R4VPL3-1 is a PROTAC-like molecule that induces proteasomal degradation of RNF4, also induces the elimination of VHL in cancer cells.
R4VPL3-1 has significant anti-cancer activity towards human squamous cancer cells (SCC1), inhibiting proliferation and sphere formation (SFA) with IC50 of 0.3 uM.
R4VPL3-1 induces death of human skin and melanoma cancer cells, but does not affect MEFs and non-oncogenic cells.
R4VPL3-1 induces ferroptosis in A375R RTKi-resistant melanoma cells, co-inactivates anti-ferroptotic selanoproteins such as GPX4, along with the elimination of RNF4 and the anti-ferroptotic E3 ligase VHL.
