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R4VPL3-1

Chemical Structure : R4VPL3-1

CAS No.:

R4VPL3-1 (R4VP L3-1)

Catalog No.: PC-26976Not For Human Use, Lab Use Only.

R4VPL3-1 is a PROTAC-like molecule that induces proteasomal degradation of RNF4, also induces the elimination of VHL in cancer cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 1082.75
Formula C57H72ClN7O10S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2R,4R)-1-((R)-2-(tert-butyl)-18-(4-(4-(2-chloro-N-(4-(dimethylamino)benzyl)acetamido)phenoxy)phenoxy)-4,13-dioxo-7,10-dioxa-3,14-diazaoctadecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

References

1. Oknin-Vaisman A, et al. Oncogene. 2026 Jun 5. doi: 10.1038/s41388-026-03829-2.

2. Carl C Ward, et al. ACS Chem Biol. 2019 Nov 15;14(11):2430-2440.

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