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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
32 Results for "
VHL-recruiting PROTAC
" in MedChemExpress (MCE) Product Catalog:
Products (32)
32 Results for "VHL-recruiting PROTAC" in MCE Product Catalog:
3
3 Cited Publications
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ARCC-4 is a low-nanomolar Androgen Receptor (AR) degrader based on PROTAC, with a DC50 of 5?nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy .
Cat. No.: HY-168016
CAS No.: 3058483-58-9
PROTAC YAP degrader-1 is a VHL-recruiting PROTAC degrader (DC50=8.2 μM) and antiproliferative agent that targets YAP. PROTAC YAP degrader-1 recruits the E3 ligase VHL and binds to VHL to form a ternary complex containing YAP. PROTAC YAP degrader-1 inhibits the nuclear localization of YAP in cancer cells, reduces YAP/TEAD-mediated transcription, and induces TAZ protein degradation. PROTAC YAP degrader-1 reduces the oncogenic activity of YAP and exerts antiproliferative effects in the Huh7 xenograft mouse model. PROTAC YAP degrader-1 can be used for the research of hepatocellular carcinoma and mesothelioma .
Cat. No.: HY-162362
CAS No.: 3060730-06-2
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MS8709 is a PROTAC degrader that induces the degradation of G9a (EHMT2)/GLP (EHMT1) by recruiting VHL. MS8709 induces G9a/GLP protein degradation via a mechanism that simultaneously depends on G9a/GLP target protein binding, VHL recruitment, and the ubiquitin-proteasome system (UPS), while the mRNA levels of G9a and GLP do not show significant changes, indicating that the effect occurs primarily at the protein level rather than the transcriptional level. MS8709 retains the inhibitory effect on G9a/GLP methyltransferase activity and reduces H3K9me2 levels, thereby simultaneously affecting the catalytic and non-catalytic functions of G9a/GLP. MS8709 can be used for studies related to G9a/GLP biology, prostate cancer, lung cancer, and other relevant fields .
MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 also degrades CRAF. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma .
Cat. No.: HY-143883
CAS No.: 2376137-41-4
MS143 is a VHL-recruiting AKT protein PROTAC degrader with a DC50 of 46 nM in PC3 prostate cancer cells. MS143 preferentially binds to AKT1 and AKT3, with weaker binding activity towards AKT2. MS143 degrades AKT and blocks the phosphorylation of downstream signaling molecules in the PI3K/AKT/mTOR pathway. MS143 inhibits cancer cell growth and xenograft tumor growth. MS143 can be used for research on prostate cancer, triple-negative breast cancer, and breast cancer .
Cat. No.: HY-175358
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PROTAC USP7 Degrader-1 is a VHL-recruiting PROTAC and USP7 degrader with binding activity to both USP7 and the VHL E3 ubiquitin ligase. PROTAC USP7 Degrader-1 recruits the VHL E3 ligase to mediate the ubiquitination and subsequent proteolytic degradation of USP7 .
Cat. No.: HY-175025
CH091138 is an orally active VHL-recruiting PROTAC degrader targeting KRAS G12D, with a DC50 of 148.3 nM in HeLa cells. CH091138 inhibits cancer cell proliferation and tumor growth by mediating the ubiquitin-proteasome degradation of KRAS G12D. CH091138 can be used in research related to pancreatic cancer and colorectal cancer .
Cat. No.: HY-160694
CAS No.: 2417369-73-2
Synonyms: cBu-Cit-PROTAC BRD4 Degrader-5
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cBu-Cit-GAL-02-221 (cBu-Cit-PROTAC BRD4 Degrader-5) is a BRD4 PROTAC-linker conjugate with a protease-cleavable cBu-Cit linker. cBu-Cit-GAL-02-221 can be conjugated with antibodies to form PACs, and releases a VHL-recruiting BRD4 degrader inside cells. cBu-Cit-GAL-02-221 is applicable to studies on BRD4-targeted degradation, antibody-mediated PROTAC delivery and PAC construction .
Cat. No.: HY-155506
PROTAC NAMPT Degrader-32 is a PROTAC degrader targeting NAMPT with an IC50 of 2.14 nM. PROTAC NAMPT Degrader-32 induces proteasome-dependent degradation of NAMPT and induces apoptosis in ovarian cancer cells (apoptosis). PROTAC NAMPT Degrader-32 can be used in research related to ovarian cancer .
Cat. No.: HY-163152
CAS No.: 2378051-80-8
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PROTAC BRM degrader-1 is a VHL-recruiting PROTAC degrader that exhibits higher selectivity for the degradation of SMARCA2 (BRM) over its highly homologous protein SMARCA4 (BRG1). The KD values of PROTAC BRM degrader-1 for BRM and BRG1 are 72 nM and 108 nM, respectively. PROTAC BRM degrader-1 can be used in studies related to selective SMARCA2 degradation, SWI/SNF function, and SMARCA4-mutant non-small cell lung cancer .
Cat. No.: HY-173422
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MS2133 is a VHL-recruiting DOT1L PROTAC degrader. MS2133 possesses antiproliferative activity with a human DOT1L IC50 of 4.6 nM, forms a ternary complex with DOT1L and VHL E3 ligase to drive DOT1L ubiquitination and subsequent proteasomal degradation without affecting DOT1L mRNA transcription, inhibits the proliferation of mixed lineage leukemia-rearranged leukemia cells and downregulates H3K79Me2, restrains proliferation of both tumor and normal cells but lacks cytotoxicity against normal cells, and can be used for the research of mixed lineage leukemia-rearranged leukemia .
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PROTAC BRD4 Degrader linker conjugate-3 is a VHL-recruiting PROTAC that targets and degrades BRD4. It can be used in studies related to prostate cancer .
Cat. No.: HY-135558
CAS No.: 2313234-00-1
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PROTAC BRD4 Degrader-3 is a VHL-recruiting PROTAC degrader that targets BRD4. PROTAC BRD4 Degrader-3 consists of a VHL E3 ubiquitin ligase ligand and a BRD4 inhibitor linked by a connector .
Cat. No.: HY-174920
CAS No.: 1797406-70-2
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PROTAC BRD4 Degrader-34 (1797406-70-2) is a VHL-recruiting PROTAC BRD4 degrader. PROTAC BRD4 Degrader-34 induces degradation of the short isoform of BRD4 and can be used in studies of BRD4-related diseases and targeted protein degradation .
Cat. No.: HY-174453
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PROTAC ERα Degrader-12 is a VHL-recruiting ERα PROTAC degrader with a DC50 of 1.02 μM in MCF-7 cells. PROTAC ERα Degrader-12 binds to ERα and recruits the VHL E3 ligase to form a ternary complex, promoting proteasomal degradation of both wild-type and mutant ERα, thereby inhibiting ER-mediated transcriptional activity and breast cancer cell proliferation. PROTAC ERα Degrader-12 can be used in the research of ERα-positive breast cancer .
Cat. No.: HY-170828
CAS No.: 3033586-04-5
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SMD-1087 is a VHL-recruiting SMARCA2 PROTAC degrader with a DC50 of 8 nM. SMD-1087 induces ubiquitination and degradation of SMARCA2 via the proteasome pathway. SMD-1087 reduces PBRM1 protein levels, inhibits the growth of SMARCA4-deficient cancer cells, and suppresses tumor growth in mouse xenograft models. SMD-1087 can be used for research on SMARCA4-deficient human cancers, including lung cancer and melanoma .
Cat. No.: HY-174981
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LC-MF-4 is an orally active VHL-recruiting FGFR3 PROTAC degrader and hERG potassium channel inhibitor. LC-MF-4 has an IC50 of 16.6 nM against human FGFR3, exhibits inhibitory activity against hERG potassium channels, suppresses the expression of genes related to mitochondrial biogenesis and ATP synthesis, inhibits cancer cell proliferation, and shows significant antitumor activity in mice. LC-MF-4 can be used in the research of bladder cancer, urothelial carcinoma, FGFR3 Y373C mutant cancers, and FGFR3-TACC3 fusion-positive cancers .
Cat. No.: HY-44630
CAS No.: 2172819-75-7
Synonyms: (S,R,S)-AHPC-CO-C6-COOH
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VH 032 amide-alkylC6-acid ((S,R,S)-AHPC-CO-C6-COOH) is a VH032 analog that acts as a ligand for VHL, recruiting von Hippel-Lindau (VHL) protein. VH 032 amide-alkylC6-acid can be used in the synthesis of PROTACs .
Cat. No.: HY-174469
CAS No.: 3070438-79-5
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PROTACs Apoptosis PI3K Akt Bcl-2 Family P-glycoprotein Reactive Oxygen Species (ROS) Na+/K+ ATPase
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PROTAC PI3K/110β degrader-2 is a VHL-recruiting PI3K/110β PROTAC degrader, with DC50 values of 1.258 μM and 2.185 μM in MCF-7/ADM and A549/DDP cells, respectively. PROTAC PI3K/110β degrader-2 induces proteasomal degradation of PI3K/110β, inhibits phosphorylation of AKT and expression of Bcl-2, while suppressing the activity and expression of P-gp. It also induces endoplasmic reticulum stress and mitochondrial apoptosis via the PERK/CHOP pathway. PROTAC PI3K/110β degrader-2 exerts anti-tumor activity against multidrug-resistant cancer cells both in vitro and in vivo, and produces a synergistic effect when combined with Doxorubicin (HY-15142A) or Cisplatin (HY-17394), making it applicable for the research of multidrug-resistant cancers .
Cat. No.: HY-180907
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PROTAC USP39 Degrader-1 is a USP39 PROTAC degrader with Kd values of 136 nM and 232 nM, and a DC50 value of 1.06 nM (24 h). PROTAC USP39 Degrader-1 binds to the VHL E3 ubiquitin ligase, forms a ternary complex with USP39, mediates USP39 ubiquitination and proteasomal degradation dependent on VHL recruitment, modulates splicing activity and induces 5' splice site-specific splicing patterns. PROTAC USP39 Degrader-1 can be used in the research of cervical 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
