TABLE 1.
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 |