tt-012

TT-012 has anti-tumor activity, selectively binds dynamic MITF and disrupts the dimer formation and DNA binding of the latter. TT-012 can inhibit the transcription of MITF in B16F10 melanoma cells. TT-012 inhibited the growth and metastasis of MITF melanoma cells in animal models. TT-012 is less cytotoxic to liver and immune cells.

TT-012-Br (Compound 4) is a ligand of MITF and can be used in the synthesis of PROTACs, such as WZS0347.

WZS0347Ligand-Linker Conjugate 1 (Compound 5d) is a synthetic target protein ligand-linker conjugate used in the synthesis of PROTACs, such as WZS0347. WZS0347 serves as a potent MITFPROTAC degrader with anti-cancer properties.