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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:
Research Areas:
(S,R,S)-AHPC-C10-NHBoc is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC (HY-125845) based VHL ligand and a linker used for BET-Targeted PROTAC .
Cat. No.: HY-168646
Target:
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SJ46411-Br is one of CRL2 KLHDC2 targeting Ligands for E3 Ligase. SJ46411-Br can bind to KLHDC2 to form a complex to promote cooperative homologous selective ternary complex formation. SJ46411-Br can be coupled to BET ligand JQ1 (HY-13030) through PROTAC linker to synthesize corresponding PROTACs .
Cat. No.: HY-129941
CAS No.: 2341796-74-3
Synonyms: VH032-C10-NH2
Research Areas:
(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for BET-Targeted PROTAC .
Cat. No.: HY-159077
Target:
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H2N-C6-NH-CO-CH2-O-Ph-CH2-NH-Boc is a linker. H2N-C6-NH-CO-CH2-O-Ph-CH2-NH-Boc can be utilized for synthesis of PROTAC BET Degrader-12 (HY-158764) .
Research Areas:
Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc can be used for the synthesis of PROTAC BET degrader . (From patent WO2017180417A1 compound s7).
Cat. No.: HY-153414
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GXF-111 is a BRD3 and BRD4-L PROTAC degrader. Its BD1 and BD2 Ki values against human BRD3 are 11.97 nM and 2.45 nM, respectively. The degradation activity of GXF-111 depends on its binding to BET proteins and Cereblon, as well as the involvement of a functional proteasome. The degradation selectivity of GXF-111 is mainly determined by differences in degradation kinetics and cell types. GXF-111 induces G1 phase cell cycle arrest, downregulates c-Myc expression, upregulates p21 expression, and exhibits antiproliferative activity against a variety of cancer cell lines. GXF-111 can serve as a research tool for cancer-related studies .
Cat. No.: HY-157749
Research Areas:
Thalidomide-piperazine-(S)-CH2-Pyrrolidine-C2-O-CH2-COO-C (CH3)3 is a synthetic E3 ligase ligand-Linker conjugate. Thalidomide-piperazine-(S)-Ch2-Pyrrolidine-C2-O-CH2-COO-C(CH3)3 includes Thalidomide-based cereblon ligands and linkers. Thalidomide-piperazine-(S)-CH2-Pyrrolidine-C2-O-CH2-COO-C(CH3)3 can be used to synthesize PROTAC BET .
Cat. No.: HY-107443R
CAS No.: 1300019-38-8
Synonyms: Molibresib carboxylic acid (Standard); GSK525762A carboxylic acid (Standard); PROTAC BRD4-binding moiety 2 (Standard)
Research Areas:
I-BET762 carboxylic acid (Standard) is the analytical standard of I-BET762 carboxylic acid (HY-107443). This product is intended for research and analytical applications. I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1 .
Cat. No.: HY-107443AR
CAS No.: 1786401-70-4
Synonyms: (R)-Molibresib carboxylic acid (Standard); (R)-GSK525762A carboxylic acid (Standard); (R)-PROTAC BRD4-binding moiety 2 (Standard)
Research Areas:
(R)-I-BET762 carboxylic acid (Standard) is the analytical standard of (R)-I-BET762 carboxylic acid (HY-107443A). This product is intended for research and analytical applications. (R)-I-BET762 carboxylic acid, the R-enantiomer of I-BET762 carboxylic acid (HY-107443). I-BET762 carboxylic acid is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid is a BRD4 inhibitor with a pIC50 value of 5.1 .
Cat. No.: HY-L129
128 compounds
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.
MCE carefully prepared a unique collection of 128 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.
Cat. No.: HY-175790
CAS No.: 2493425-86-6
Research Areas:
AR/BET ligand-1 is a AR/BET ligand, which can be used for the synthesis of PROTACs, such as PROTAC AR/BET protein degrader-1 (HY-160262) .
Cat. No.: HY-181735
Research Areas:
BET-IN-30 (Compound 11d) is a BTE family protein inhibitor, which can act as a BRD2/BRD3/BRD4 target protein ligand and be used for the synthesis of PROTACs, such as PROTAC BET Degrader-15 (HY-181729). BET-IN-30 exhibits potent anti-proliferative activity against acute myeloid leukemia (AML) cells such as MV4-11. BET-IN-30 can be used for the study of AML .
Cat. No.: HY-181736
CAS No.: 2461559-77-1
Research Areas:
Pomalidomide-C2-piperazine-Boc is an E3 ligase ligand-linker conjugate that can be used to synthesize PROTACs, such as PROTAC BET Degrader-15 (HY-181729).
Cat. No.: HY-175791
CAS No.: 2703756-19-6
Research Areas:
Ethyl-Cha-thalidomide-NH2 is a conjugate of an E3 ligase and a linker, which can be used for the synthesis of PROTACs, such as PROTAC AR/BET protein degrader-1 (HY-160262) .
Cat. No.: HY-177244
CAS No.: 3031540-97-0
Research Areas:
EBET-1593 is a BET PROTAC degrader. EBET-1593 can promote the ubiquitination and degradation of BET. EBET-1593 is a lead payload. EBET-1593 can be used to synthesize ADCs, such as 84-EBET. 84-EBET has antitumor effects against pancreatic ductal adenocarcinoma .
Cat. No.: HY-161387A
CAS No.: 3031540-02-7
Research Areas:
(Rac)-EBET-590 is the racemate of EBET-590 (HY-161387). (Rac)-EBET-590 is a BET ligand. (Rac)-EBET-590 can serve as a ligand for the target protein in the synthesis of PROTAC BET degraders, such as (Rac)-EBET-1055 (HY-161346A). (Rac)-EBET-590 is suitable for cancer research .
Cat. No.: HY-181868
CAS No.: 1957236-16-6
Research Areas:
Lenalidomide-CO-C7-NH2 is a CRBN-dependent intermediate of BET PROTAC degrader. Consisting of the E3 ubiquitin ligase ligand Lenalidomide (HY-A0003) conjugated with a PROTAC linker, Lenalidomide-CO-C7-NH2 induces the protein degradation. By depleting BRD4, PROTAC BET Degrader-16 effectively inhibits cancer cell proliferation, induces cell cycle arrest and promotes apoptosis, thereby exhibiting significant anti-tumor activity in xenograft models. Lenalidomide-CO-C7-NH2 serves as an important tool molecule for the study of acute myeloid leukemia .
Cat. No.: HY-182577
CAS No.: 2154350-81-7
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CFT-743, a PROTAC-based heterobifunctional degrader and BET inhibtor, is a degrader of BRD4 bromodomain 1 (BD1) with a DC50 of 4.3 nM. CFT-743's antitumor activitiy is dependent on BET degradation and can be attenuated by Pomalidomide (HY-10984), which is a CRBN binding molecule. CFT-743 induces ubiquitination of BRD4 BD1. CFT-743 can be used for cancer research .
Cat. No.: HY-112588R
CAS No.: 1950634-92-0
Research Areas:
dBET6 (Standard) is the analytical standard of dBET6 (HY-112588). This product is intended for research and analytical applications. dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity.
Cat. No.: HY-176336
CAS No.: 1957236-06-4
Research Areas:
Thalidomide-C-amide-C5-amine is an E3 ligase ligand-linker conjugate. Thalidomide-C-amide-C5-amine can be used for synthesis of PROTAC BET Degrader-10 (HY-112718) .
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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
