1-[5-(2,3-Dichloro-phenylsulfanyl)-4-nitro-thiophen-2-yl]-ethanone
Oxytocin-d5
CAS: 882257-11-6
Molecular Formula: C12H7Cl2NO3S2
1-[5-(2,3-Dichloro-phenylsulfanyl)-4-nitro-thiophen-2-yl]-ethanone - Names and Identifiers
1-[5-(2,3-Dichloro-phenylsulfanyl)-4-nitro-thiophen-2-yl]-ethanone - Physico-chemical Properties
| Molecular Formula | C12H7Cl2NO3S2 |
| Molar Mass | 348.22 |
| Density | 1.60±0.1 g/cm3(Predicted) |
| Boling Point | 452.4±45.0 °C(Predicted) |
| Solubility | DMSO: soluble10mg/mL, clear |
| Appearance | powder |
| Color | light yellow to dark yellow |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| In vitro study | P5091 is a trisubstituted thiophene with three substituents: dichlorophenylthio, Nitro and acetyl, which mediates the activity against usp7. P5091 acts on USP7 with potent, specific, selective deubiquitinating enzyme activity. In contrast, P5091 did not inhibit other DUBs and other family cysteine proteases (EC50 > 100 mM). P5091 inhibited USP7 with a HA-UbVME tag, a concentration-dependent effect. P5091 inhibits usp7-mediated cleavage of ultra-high molecular weight ubiquitin chains in a dose-dependent manner. Furthermore, P5091 inhibits USP7-but not USP2-or USP8-mediated cleavage of the Poly K48-linked ubiquitin chain. P5091 inhibits USP7, induces multiple ubiquitination of HDM2, and accelerates HDM2 degradation. P5091 acts on MM cells to inhibit the activity of USP7 deubiquitination enzyme, but does not inhibit protease activity. P5091 inhibits MM cell growth, overcoming the resistance to Bortezomib. P5091 induces a dose-dependent reduction in the viability of multiple MM cell lines, including those resistant to conventional therapy dexamethone (Dex) (MM.1R), Doxorubicin (Dox-40), or Melphalan (LR5). (IC50 6-14 μm) resistance. P5091 overcomes bone marrow mesenchymal stem cell-induced MM cell growth. P5091 reduced HDM2 and HDMX and upregulated p53 and p21 levels. Overall, P5091-induced cytotoxicity is mediated in part by the HDM2-p21 signaling axis, and although p53 is upregulated after P5091 treatment, the cytotoxic activity of P5091 is p53 independent. |
| In vivo study | P5091 acts on animal tumor models, is well tolerated, inhibits tumor growth, and prolongs animal life. P5091 in combination with Lenalidomide, the HDAC inhibitor SAHA, or dexametone triggers synergistic anti-MM activity. |
1-[5-(2,3-Dichloro-phenylsulfanyl)-4-nitro-thiophen-2-yl]-ethanone - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
1-[5-(2,3-Dichloro-phenylsulfanyl)-4-nitro-thiophen-2-yl]-ethanone - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 0.988 ml | 4.94 ml | 9.879 ml |
| 5 mM | 0.198 ml | 0.988 ml | 1.976 ml |
| 10 mM | 0.099 ml | 0.494 ml | 0.988 ml |
| 5 mM | 0.02 ml | 0.099 ml | 0.198 ml |
Last Update：2024-01-02 23:10:35
1-[5-(2,3-Dichloro-phenylsulfanyl)-4-nitro-thiophen-2-yl]-ethanone - Reference Information
| Biological activity | P5091 (P005091) is a selective, effective ubiquitin-specific protease 7 (USP7)(ubiquitin-specific protease 7) inhibitor, EC50 is 4.2 μM, similar to acting on USP47. |
| target | TargetValue USP7 (Cell-free say) 4.2 μM(EC50) USP47 (Cell-free say) 4.3 μM |
| Target | Value |
| USP7 (Cell-free assay) | 4.2 μM(EC50) |
| USP47 (Cell-free assay) | 4.3 μM |
| In vitro study | P5091 is a trisubstituted thiophene with three substituents of dichlorophenyl, nitro and acetyl, mediating anti-USP7 activity. P5091 acts on USP7 with potent, specific, selective deubiquitination activity. In contrast, P5091 did not inhibit other DUBs and other family cysteine proteases (EC50 > 100 mM). P5091 inhibits USP7 with HA-UbVME labels, and this effect is concentration-dependent. P5091 inhibits USP7-mediated cleavage of ultra-high molecular weight ubiquitin chains in a dose-dependent manner. Moreover, P5091 inhibits USP7-but not USP2-or USP8-mediated cleavage of the poly-K48-linked ubiquitin chain. P5091 inhibits USP7, induces HDM2 polyubiquitination, and accelerates HDM2 degradation. P5091 acts on MM cells, inhibiting USP7 deubiquitination activity, but not protease activity. P5091 inhibits MM cell growth and overcomes Bortezomib resistance. P5091 induces a dose-dependent decrease in viability of multiple MM cell lines, including those resistant to conventional therapy Dexamethasone (Dex) (MM.1R), Doxorubicin (Dox-40), or Melphalan (LR5) (IC50 is 6-14 μM). P5091 overcomes MM cell growth induced by bone marrow mesenchymal stem cells. P5091 reduces HDM2 and HDMX and up-regulates p53 and p21 levels. In general, the cytotoxicity induced by P5091-is partially mediated by the HDM2-p21 signal axis. Although p53 is up-regulated after P5091 treatment, the cytotoxic activity of P5091 is independent of p53. |
| in vivo study | P5091 acts on animal tumor models, which is well tolerated, inhibits tumor growth and prolongs animal life. P5091 is used in combination with Lenalidomide, HDAC inhibitor SAHA, or Dexamethasone to trigger synergistic anti-MM activity. |
Last Update：2024-04-09 21:53:21
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Spot supply
Product Name: Oxytocin-d5 Visit Supplier Webpage Request for quotationCAS: 882257-11-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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