather than BRD2/BRD3) and can also inhibit the expression of KLF5 transcription factor and exert anti-cancer activity. PROTAC BRD4 Degrader-27 is composed of E3 ubiquitinase ligand Thalidomide-4-OH (HY-103596) (red part), PROTAC Linker γ-Aminobutyric acid (HY-N0067) (black part) and PROTAC target protein ligand PROTAC BRD4 ligand-3 (HY-162876) (blue part), of which the active control of the target protein ligand is Mivebresib (HY-100015), and the conjugate of E3 ubiquitin ligase ligand + Linker is Pomalidomide 4'-alkylC3-acid (HY-131875) [1] .
|
-
- HY-180150
-
|
|
Epigenetic Reader Domain
c-Myc
Bcl-2 Family
Apoptosis
|
Cancer
|
|
PROTAC BRD4 Degrader-42 (Compound P6) is a PROTAC-based BRD4 degrader with a DC50 of 1.11 μM. PROTAC BRD4 Degrader-42 promotes the ubiquitination and degradation of BRD4. PROTAC BRD4 Degrader-42 downregulates c-Myc expression and induces Apoptosis by upregulating BAD and BAX protein expression. PROTAC BRD4 Degrader-42 also exhibits anticancer activity against myeloid monocytic leukemia .
|
-
- HY-183077
-
|
|
Epigenetic Reader Domain
Molecular Glues
|
Cancer
|
|
BRD4 degrader-7 (Compound ZZ1) is a CTLH-dependent BRD4 degrader and c-Glue with a DC50 of 489 nM. BRD4 degrader-7 converts to a sulfinic acid derivative inside cells, interacts with the basic pocket of YPEL5, mediates the bridging of BRD4 BD1 to the YPEL5 subunit of the CTLH E3 ubiquitin ligase, and thereby promotes the formation of a ternary complex. BRD4 degrader-7 can be used in research on Ewing's sarcoma and leukemia .
|
-
- HY-182801
-
|
|
PROTACs
Epigenetic Reader Domain
c-Myc
|
Cancer
|
|
PROTAC BRD4 Degrader-46 is a heterobifunctional BRD4 PROTAC degrader. PROTAC BRD4 Degrader-46 binds to both BRD4 and CRBN, thereby triggering ubiquitination and proteasomal degradation of BRD4. PROTAC BRD4 Degrader-46 downregulates the levels of downstream BRD2, BRD3 and MYC. PROTAC BRD4 Degrader-46 can be used in the research of cancers such as multiple myeloma .
|
-
- HY-181553
-
|
|
PROTACs
|
Others
|
|
PROTAC BRD4 Degrader-44 is a BRD4 PROTAC degrader with a DC50 of 16 nM. PROTAC BRD4 Degrader-44 is applicable to studies on membrane-permeable PROTACs .
|
-
- HY-161167
-
|
|
PROTACs
|
Cancer
|
|
MM-02-08 is the potent BRD4 degrader and binds to DDB1 .
|
-
- HY-179734
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
c-Myc
|
Cancer
|
|
PROTAC BRD4 Degrader-41 (Compound A5) is a BRD4 PROTAC degrader with a DC50 of 0.97 nM. PROTAC BRD4 Degrader-41 exhibits potent anti-proliferative activity against various types of cancer cells such as AML, lymphoma, breast cancer, ovarian cancer, and non-small cell lung cancer. PROTAC BRD4 Degrader-41 can induce G0/G1 phase arrest and apoptosis in MV4-11 cells. PROTAC BRD4 Degrader-41 downregulates the transcriptional level of c-Myc .
|
-
- HY-149328
-
|
|
PROTACs
|
Cancer
|
|
phoBET1 is a photocaged-PROTAC. phoBET1 can achieve BRD4 degradation and effectively suppress tumor growth .
|
-
- HY-172125
-
|
|
PROTAC Linkers
|
Cancer
|
|
AMPRO-222 is a PROTAC linker that can act as a linker of PROTAC PROTAC BRD4 Degrader-29 (HY-172124) .
|
-
- HY-181553A
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-45 (Compound 2b) is a PROTAC degrader targeting BRD4. PROTAC BRD4 Degrader-45 exhibits enhanced passive membrane permeability, stability in cell culture medium supplemented with 10% FBS, and higher intracellular concentrations in cancer cells .
|
-
- HY-181164
-
|
|
PROTACs
Epigenetic Reader Domain
HIV
|
Infection
|
|
PROTAC BRD4 Degrader-43 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-43 recruits the DCAF1-DDB1-Cul4A E3 ligase complex via a Vpr-derived peptide moiety to induce BRD4 ubiquitination and degradation through the ubiquitin-proteasome system. PROTAC BRD4 Degrader-43 exhibits potent HIV latency-reversing activity. PROTAC BRD4 Degrader-43 can be used for the research of HIV-1 latent infection . (Pink: BRD4 ligand (HY-13030); Blue: Cul4A-DDB1-DCAF1 ligand (HY-P11640); Black: conjugate of PEG linker + cell-penetrating peptide (HY-P2483))
|
-
- HY-176725
-
-
- HY-138553A
-
-
- HY-182958
-
|
|
Hsp-targeting Chimeras
Epigenetic Reader Domain
HSP
|
Cancer
|
|
Hsp70TAC BRD4 Degrader-1 is a degrader targeting BRD4, with a KD value of 0.22 μM. Hsp70TAC BRD4 Degrader-1 forms a ternary complex with Hsp70 (KD: 5.13 μM), and specifically and efficiently degrades intracellular BRD4 via the ubiquitin-proteasome pathway. Hsp70TAC BRD4 Degrader-1 exhibits potent anti-tumor proliferative activity. Hsp70TAC BRD4 Degrader-1 can be used in studies related to triple-negative breast cancer and glioblastoma multiforme. (Pink: BRD4 ligand (HY-78695); Blue: HSP70 ligand (HY-182979); Black: linker (HY-B0236)) .
|
-
- HY-176769
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
E3 Ligase Ligand-linker Conjugate 196 is an E3 ligase ligand-linker conjugate. E3 Ligase Ligand-linker Conjugate 196 can be used in the synthesis of PROTAC BRD4 Degrader-38 (HY-175240) .
|
-
- HY-157561
-
-
- HY-172126
-
-
- HY-162876
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
PROTAC BRD4 ligand-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PROTAC BRD4 ligand-3 can be used for synthesis PROTAC BRD4 Degrader-27 (HY-162875) .
|
-
- HY-157591
-
-
- HY-161653
-
|
|
PROTAC Linkers
|
Cancer
|
|
Boc-NH-C3-O-Ph(NO2)-methylester-O-pyrrolidine-2,5-dione is a linker of PROTAC BRD4 Degrader-26 (HY-161650), and can be used for synthesis of PROTACs .
|
-
- HY-203082
-
|
|
Ligands for E3 Ligase
|
Others
|
|
4-[(1E)-2-Nitroethenyl]benzoic acid is an E3 ligase ligand. 4-[(1E)-2-Nitroethenyl]benzoic acid can be used for synthesis of PROTAC BRD4 Degrader-38 (HY-175240) .
|
-
- HY-W957152
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Deoxy-thalidomide-C4-NH2 is a ligand-linker conjugate for the E3 ligase Cereblon (CRBN). Deoxy-thalidomide-C4-NH2 can be used in the synthesis of PROTAC BRD4 Degrader (HY-176449) .
|
-
- HY-175241
-
-
- HY-174220
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Boc-Dipiperidine-KLHDC2 ligand 1 is an E3 ligase ligand-linker conjugate that incorporates a KLHDC2 ligand (HY-174218). Boc-Dipiperidine-KLHDC2 ligand 1 can be used for synthesis of PROTAC BRD4 Degrader-31 (HY-174210) .
|
-
- HY-173255
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
DAO-dBET1 is a Dual-Action-Only PROTAC containing a PROTAC degrader, dBET1 (HY-101838). DAO-dBET1 is a potent BRD4 degrader with a DC50 value of 277 nM in the presence of CoCl2. DAO-dBET1 inhibits hypoxia and Cath-L trigger with an IC50 value of 281 nM .
|
-
- HY-181758
-
|
|
PROTACs
Epigenetic Reader Domain
Histone Acetyltransferase
c-Myc
Apoptosis
|
Cancer
|
|
PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer .
|
-
- HY-179735
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
CRBN ligand-192 is an E3 ligand that can be used for the synthesis of PROTACs, such as PROTAC BRD4 Degrader-41 (HY-179734). PROTAC BRD4 Degrader-41 is a potent BRD4 PROTAC degrader with anti-cancer activity .
|
-
- HY-180152
-
|
|
Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 ligand 14 (Compound Y47) is a BRD4 inhibitor. BRD4 ligand 14 exhibits mild anticancer properties against acute myeloid leukemia by inhibiting BRD4. BRD4 ligand 14 can also be used as a ligand for target protein for PROTAC in the development and design of PROTAC BRD4 degraders, such as PROTAC BRD4 Degrader-42 (HY-180150) .
|
-
- HY-176450
-
|
|
|
Cancer
|
|
4-Aminobutyl 4-methylbenzenesulfonate is a PROTAC linker. 4-Aminobutyl 4-methylbenzenesulfonate can be used to synthesize PROTACs, such as PROTAC BRD4 Degrader-32 (HY-176449) .
|
-
- HY-180153
-
|
|
PROTAC Linkers
|
Cancer
|
|
Piperidine-CO-C8-COOH is a PROTAC linker. Piperidine-CO-C8-COOH can be used to synthesize PROTAC BRD4 Degrader-42 (HY-180150) .
|
-
- HY-181496
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
(S)-JQ-35-Boc is a BRD4 ligand. (S)-JQ-35-Boc can be used to synthesize BRD4 degrader RAJQ14 (HY-181495). RAJQ14 can be used for cancer research .
|
-
- HY-W288798
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
DCAF11 ligand 2 is an E3 ligase ligand that can be used in the recruitment of DCAF11. DCAF11 ligand 2 can be connected to the BRD4 ligand (HY-78695) by a linker to synthesis of PROTAC BRD4 degrader LGF308 (HY-181756) .
|
-
- HY-182979
-
|
|
HSP
|
Cancer
|
|
HSP70 ligand 2 is an HSP70 ligand and serves as a ligand for PROTAC target proteins. HSP70 ligand 2 can be used to synthesize Hsp70TAC BRD4 Degrader-1 (HY-182958) and Hsp70TAC PD-1 Degrader-2 (HY-182959) .
|
-
- HY-W879795
-
|
|
Ligands for E3 Ligase
|
Others
|
|
NH2-MeO-Ph-amide-(2,6-Dioxo-3-Pip) is a CRBN ligand. NH2-MeO-Ph-amide-(2,6-Dioxo-3-Pip) can be used to synthesize PROTAC BRD4 Degrader-22 (HY-155393) .
|
-
- HY-114407
-
|
|
PROTACs
Epigenetic Reader Domain
|
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 .
|
-
- HY-42429
-
-
- HY-169358
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
L134 is a potent PROTAC BRD4 degrader with a DC50 value of 7.36 nM. L134 mediates the degradation of BRD4 via the ubiquitin-proteasome system in a DCAF11-dependent manner (Blue: JQ-1 (carboxylic acid) (HY-78695), Black: linker (HY-W004640); Pink: E3 ligase ligand, L321 (HY-169359)) .
|
-
- HY-182912
-
|
|
Molecular Glues
Epigenetic Reader Domain
|
Cancer
|
|
PLX-4104 is an orally active BRD4 molecular glue degrader with a DC50 of 2 nM. PLX-4104 selectively promotes BRD4 degradation via DCAF11 recruitment, triggering ubiquitination and proteasomal breakdown. PLX-4104 inhibits cancer cell proliferation. PLX-4104 induces complete regression of AML xenograft tumors. PLX-4104 can be used for the research of acute myeloid leukemia .
|
-
- HY-161652
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C3-O-Ph(NO2)-methylester-O-pyrrolidine-2,5-dione is the conjugate of a linker and a ligand for E3 ligase. Thalidomide-NH-C3-O-Ph(NO2)-methylester-O-pyrrolidine-2,5-dione can be used for synthesis of PROTAC BRD4 Degrader-26 (HY-161650) .
|
-
- HY-P11640
-
|
|
Ligands for E3 Ligase
HIV
|
Infection
|
|
Vpr (1-14) is a viral protein R and acts as an accessory protein of HIV-1. Vpr (1-14) can binds to Cul4A-DDB1-DCAF1 E3 ligase complex and can be used as an E3 ligase-binding component in PROTACs. Vpr (1-14) can be used to synthesize PROTAC BRD4 Degrader-43 (HY-181164) .
|
-
- HY-138634
-
|
|
Drug-Linker Conjugates for ADC
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
GNE-987 GSH linker-2 is a drug-linker conjugates for ADC. GNE-987 GSH linker-2 is a conjugation of PROTAC GNE-987 (HY-129937A) and ADC linker GSH linker-2 (HY-182740), and can be used to prepare antibody-drug conjugates (ADC) for BRD4 degradation. GNE-987 GSH linker-2 can be used for the research of cancer .
|
-
- HY-176726
-
|
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
ZnPc-amide-PEG3-C2-NH2 is a photosensitizer-linker conjugate which consists of ZnPcPs (HY-176725) and a linker (HY-W040165). ZnPc-amide-PEG3-C2-NH2 can be used to synthesize the photo-activated BRD4 degrader pZnPc-O3-JQ1 (HY-176724) .
|
-
- HY-181756
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
LGF308 is a PROTAC degrader of BRD4 that exhibits selective cytotoxicity toward cancer cells over normal cells. LGF308 mediates the formation of a ternary complex between BRD4 and DCAF11 to achieve BRD4 degradation. LGF308 induces tumor cell apoptosis by upregulating apoptosis-related proteins. LGF308 inhibits tumor cell proliferation and migration in breast cancer and triple-negative breast cancer cell lines. LGF308 can be used for the research of breast cancer .
|
-
- HY-129937A
-
GNE-987
1 Publications Verification
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
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 .
|
-
- HY-176071
-
|
|
ByeTAC
Epigenetic Reader Domain
|
Cancer
|
|
TEC 4 is a ByeTAC (Bypassing E-Ligase-Targeting Chimera) BRD4 degrader, with 33% BRD4 remaining at 500 nM in Ramos B-cells. TEC 4 shows toxicity for Ramos B-cells, with an IC50 of 30.5 nM. ByeTACs directly recruits a protein to the proteasome via interactions with Rpn-13 for degradation. Pink: BRD4 lignad (HY-78695); Blue: Rpn-13 ligand (HY-159808); Black: linker (HY-W008352) .
|
-
- HY-175611
-
-
- HY-183061
-
|
|
LYTACs
Epigenetic Reader Domain
|
Neurological Disease
Cancer
|
|
MrTAC-8, methylarginine-targeting chimera (MrTAC), is a BRD4 degrader with DC50 values of 46 nM in HeLa cells. MrTAC-8 recruits PRMT1, PRMT3, PRMT4, PRMT5, and PRMT7 to target proteins, inducing arginine methylation that triggers lysosomal degradation. MrTAC-8 degrades proteins across diverse subcellular localizations and independent of native proteolytic routes. MrTAC-8 can be used for the research of cervical cancer, glioblastoma .
|
-
- HY-132941
-
|
|
PROTACs
Epigenetic Reader Domain
c-Myc
Apoptosis
|
Cancer
|
|
CFT-2718 is a selective CRBN-dependent BRD4 PROTAC degrader. CFT-2718 mediates rapid, selective BRD4 degradation, reduces total and phosphorylated Ser2 RPB1 levels, and reduces MYC protein levels. CFT-2718 can inhibit cancer cells proliferation and induce apoptosis. CFT-2718 reduces growth of lung cancer and pancreatic patient-derived xenograft models. CFT-2718 can be used for the research of cancer, such as small-cell lung cancer and pancreatic cancer .
|
-
- HY-133139
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-W877997
-
|
|
E3 Ligase Ligand-Linker Conjugates
Drug Derivative
|
Cancer
|
|
Pomalidomide 5'-pip-acid is an E3 ligase ligand-linker conjugate derived from the molecular glue Pomalidomide (HY-10984), which can be used to synthesize the dual-target PROTAC degrader PROTAC CBP/p300/BRD4 Degrader-1 (HY-181758) targeting CBP/p300 and BRD4. Pomalidomide 5'-pip-acid shows anti-proliferative activity against cancer cells with an IC50 of 2.73 nM. Pomalidomide 5'-pip-acid induces anti-proliferative effects in cancer cells. Pomalidomide 5'-pip-acid is applicable to research related to prostate cancer and colorectal cancer .
|
-
- HY-130984
-
|
|
PROTAC Linkers
|
Cancer
|
|
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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-133138
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-176724
-
|
|
Epigenetic Reader Domain
Reactive Oxygen Species (ROS)
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
ZnPc-O3-JQ1 is a light-triggered BRD4 degrader. Under illumination, ZnPc-O3-JQ1 generates reactive oxygen species (ROS) that degrades BRD4. The degradation of BRD4 results in downregulation of HIF-1α, thereby counteracting the photodynamic therapy (PDT) resistance induced by tumor hypoxia. ZnPc-O3-JQ1 exhibits both Type I and Type II PDT mechanisms. The structure of ZnPc-O3-JQ1 consists of three parts: BRD4 ligand (HY-78695); Linker (HY-W040165); Photosensitizer (HY-176725) .
|
-
- HY-108369R
-
|
|
Reference Standards
PROTAC Linkers
|
Cancer
|
|
Azido-PEG1-CH2CO2H (Standard) is the analytical standard of Azido-PEG1-CH2CO2H (HY-108369). This product is intended for research and analytical applications. 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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P11640
-
|
|
Ligands for E3 Ligase
HIV
|
Infection
|
|
Vpr (1-14) is a viral protein R and acts as an accessory protein of HIV-1. Vpr (1-14) can binds to Cul4A-DDB1-DCAF1 E3 ligase complex and can be used as an E3 ligase-binding component in PROTACs. Vpr (1-14) can be used to synthesize PROTAC BRD4 Degrader-43 (HY-181164) .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-133736
-
|
|
|
Azide
PROTAC Synthesis
|
|
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 .
|
-
- HY-136857
-
|
|
|
PROTAC Synthesis
|
|
BRD4 degrader-3 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-133139
-
|
|
|
PROTAC Synthesis
Azide
|
|
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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-133138
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PROTAC Synthesis
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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-130984
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PROTAC Synthesis
Azide
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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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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