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Results for "

palmitoylation pocket

" in MedChemExpress (MCE) Product Catalog:

4

Inhibitors & Agonists

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-155338

    YAP Cancer
    SWTX-143 is an orally active YAP/TAZ-TEAD inhibitor that binds to the palmitoylation pocket of all four TEAD isoforms. SWTX-143 causes irreversible and specific inhibition of the transcriptional activity of YAP/TAZ-TEAD and shows antitumor activity .
    SWTX-143
  • HY-147209

    YAP Metabolic Disease
    DC-TEAD3in03 is a subtype-selective and covalent TEAD3 inhibitor with an IC50 of 0.16 μM. DC-TEAD3in03 exhibits the inhibitory activity on TEAD1/2/4 reduced by more than 100 times. DC-TEAD3in03 has the IC50 for TEAD3 of 1.15 μM in the GAL4-TEAD reporter gene experiment in cells, and it does not interfere with the β-catenin pathway. DC-TEAD3in03 reduces the growth rate of the zebrafish tail fin. DC-TEAD3in03 can be used to study the proportional growth of appendages in vertebrates .
    DC-TEAD3in03
  • HY-181534

    PROTACs YAP IAP SNIPERs Cancer
    PROTAC TEAD1/IAP degrader-1 (Compound A232) is a selective TEAD1 and cIAP1 PROTAC degrader, with DC50 values of 14 nM and 270 nM, respectively. PROTAC TEAD1/IAP degrader-1 promotes the ubiquitination and degradation of TEAD1 and cIAP1. PROTAC TEAD1/IAP degrader-1 downregulates the expression of the TEAD-dependent gene CTGF. PROTAC TEAD1/IAP degrader-1 exhibits anticancer activity against mesothelioma .
    PROTAC TEAD1/IAP degrader-1
  • HY-181607

    YAP Others
    TEAD ligand-Linker Conjugate 3 (the blue structure + black structure of A536 in the literature) is a conjugate of a TEAD1-targeting ligand and a linker. TEAD ligand-Linker Conjugate 3 can be coupled with an IAP ligand (HY-181531) to form an IAP-recruiting bifunctional protein degrader (IPD) (HY-181594), also known as a SNIPER degrader. This TEAD SNIPER simultaneously binds to the TEAD1 palmitoylation pocket and the BIR3 domain of cIAP1 to form a ternary complex, efficiently inducing the ubiquitination and degradation of both TEAD1 and cIAP1 (DC50=110 nM, Dmax=51%; IC50=122 nM for cIAP1). TEAD ligand-Linker Conjugate 3 and its synthesized SENIPER molecule can be utilized in research on Hippo pathway dysregulation-related diseases, such as NF2-mutant tumors .
    TEAD ligand-Linker Conjugate 3

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