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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
88 Results for "
BET PROTAC
" in MedChemExpress (MCE) Product Catalog:
Products (88)
88 Results for "BET PROTAC" in MCE Product Catalog:
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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 .
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).
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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) .
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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-W008425
CAS No.: 10160-24-4
Synonyms: 7-Bromoheptan-1-ol
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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 .
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-42424A
CAS No.: 2504950-56-3
Synonyms: VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride
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(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) 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 dihydrochloride 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-175678
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PROTAC BRD2 BD1 Degrader-1 is a potent and selective BRD2 BD1 PROTAC degrader, with a DC50 of 65 nM, an EC50 of 423 nM, and a Kd of 69 nM against BRD2 BD1. PROTAC BRD2 BD1 Degrader-1 induces the formation of a ternary complex between the BET bromodomain and the VHL E3 ubiquitin ligase complex, triggering VCB-dependent degradation of the target bromodomain. PROTAC BRD2 BD1 Degrader-1 can be used in cancer research .
Cat. No.: HY-161346
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EBET-1055 is a bromodomain and extra-terminal (BET) PROTAC degrader. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures .
Cat. No.: HY-161346A
CAS No.: 3031540-65-2
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(Rac)-EBET-1055 is the racemate of EBET-1055 (HY-161346). EBET-1055 is a bromodomain and extra-terminal (BET) PROTAC degrader. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures .
Cat. No.: HY-130813
CAS No.: 2570470-39-0
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BET-IN-6 is a BET inhibitor. BET-IN-6 can be used as a Ligand for Target Protein for PROTAC for the synthesis of BRD2/BRD4 PROTAC degraders, such as PROTAC BRD2/BRD4 degrader-1 (HY-130612). BET-IN-6 can be used for cancer research .
Cat. No.: HY-175354
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PROTAC BET Degrader-13 is a BET PROTAC degrader that recruits TRIM21. PROTAC BET Degrader-13 utilizes wild-type TRIM21 to mediate the degradation of PML-eGFP-BRD4 (BD2) fusion protein aggregates, with an EC50 of 1.4 μM in A549 cells expressing TRIM21-FLAG. PROTAC BET Degrader-13 can be used for research on targeted protein degradation and protein aggregate clearance .
Synonyms: VHL ligand 6
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VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC .
Cat. No.: HY-130612
CAS No.: 2570470-42-5
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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. PROTAC BRD2/BRD4 degrader-1 effectively inhibits solid tumors with low cytotoxic effect .
Cat. No.: HY-170900
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SJ44236 is a BET PROTAC degrader with activity against BRD2, BRD3 and BRD4 (DC50 = 127 pM). SJ44236 induces ubiquitination and proteasomal degradation by forming a ternary complex with BET proteins and CRBN-DDB1. SJ44236 downregulates c-Myc, upregulates p53 and reduces cancer cell viability. SJ44236 can be used for the research of leukemia and medulloblastoma .
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ZEN-3862 is a BET inhibitor with IC50s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively. ZEN-3862 can be used to form PROTACs to induce degradation of BRD4 .
Cat. No.: HY-78695A
CAS No.: 202592-24-3
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(R)-JQ-1 carboxylic acid, is an isomer of JQ-1 carboxylic acid (HY-78695). 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.
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ZEN-3219 is a BET inhibitor with IC50s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4 .
Cat. No.: HY-111979
CAS No.: 1952264-36-6
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ZEN-3411 is a BET inhibitor with IC50s of 0.05, 0.05 and 0.06 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTACs to induce degradation of BRD4 .
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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
