PD-1/PD-L1 Degrader
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PDL1 degrader-1
0 ImagesCat. No.: HY-168530PDL1 degrader-1 (compound PMT-O9-1A) is a potent PD-L1 degrader. PDL1 degrader-1 decreases the protein expression of PD-L1. PDL1 degrader-1 shows cytotoxicity. PDL1 degrader-1 shows anticancer activity.
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PDL1 degrader-2
0 ImagesCat. No.: HY-169363Purity: 99.41%PD-L1 degrader-2 (Compound B3) is an orally active AUTAC degrader, that degrades PD-L1 through autophagy-lysosome pathway with a DC50 of 0.5 μM. PD-L1 degrader-2 exhibits inhibitory activity against PD-1/PD-L1 interaction with an IC50 of 22.8 nM. PD-L1 degrader-2 upregulates the expressions of Atg9b, Lamp1 and Mitf, and activates the autophagy lysosome system. PD-L1 degrader- exhibits antitumor efficacy in CT26 mouse model. (Pink: autophagy-lysosome activator (HY-159894); Black: linker (HY-W015088); Blue: PD-L1 ligand (HY-169365))
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PROTAC PD-L1 degrader-2
0 ImagesCat. No.: HY-162972CAS No.: 2995357-09-8PROTAC PD-L1 degrader-2 is a PD-L1 PROTAC degrader with an IC50 of 197.4 nM and a Kd of 301 nM. PROTAC PD-L1 degrader-2 induces PD-L1 endocytosis, drives degradation via the proteasomal and lysosomal pathways, and inhibits the PD-1/PD-L1 interaction. As an immune activator, PROTAC PD-L1 degrader-2 increases the levels of CD4+, CD8+, granzyme B and perforin. PROTAC PD-L1 degrader-2 can be used in studies related to colon cancer immunology.
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MS1-96
0 ImagesCat. No.: HY-179558MS1-96 is an orally active PD-L1 (programmed death-ligand 1) degrader. MS1-96 effectively reduced PD-L1 protein levels across multiple colorectal cancer (CRC) cell lines. MS1-96 directly binds to PD-L1 (KD = 2.58 μM) and enhances the interaction between HIP1R and PD-L1, thereby altering the intracellular trafficking of PD-L1 within clathrin-coated vesicles. MS1-96 induces abnormal N-glycosylation of PD-L1, destabilizing the protein and hastening its lysosome-mediated degradation. MS1-96 can be used for the study of colorectal cancer.
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Hsp70TAC PD-1 Degrader-2
0 ImagesCat. No.: HY-182959Hsp70TAC PD-1 Degrader-2 is a PD-L1 Hsp70TAC (Hsp70-targeting Chimeras) degrader with Kd values of 0.36 μM. Hsp70TAC PD-1 Degrader-2 forms a ternary complex with Hsp70 and PD-L1 to drive PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 induces degradation of mature membrane-bound PD-L1 in an Hsp70-dependent manner and via caveolin-mediated endocytosis and lysosomal trafficking. Hsp70TAC PD-1 Degrader-2 accumulates preferentially in tumor cells with elevated Hsp70 expression for tumor-selective PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 can be used for the research of cancer, such as breast invasive carcinoma, glioblastoma multiforme, diffuse large b-cell lymphoma. (Pink: PD-1/PD-L1 ligand (HY-19745A); Blue: Hsp70 ligand (HY-182979); Black: linker (HY-182982)).
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CSN5-IN-3
0 ImagesCat. No.: HY-181795CSN5-IN-3 (Compound 30) is a CSN5 inhibitor with an IC50 of 0.58 μM. CSN5-IN-3 inhibits the enzymatic activity of CSN5, leading to increased accumulation of NEDD8-Cul1 and promoting the degradation of PD-L1. CSN5-IN-3 downregulates Bcl-2, and upregulates P53 and Cleaved caspase-3. CSN5-IN-3 exhibits anticancer activity against triple-negative breast cancer.
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dPDL1-4
0 ImagesCat. No.: HY-174468dPDL1-4 is a potent and selective eHSPTAC eHSP90 PD-L1 degrader with DC50s of 7.77 μM and 6.52 μM in HeLa and B16F10 cells. dPDL1-4 bridges eHSP90 with the target protein, inducing lysosomal degradation. dPDL1-4 can degrade PD-L1 significantly and inhibits tumor growth. dPDL1-4 can be used for the study of cervical cancer and melanoma. ((Pink: eHSP90 ligand (HY-174476); Blue: PD-L1 ligand (HY-116274); Black: Linker (HY-W021787); HSP ligand + linker: HY-174799)).
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PCC16 chloride
0 ImagesCat. No.: HY-169232PCC16 chloride is a dual PROTAC degrader targeting DHHC3 and PD-L1, with a DC50 of 0.103 μM for PD-L1 degradation. PCC16 chloride induces DHHC3 degradation via the ubiquitin-proteasome pathway by recruiting the CRBN E3 ubiquitin ligase (E3 ubiquitin ligase). By targeting DHHC3-which is essential for PD-L1 palmitoylation and membrane stability-PCC16 chloride reduces PD-L1 levels, decreases PD-L1 membrane retention time, and impairs its immunosuppressive function. PCC16 chloride enhances anti-tumor immunity by disrupting PD-L1-mediated immunosuppression. PCC16 chloride can be used in the research of immune checkpoint blockade-resistant cancers.
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HDAC3-IN-7
0 ImagesCat. No.: HY-172601CAS No.: 3104610-92-3HDAC3-IN-7 (Compound 8ae) is a selective HDAC3 inhibitor with an IC50 value of 311 nM. HDAC3-IN-7 degrades PD-L1 through the lysosome pathway mediated by Cathepsin B, exerting activities such as inhibiting tumor cell proliferation, migration, and invasion. HDAC3-IN-7 is promising for research of cancers.
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