PTP1B-IN-9

PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor. PTP1B-IN-9 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. PTP1B-IN-9 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome

PTP1B-IN-9 (0-30 µM; 48 hours) treatment produces a dose dependent reduction in the viability of HPV16-positive SiHa and Caski cells and HPV-39-positive ME180 cervical cancer cell lines respectively[1]. PTP1B-IN-9 reduces the cell viability of exponentially growing HeLa cervical cancer cells in a dose-dependent fashion with an IC50 value of 2 µM[1]. Cell Viability Assay[1] Cell Line: Keratinocytes, SiHa, CaSki and ME180 cells Concentration: 5, 10, 15, 20, 25, 30 µM Incubation Time: 48 hours Result: Produced a dose dependent reduction in the viability of HPV16-positive SiHa and Caski cells and HPV-39-positive ME180 cervical cancer cell lines respectively with minimal effects on the viability of primary human keratinocytes and with IC50 similar to the obtained with HeLa cells.

[1]. Anchoori RK, et al. Stressing the ubiquitin-proteasome system without 20S proteolytic inhibition selectively kills cervical cancer cells.PLoS One. 2011;6(8):e23888.