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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
12 Results for "
PROTAC Component
" in MedChemExpress (MCE) Product Catalog:
Products (12)
12 Results for "PROTAC Component" in MCE Product Catalog:
Cat. No.: HY-160924
Research Areas:
MS147 is a VHL-based PROTAC degrader of BMI1 and RING1B (polycomb repressive complex 1 core components). MS147 directly binds EED and VHL E3 ligase, recruiting the ligase to the EED-BMI1/RING1B complex to induce time-dependent, ubiquitination-mediated degradation of BMI1 and RING1B. MS147 reduces histone H2A Lys119 mono-ubiquitination without altering histone H3 Lys27 tri-methylation and inhibits cancer cells proliferation. MS147 can be used for the research of cancer, such as chronic myelogenous leukemia and b-cell lymphoma .
Cat. No.: HY-157558
Synonyms: 8SGE
Target:
Research Areas:
KDRLKZ-1 (8SGE) is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 0.36 μM), with an IC50 of 0.21 μM and 0.31 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-1 binds to the substrate-binding pocket of the KLHDC2 kelch domain, mimics the interaction of natural substrates and displaces them. KDRLKZ-1 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-1 can be used in scaffold ligand research for PROTAC degraders targeting KLHDC2 .
Cat. No.: HY-157559
Target:
Research Areas:
KDRLKZ-2 is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 95 nM), with an IC50 of 68 nM and 0.1 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-2 binds to the substrate-binding pocket of the kelch domain of KLHDC2, mimics the interaction of natural substrates and displaces them. KDRLKZ-2 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-2 can be used in scaffold ligand studies of PROTAC degraders targeting KLHDC2 .
Cat. No.: HY-162411
CAS No.: 3038773-47-3
Target:
Research Areas:
E3 ligase Ligand 24 (Compound 24) is a Potent Ligand for the E3 Ligase DCAF15 (IC50= 0.053 μM). Due to E3 ligase Ligand 24’s selectivity and potent binding characteristics, it is pivotal in the study of targeted protein degradation .
Cat. No.: HY-168869
CAS No.: 3104316-29-9
Target:
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Tamoxifen-PEG-Clozapine is a ERα PROTAC degrader. Tamoxifen-PEG-Clozapine induces ubiquitination and degradation of ERα protein. Tamoxifen-PEG-Clozapine mediates ERα degradation by utilizing UBR5 as a component of the ubiquitin-proteasome system. Tamoxifen-PEG-Clozapine exhibits anticancer activity against breast cancer. Tamoxifen-PEG-Clozapine can be used in the research of breast cancer .
Target:
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VHLL-BCN is a ligand targeting the VHL E3 ligase, which can be used for the synthesis of PROTAC molecules. As a key component of the copper-free SPAAC-based rapid synthesis platform for transcription factor PROTACs, VHLL-BCN is applicable to cancer-related research .
Cat. No.: HY-W425461
CAS No.: 1103506-79-1
Research Areas:
c-Met ligand-1 is a c-Met ligand and component of c-Met PROTAC degrader (HY-175320) .
Cat. No.: HY-187349
Research Areas:
E3 Ligase Ligand-linker Conjugate 241 is an E3 ligase ligand-linker conjugate that serves as a component of PROTAC, such as PROTAC NAMPT Degrader-31 (HY-187347). E3 Ligase Ligand-linker Conjugate 241 is applicable to research related to PROTAC synthesis .
Cat. No.: HY-184329
CAS No.: 3114874-73-3
Target:
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PROTAC AURKB Degrader-1 is a selective AURKB PROTAC degrader with a DC50 value of 0.6 nM. PROTAC AURKB Degrader-1 promotes ubiquitination and degradation of AURKB. PROTAC AURKB Degrader-1 downregulates the expression levels of chromosomal passenger complex components Borealin, INCENP, Survivin as well as the transcription factor YY1. PROTAC AURKB Degrader-1 induces G2/M phase arrest and triggers Apoptosis in cells. PROTAC AURKB Degrader-1 serves as a chemical probe for biological studies of the chromosomal passenger complex. PROTAC AURKB Degrader-1 can be used in research related to acute myeloid leukemia, colorectal cancer, and non-small cell lung cancer .
Cat. No.: HY-P11640
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Research Areas:
Cat. No.: HY-183440
CAS No.: 1249297-44-6
Target:
Research Areas:
Amine-C2-piperazine-C4-OH is a flexible alkyl linker component that can be used in the synthesis of PROTAC ALK5 Degrader-1 (HY-183785). Amine-C2-piperazine-C4-OH can be applied to the research of pulmonary fibrosis .
Cat. No.: HY-181413
CAS No.: 3093642-25-9
Research Areas:
PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the EZH2-PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer .
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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
