For research use only. Not for therapeutic Use.
<p>
P005091(cas# 882257-11-6) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM.<br />
IC50 Value: 4.2 uM (EC50).
</p>
<p>
Ubiquitin-specific proteases (USP/UBP) remove ubiquitin from proteins, sparing them from degradation by the proteasome. USP7 is a cysteine protease associated with prostate cancer that selectively deubiquitylates HDM2, the ubiquitin E3 ligase for the tumor suppressor p53. P005091 is a trisubstituted thiophene that inhibits USP7 and the closely related USP47 (EC50s = 4.2 and 4.3 μM, respectively) with little activity against other classes of proteases, including caspases, cathepsins, calpain, metalloproteases, and serine proteases (EC50s = > 100 μM). P005091 has been shown to accelerate the degradation of the USP7 substrate HDM2 in several multiple myeloma cell lines (EC50 = 11 μM) and to inhibit the growth of HCT116 human colorectal cancer cells (EC50 = 11 μM) synergistically with doxorubicin, etoposide, or mechlorethamine. In vivo, 10 mg/kg P005091 prolongs survival and reduces tumor growth in mice bearing human multiple myeloma and B cell leukemia xenografts.
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| Catalog Number | I005302 |
| CAS Number | 882257-11-6 |
| Synonyms | P005091; 1-[5-(2,3-dichlorophenyl)sulfanyl-4-nitrothiophen-2-yl]ethanone |
| Molecular Formula | C₁₂H₇Cl₂NO₃S₂ |
| Purity | ≥95% |
| Target | Deubiquitinase |
| Solubility | DMSO: 28 mg/mL, H2O: <1 mg/mL |
| Storage | Store at 4°C |
| IC50 | 4.2 uM (EC50) |
| InChI | InChI=1S/C12H7Cl2NO3S2/c1-6(16)10-5-8(15(17)18)12(20-10)19-9-4-2-3-7(13)11(9)14/h2-5H,1H3 |
| InChIKey | LKZLGMAAKNEGCH-UHFFFAOYSA-N |
| SMILES | CC(=O)C1=CC(=C(S1)SC2=C(C(=CC=C2)Cl)Cl)[N+](=O)[O-] |
| Reference | 1. Cell Biochem Biophys. 2011 Jun;60(1-2):61-8. doi: 10.1007/s12013-011-9185-5. |
