Results for Chemicals & Small Molecules ( 84800 )
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MS 39 is a highly effective, highly affinity and selective depressant of mutant epidermal growth factor receptor (EGFR) with high efficiency, high affinity and selectivity. MS 39, conjured by gefitinib to VHL ligand via a linker, effectively induced the degradation of mutant EGFR (DC50 values in HCC827(exon 19 del) and H3255 (L858R mutation) lung cancer cell lines were 5 nM and 3.3 nM, respectively). However, there was no significant effect in wild-type EGFR cell lines with concentrations up to 10 μM. MS 39 inhibited the proliferation of H3255 lung cancer cells in vitro and was bioavailable in mice after administration.
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PROTAC(H-PGDS)-7 is a selective and potent small molecule hematopoietic prostaglandin D synthase (H-PGDS) PROTAC degradation agent that exhibits degradation activity in KU812 cells with a DC50 of 17.3 pM. PROTAC(H-PGDS)-7 is a pharmacological compound that effectively inhibits prostaglandin D2 (PGD2) PROTAC(H-PGDS)-7 is a candidate compound for the treatment of DMD and other H-PGDS-related diseases.
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Tipranavir is a protease inhibitor that inhibits HIV-1 resistant to more than 1 protease inhibitor .Tipranavir effectively inhibits HIV-1 protease enzyme activity and dimerisation and has potent activity against multiple protease inhibitor (PI) HIV-1 isolates (IC50 of 66-410 nM). Tipranavir inhibits SARS-CoV-2 3CLpro activity.