DU-14，5MG，SML3882-5MG，Sigma

Biochem/physiol Actions

VHL E3 ligase-dependent, highly potent and selective dual degrader of cellular PTP1B and TC-PTP (TCPTP) with anti-tumor efficacy in vivo.


DU-14 is a VHL E3 ligase-dependent, highly potent and selective dual degrader of PTP1B and TC-PTP (PTP1B/TCPTP DC50 post 16h treatment from 4.3/4.4 nM to 67.4/62.5 nM among 10 cell lines; 95% PTP1B & 92% TC-PTP degradation in HEK293 cells post 16h at 200 nM) with 88/162/302/342-fold selectivity over PTP-Meg2/FAP1/CD45/SHP2 and >400-fold over 8 other PTPs. DU-14 promotes CD8+ T-cell activation (48h 1 nM treatment prior to stimulation by α-CD3/α-CD28; murine CD8+ T-cells) and increases IFN-γ signaling (16h 25-500 nM treatment prior to IFN-γ stimulation; MC38 & U2OS cells). DU-14 blocks MC38 tumor growth in a syngeneic mouse model in vivo (25 or 50 mg/kg i.p.).