
P005091
CAS No. 882257-11-6
P005091 ( P005091 | P-005091 | P 005091 | P 5091 )
产品货号. M19224 CAS No. 882257-11-6
P005091 是一种选择性有效的泛素特异性蛋白酶 7 (USP7) 抑制剂,EC50 为 4.2 μM。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
2MG | ¥316 | 有现货 |
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5MG | ¥510 | 有现货 |
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10MG | ¥656 | 有现货 |
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25MG | ¥1280 | 有现货 |
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50MG | ¥2187 | 有现货 |
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100MG | ¥3499 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称P005091
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述P005091 是一种选择性有效的泛素特异性蛋白酶 7 (USP7) 抑制剂,EC50 为 4.2 μM。
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产品描述P005091 is a potent and selective inhibitor of ubiquitin-specific protease (USP) 7 (IC50 = 4.2 μ M). P005091 induces elevated p53 and apoptosis in cancer cell lines and displays antiangiogenic activity in vivo . The deubiquitylating enzyme USP7 (HAUSP) sits at a critical node regulating the activities of numerous proteins broadly characterized as tumor suppressors, DNA repair proteins, immune responders, viral proteins, and epigenetic modulators. Aberrant USP7 activity may promote oncogenesis and viral disease making it a compelling target for therapeutic intervention.(In Vitro):P005091 is a trisubstituted thiophene with dichlorophenylthio, nitro, and acetyl substituents mediating anti-USP7 activity. P005091 exhibits potent, specific, and selective deubiquitylating activity against USP7. In contrast, P005091 does not inhibit other DUBs or other families of cysteine proteases tested (EC50 > 100 mM). P005091 inhibits the labeling of USP7 with HA-UbVME in a concentration-dependent manner. USP7-mediated cleavage of high molecular weight polyubiquitin chains is inhibited in a dose-dependent manner by P005091. Moreover, P005091 inhibits USP7- but not USP2- or USP8-mediated cleavage of poly K48-linked ubiquitin chains. USP7 inhibition by P005091 induces HDM2 polyubiquitylation and accelerates degradation of HDM2. P005091 inhibits USP7 deubiquitylating activity, without blocking proteasome activity in MM Cells. P005091 inhibits growth in MM cells and overcomes bortezomib-resistance. P005091 induces a dose-dependent decrease in viability of various MM cell lines, including those that are resistant to conventional therapies dexamethasone (Dex) (MM.1R), doxorubicin (Dox-40), or melphalan (LR5) (IC50 range 6-14 μM). P005091 overcomes bone marrow stromal cell-induced growth of MM Cells. P005091 decreases HDM2 and HDMX, as well as upregulated p53 and p21 levels. Overall, P005091-induced cytotoxicity is mediated in part via HDM2-p21 signaling axis and although p53 is upregulated in response to P005091 treatment, the cytotoxic activity of P005091 is not dependent on p53.(In Vivo):In animal tumor model studies, P005091 is well tolerated, inhibits tumor growth, and prolongs survival. Combining P005091 with lenalidomide, HDAC inhibitor SAHA, or dexamethasone triggers synergistic anti-MM activity.
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体外实验P005091 is a trisubstituted thiophene with dichlorophenylthio, nitro, and acetyl substituents mediating anti-USP7 activity. P005091 exhibits potent, specific, and selective deubiquitylating activity against USP7. In contrast, P005091 does not inhibit other DUBs or other families of cysteine proteases tested (EC50 > 100 mM). P005091 inhibits the labeling of USP7 with HA-UbVME in a concentration-dependent manner. USP7-mediated cleavage of high molecular weight polyubiquitin chains is inhibited in a dose-dependent manner by P005091. Moreover, P005091 inhibits USP7- but not USP2- or USP8-mediated cleavage of poly K48-linked ubiquitin chains. USP7 inhibition by P005091 induces HDM2 polyubiquitylation and accelerates degradation of HDM2. P005091 inhibits USP7 deubiquitylating activity, without blocking proteasome activity in MM Cells. P005091 inhibits growth in MM cells and overcomes bortezomib-resistance. P005091 induces a dose-dependent decrease in viability of various MM cell lines, including those that are resistant to conventional therapies dexamethasone (Dex) (MM.1R), doxorubicin (Dox-40), or melphalan (LR5) (IC50 range 6-14 μM). P005091 overcomes bone marrow stromal cell-induced growth of MM Cells. P005091 decreases HDM2 and HDMX, as well as upregulated p53 and p21 levels. Overall, P005091-induced cytotoxicity is mediated in part via HDM2-p21 signaling axis and although p53 is upregulated in response to P005091 treatment, the cytotoxic activity of P005091 is not dependent on p53.
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体内实验In animal tumor model studies, P005091 is well tolerated, inhibits tumor growth, and prolongs survival. Combining P005091 with lenalidomide, HDAC inhibitor SAHA, or dexamethasone triggers synergistic anti-MM activity.
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同义词P005091 | P-005091 | P 005091 | P 5091
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通路Others
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靶点Other Targets
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受体USP7
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研究领域Cancer
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适应症——
化学信息
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CAS Number882257-11-6
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分子量348.21
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分子式C12H7Cl2NO3S2
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纯度>98% (HPLC)
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溶解度DMSO : 50 mg/mL 143.59 mM; H2O : < 0.1 mg/mL
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SMILESCC(=O)c1cc(c(Sc2cccc(Cl)c2Cl)s1)[N+](=O)[O-]
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化学全称1-(5-((2,3-dichlorophenyl)thio)-4-nitrothiophen-2-yl)ethanone
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.Chauhan D, et al. A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance. Cancer Cell. 2012 Sep 11;22(3):345-58.
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