2488699-00-7
Chemical Structure
PDL1 degrader-3
- CAS. Nr.: 2488699-00-7
- Formula:C16H12N2O2
- Molecular Weight:264.28
InChIKey: VVESARTXPSODKZ-UHFFFAOYSA-N
SMILES: COC1=C(C=C(C2=C1)C=NC3=C2C(C#N)=CC=C3)OC
Biological Activity: PDL1 degrader-3 (compound e24) is a DUBTAC-like PD-L1 degrader. PDL1 degrader-3 inhibits CSN5 enzymatic activity, increases PD-L1 ubiquitination, and induces PD-L1 degradation via the ubiquitin-proteasome pathway, reducing PD-L1 expression on tumor cell membranes. PDL1 degrader-3 blocks PD-1/PD-L1 interaction, activates the tumor immune microenvironment, enhances tumor-infiltrating T-cell immunity, and inhibits activation of immunosuppressive MDSCs and Tregs. PDL1 degrader-3 exerts antitumor effects in mouse tumor models. PDL1 degrader-3 can be used for the research of colorectal cancer, lung cancer[1].
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PDL1 degrader-3 | PDL1 degrader-3 (compound e24) is a DUBTAC-like PD-L1 degrader. PDL1 degrader-3 inhibits CSN5 enzymatic activity, increases PD-L1 ubiquitination, and induces PD-L1 degradation via the ubiquitin-proteasome pathway, reducing PD-L1 expression on tumor cell membranes. PDL1 degrader-3 blocks PD-1/PD-L1 interaction, activates the tumor immune microenvironment, enhances tumor-infiltrating T-cell immunity, and inhibits activation of immunosuppressive MDSCs and Tregs. PDL1 degrader-3 exerts antitumor effects in mouse tumor models. PDL1 degrader-3 can be used for the research of colorectal cancer, lung cancer. | |||||||||||||||||||||
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Keywords
