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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
5 Results for "
CRL2VHL
" in MedChemExpress (MCE) Product Catalog:
Products (5)
5 Results for "CRL2VHL" in MCE Product Catalog:
5
5 Cited Publications
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UNC6852 is a PRC2 PROTAC degrader, with a DC50 value of 0.79 μM for EED (HeLa), 0.3 μM for EZH2 (HeLa), and 0.59 μM for SUZ12 (DLBCL). UNC6852 binds to the WD40 aromatic cage of EED and CRL2-VHL, inducing proteasomal degradation of EED, EZH2 and SUZ12. UNC6852 reduces the level of H3K27me3 and exerts antiproliferative effects in cancer cells. UNC6852 can be used in studies related to diffuse large B-cell lymphoma, triple-negative breast cancer and prostate cancer [2] .
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2 Cited Publications
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VZ185 is a BRD9 and BRD7 PROTAC degrader, with DC50 values of 1.76 nM and 4.5 nM, respectively, in RI-1 cells; and DC50 values of 4 nM and 34 nM, respectively, in HEK293 cells. VZ185 hijacks the CRL2 VHL E3 ubiquitin ligase complex to induce ubiquitination and subsequent proteasomal degradation of BRD9 and BRD7. VZ185 can be used in research related to acute myeloid eosinophilic leukemia and malignant rhabdoid tumors .
Cat. No.: HY-162835
CAS No.: 2409844-88-6
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PROTAC SMARCA2/4 degrader-28 is a heterobifunctional PROTAC degrader targeting SMARCA2 and SMARCA4. PROTAC SMARCA2/4 degrader-28 forms a ternary complex with CRL2VHL E3 ligase and SMARCA2 or SMARCA4, mediating the ubiquitination and degradation of SMARCA2, while acting as a partial degrader of SMARCA4. PROTAC SMARCA2/4-degrader-28 can be used in cancer-related research .
Cat. No.: HY-162834
CAS No.: 2375564-54-6
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PROTAC SMARCA2/4 degrader-27 is a VHL-recruiting PROTAC degrader targeting SMARCA2 and SMARCA4, derived from structure-guided modification of PROTAC SMARCA2/4 degrader-28 (HY-162835). PROTAC SMARCA2/4-degrader-27 forms a cooperative ternary complex with CRL2VHL E3 ligase to induce ubiquitination and degradation. PROTAC SMARCA2/4-degrader-27 induces a novel protein-protein interaction between VHL and SMARCA2/SMARCA4, thereby stabilizing ternary complex formation and promoting proteasomal degradation of target proteins. PROTAC SMARCA2/4-degrader-27 exhibits enhanced cell permeability and stronger ternary complex formation ability, leading to improved degradation activity. PROTAC SMARCA2/4-degrader-27 can be used in cancer-related research[1].
Cat. No.: HY-180787
G6374 is a IRE1 PRORAC degrader with DC50 values of 0.04 μM (AMO1) and 0.13 μM (KMS27), an EC50 value of 0.11 μM, and KD values of 0.56 nM and 90.2 nM for IRE1 and VHL, respectively. G6374 binds to the ATP pocket of the IRE1 kinase domain and VHL to form a ternary complex that recruits CRL2 VHL, inducing K48-linked polyubiquitination of IRE1 at lysine residues K704 and K717, which in turn drives proteasomal degradation of monomeric and dimeric IRE1. G6374 can be used for the research of multiple myeloma .
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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
