For research use only. Not for therapeutic Use.
USP28-IN-4 is a USP28 inhibitor (IC50=0.04 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-4 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-4 also decreases the ankyrase-1/2 level in vitro. USP28-IN-4 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331)[1].
USP28-IN-4 (compound 9p) (12.5 μM, 15 μM; 3 d) inhibits colony formation of human colorectal cancer cells HCT116 (15 μM) and Ls174T (12.5 μM)[1].
USP28-IN-4 (20-80 μM; 24 h) down-regulates the level of c-Myc by enhancing its degradation via ubiquitin-proteasome system (UPS)[1].
| Catalog Number | I041230 |
| CAS Number | 2931509-15-6 |
| Synonyms | 2-chloro-N-[4-chloro-3-(2,3-dihydro-1H-isoindol-5-yl)phenyl]-4-methylsulfonylbenzamide |
| Molecular Formula | C22H18Cl2N2O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C22H18Cl2N2O3S/c1-30(28,29)17-5-6-18(21(24)10-17)22(27)26-16-4-7-20(23)19(9-16)13-2-3-14-11-25-12-15(14)8-13/h2-10,25H,11-12H2,1H3,(H,26,27) |
| InChIKey | FZNJOQKABIINMG-UHFFFAOYSA-N |
| SMILES | CS(=O)(=O)C1=CC(=C(C=C1)C(=O)NC2=CC(=C(C=C2)Cl)C3=CC4=C(CNC4)C=C3)Cl |
| Reference | [1]. Zhou D, et al. Structure-based discovery of potent USP28 inhibitors derived from Vismodegib. Eur J Med Chem. 2023 Jun 5;254:115369. |
