WZS0347 is a MITF PROTAC degrader. WZS0347 effectively reduces MITF protein levels in various melanoma cell lines. WZS0347 induces MITF degradation via the cereblon -dependent ubiquitin-proteasome pathway, downregulates the expression of downstream target genes of MITF, and inhibits the colony formation and migration abilities of cancer cells. WZS0347 can be used in melanoma-related research [1]. (Pink: Microphthalmia Associated Transcription Factor (MITF) ligand; Blue: Cereblon ligand; Black: linker ).
In Vitro, WZS0347 (0.1-1 μM; 48 h) potently induces MITF degradation in B16F10 mouse melanoma cells[1]. WZS0347 (10 nM-10000 nM; 24 h) induces concentration-dependent degradation of MITF in B16F10 mouse melanoma cells[1]. WZS0347 (1 μM; 1-24 h) induces time-dependent degradation of MITF in B16F10 mouse melanoma cells[1]. WZS0347 (1 nM-1000 nM; 12 h) induces MITF degradation in human melanoma A375 cells in a concentration-dependent manner[1]. WZS0347 (1 nM-1000 nM; 24 h) induces concentration-dependent degradation of MITF in GAK human melanoma cells[1]. WZS0347 (1 μM; 24 h) induces MITF degradation in B16F10 mouse melanoma cells through binding to MITF, as pretreatment with the MITF ligand TT-012 reverses this degradation effect[1]. WZS0347 (1 μM; 24 h)-induced MITF degradation in B16F10 mouse melanoma cells is dependent on CRBN, as pretreatment with the CRBN ligand Lenalidomide reverses this degradation process[1]. WZS0347 (1 μM; 24 h) induces proteasome-dependent degradation of MITF in B16F10 mouse melanoma cells, as pretreatment with a proteasome inhibitor abrogates this degradation[1]. WZS0347 (1 μM; 0-24 h) shortens the half-life of MITF protein in B16F10 mouse melanoma cells, reducing the basal half-life from 12 h[1]. WZS0347 (0.3 μM) downregulates the mRNA levels of MITF and its downstream target genes TYR and Trpm1 in B16F10 mouse melanoma cells[1]. WZS0347 (100 nM-1000 nM; 5 days) inhibits colony formation of B16F10 mouse melanoma cells in a dose-dependent manner[1]. WZS0347 (0.5-1 μM; 24 h) inhibits the migration of B16F10 mouse melanoma cells and A375 human melanoma cells in a dose-dependent manner[1].
References:
[1]. Shen W, et al. Discovery of a first-in-class degrader for microphthalmia-associated transcription factor (MITF). European journal of medicinal chemistry. 2026 Jan 15;302(Pt 3):118367.
In Vitro, WZS0347 (0.1-1 μM; 48 h) potently induces MITF degradation in B16F10 mouse melanoma cells[1]. WZS0347 (10 nM-10000 nM; 24 h) induces concentration-dependent degradation of MITF in B16F10 mouse melanoma cells[1]. WZS0347 (1 μM; 1-24 h) induces time-dependent degradation of MITF in B16F10 mouse melanoma cells[1]. WZS0347 (1 nM-1000 nM; 12 h) induces MITF degradation in human melanoma A375 cells in a concentration-dependent manner[1]. WZS0347 (1 nM-1000 nM; 24 h) induces concentration-dependent degradation of MITF in GAK human melanoma cells[1]. WZS0347 (1 μM; 24 h) induces MITF degradation in B16F10 mouse melanoma cells through binding to MITF, as pretreatment with the MITF ligand TT-012 reverses this degradation effect[1]. WZS0347 (1 μM; 24 h)-induced MITF degradation in B16F10 mouse melanoma cells is dependent on CRBN, as pretreatment with the CRBN ligand Lenalidomide reverses this degradation process[1]. WZS0347 (1 μM; 24 h) induces proteasome-dependent degradation of MITF in B16F10 mouse melanoma cells, as pretreatment with a proteasome inhibitor abrogates this degradation[1]. WZS0347 (1 μM; 0-24 h) shortens the half-life of MITF protein in B16F10 mouse melanoma cells, reducing the basal half-life from 12 h[1]. WZS0347 (0.3 μM) downregulates the mRNA levels of MITF and its downstream target genes TYR and Trpm1 in B16F10 mouse melanoma cells[1]. WZS0347 (100 nM-1000 nM; 5 days) inhibits colony formation of B16F10 mouse melanoma cells in a dose-dependent manner[1]. WZS0347 (0.5-1 μM; 24 h) inhibits the migration of B16F10 mouse melanoma cells and A375 human melanoma cells in a dose-dependent manner[1].
References:
[1]. Shen W, et al. Discovery of a first-in-class degrader for microphthalmia-associated transcription factor (MITF). European journal of medicinal chemistry. 2026 Jan 15;302(Pt 3):118367.