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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
69 Results for "
BET degrader
" in MedChemExpress (MCE) Product Catalog:
Products (69)
69 Results for "BET degrader" in MCE Product Catalog:
9
9 Publications Verification
Cat. No.: HY-78695
CAS No.: 202592-23-2
Target:
Epigenetic Reader Domain PD-1/PD-L1 Ligands for Target Protein for PROTAC Androgen Receptor Ligands for E3 Ligase
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JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4.
2
2 Cited Publications
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PROTAC BET Degrader-1 is a BRD2/BRD3/BRD4 PROTAC degrader. PROTAC BET Degrader-1 inhibits the growth of acute leukemia cells. PROTAC BET Degrader-1 is applicable to the research of acute leukemia .
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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PROTAC BET degrader-2 is a BET PROTAC degrader. PROTAC BET degrader-2 induces dose-dependent degradation of BRD2, BRD3 and BRD4 proteins in leukemia cells. PROTAC BET degrader-2 inhibits the growth of acute leukemia cells. PROTAC BET degrader-2 can be used for the research of acute leukemia .
2
2 Cited Publications
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BETd-246 is a BRD2/3/4 PROTAC degrader targeting the BET family. BETd-246 induces ubiquitination and proteasomal degradation of BRD2, BRD3 and BRD4 by recruiting the CUL4-RBX1-DDB1-CRBN E3 ubiquitin ligase complex; it also inhibits TRAT1 expression and depletes BET proteins. BETd-246 suppresses cancer cell proliferation and invasion, disrupts the cell cycle and induces apoptosis. BETd-246 is applicable to research related to triple-negative breast cancer and T-cell acute lymphoblastic leukemia .
1
1 Cited Publications
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SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC50=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity .
1
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 .
1
1
1 Cited Publications
Cat. No.: HY-114229
CAS No.: 3031993-61-7
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PROTAC BET Degrader-3 (Example C-55) is a BET PROTAC degrader and can be used in cancer research .
Synonyms: VHL ligand 2; E3 ligase Ligand 1A
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(S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
Cat. No.: HY-42424
CAS No.: 1948273-03-7
Synonyms: VHL ligand 2 hydrochloride; E3 ligase Ligand 1
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(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
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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 .
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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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PROTAC BET Degrader-12 (Compound 8b) is a PROTAC degrader for bromodomain and extra-terminal domain (BET)-containing proteins, which degrades the BRD3 and BRD4 in a DCAF11-dependent manner. PROTAC BET Degrader-12 inhibits cell viability of KBM7 with a DC50 of 305.2 nM
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GNE-987 GSH linker-1, a PROTAC-linker Conjugate for PAC, comprises the chimeric BET degrader GNE-987 (HY-129937A) and disulfide-containing linker. GNE-987 GSH linker-1 remains inactive as a degrader until intracellular release of GNE-987 via disulfide reduction and linker self-immolation. GNE-987 GSH linker-1 can be used for the research of acute myeloid leukemia .
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OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively .
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Thalidomide-4-O-C6-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12 F36V and BET .
Cat. No.: HY-147046
CAS No.: 2421153-77-5
Research Areas:
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).
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Lenalidomide-I (Compound 72), an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570 (HY-112609) .
Cat. No.: HY-W008425
CAS No.: 10160-24-4
Synonyms: 7-Bromoheptan-1-ol
Research Areas:
7-Bromo-1-heptanol (7-Bromoheptan-1-ol) acts as a HaloTag-GPSM2 inhibitor and an organic synthesis intermediate. It forms a covalent irreversible bond with HaloTag-GPSM2, thereby blocking the subsequent labeling effect of fluorescent HaloTag ligands and enabling pulse-chase analysis of protein turnover. 7-Bromo-1-heptanol can be used to synthesize PROTAC BET degraders and multivalent glycoporphyrin antiviral compounds. It is applicable to cancer-related research .
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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
