Chemical Structure : UFSP2 inhibitor compound-8
Catalog No.: PC-20117Not For Human Use, Lab Use Only.
UFSP2 inhibitor compound-8 is a small molecule covalent inhibitor of UFSP2, binds to Cys294 of UFSP2, promotes the protein modification by Ubiquitin-fold modifier 1 (UFM1) (UFMylation) of PD-L1 and destabilizes PD-L1.
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UFSP2 inhibitor compound-8 is a small molecule covalent inhibitor of UFSP2, binds to Cys294 of UFSP2, promotes the protein modification by Ubiquitin-fold modifier 1 (UFM1) (UFMylation) of PD-L1 and destabilizes PD-L1.
Compound-8 (5 μg/mL) could significantly and consistently improve the global UFMylation activity in both MDA-MB-231 and MC38 cells.
Compound-8 (5-15 μg/mL)decreased the expression of PD-L1 without affecting the UFSP2 protein levels.
Compound-8 dose dependently enhanced the global UFMylation proteins while decreasing the expression of PD-L1.
Compound-8 imparts tumor immune evasion in vivo, exhibits better antitumor effect with no appreciable body weight loss when combined with PD-1 blockade.
UFSP2 is the primary "de-UFMylation" enzyme in human cells, UFSP2 acts as a de-UFMylation enzyme for PD-L1 through direct physical interaction.
M.Wt | 209.64 | |
Formula | C6H8ClNO3S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
1. Zhou J, et al. Proc Natl Acad Sci U S A. 2023 Mar 14;120(11):e2215732120.
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