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. 2022 Mar 24;13:821344. doi: 10.3389/fphar.2022.821344

TABLE 1.

STAT3 inhibitors in melanoma.

Small molecule inhibitor(s) Mechanism of action
Stattic, STA-21, S32-M2001, S3I-201 Antitumor activity by their ability to induce apoptosis via STAT3 inhibition
LLL-3, an early generation STAT3 inhibitor Antitumor activity in different tumor models
FLLL32, a structural analog of curcumin Inhibits STAT3 while retaining STAT1 mediated signal transduction within melanoma and immune sensitive cells, FLLL32 triggers caspase-dependent apoptosis via its inhibition of STAT3
Resveratrol, flavopiridol, indirubin, magnolol, picetannol, parthenolide, EGCG, curcubitacin Q and curcumin Downregulate the activity of STAT3 in cancer cells
Peptide aptamers Interacts with a dimerized form of STAT3 thereby causes inhibition of antiapoptotic proteins and promotes apoptosis in melanoma cells
S31–1757 and S31-201 micelle formulation Inhibits STAT3 dimerization in both cellular and animal models of melanoma with less undesirable effects on normal cells
Novel platinum (IV) compounds (CPA-1, CPA-7) Disrupts STAT3 signaling, thereby abrogates tumor-promoting activity of STAT3
C48 Promotes alkylation of STAT3 at cys468 thereby attenuating the accumulation of activated STAT3 in the nucleus to inhibit the growth of melanoma cells