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Submit ReviewPEP 005
说明： Protein kinase C activator
别名： Ingenol 3-angelate,Ingenol Mebutate
化学名： (2Z)-2-Methyl-2-butenoic acid (1aR,2S,5R,5aS,6S,8aS,9R,10aR)-1a,2,5,5a,6,9,10,10a-octahydro-5,5a-dihydroxy-4-(hydroxymethyl)-1,1,7,9-tetramethyl-11-oxo-1H-2,8a-methanocyclopenta[a]cyclopropa[e]cyclodecen-6-yl ester
纯度： ≥97% (HPLC)
生物活性 for PEP 005
PEP 005 is an activator of protein kinase C (PKC). Exhibits antileukemic activity; induces nuclear translocation of PKCδ, and induces apoptosis in acute myeloid leukemia (AML) cell lines and primary AML blast cells. Also displays antiproliferative effects and induces apoptosis in Colo205 cells. Reactivates latent HIV in cell culture. Also reactivates hypofunctional CD8+ T cells during chronic viral infection. Acts as a substrate for multidrug transporter.
技术数据 for PEP 005
| 分子量 | 430.53 |
| 公式 | C25H34O6 |
| 储存 | Store at -20°C |
| 纯度 | ≥97% (HPLC) |
| CAS Number | 75567-37-2 |
| PubChem ID | 6918670 |
| InChI Key | VDJHFHXMUKFKET-WDUFCVPESA-N |
| Smiles | CC([C@@H]2OC(/C(C)=C\C)=O)=C[C@@]1([C@H](C)C4)[C@]2(O)[C@H](O)C(CO)=C[C@]([C@@]3([H])[C@]4([H])C(C)3C)([H])C1=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for PEP 005
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 0.86 | 2 |
制备储备液 for PEP 005
以下数据基于产品分子量 430.53。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.02 mM | 116.14 mL | 580.68 mL | 1161.36 mL |
| 0.1 mM | 23.23 mL | 116.14 mL | 232.27 mL |
| 0.2 mM | 11.61 mL | 58.07 mL | 116.14 mL |
| 1 mM | 2.32 mL | 11.61 mL | 23.23 mL |
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产品说明书 for PEP 005
参考文献 for PEP 005
参考文献是支持产品生物活性的出版物。
Benhadji et al (2008) Antiproliferative activity of PEP005, a novel ingenol angelate that modulates PKC functions, alone and in combination with cytotoxic agents in human colon cancer cells. Br.J.Cancer 99 1808 PMID: 19034280
Li et al (2010) The skin cancer chemotherapeutic agent ingenol-3-angelate (PEP005) is a substrate for the epidermal multidrug transporter (ABCB1) and targets tumor vasculature. Cancer Res. 70 4509 PMID: 20460505
Kedei et al (2004) Characterization of the interaction of ingenol-3-angelate with protein kinase C. Cancer Res. 64 3243 PMID: 15126366
Hampson et al (2005) PEP005, a selective small-molecule activator of protein kinase C, has potent antileukemic activity mediated via the delta isoform of PKC. Blood 106 1362 PMID: 15845901
Jiang et al (2015) Synergistic reactivation of latent HIV expression by Ingenol-3-Angelate, PEP005, targeted NF-kB signaling in combination with JQ1 induced p-TEFb activation. PLoS Pathog. 11 e1005066 PMID: 26225771
Marro et al (2019) Discovery of small molecules for the reversal of T cell exhaustion. Cell Rep. 29 3293 PMID: 31801090
If you know of a relevant reference for PEP 005, please let us know.
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关键词: PEP 005, PEP 005 supplier, Ingenol, 3-angelate, PEP005, protein, kinase, C, PKC, activators, anticancer, antileukemic, PKCd, PKCdelta, PKCδ, T, cells, exhaustion, CD8, hypofunction, ingenol, mebuate, IngMb, Mebutate, Protein, Kinase, Multidrug, Transporters, 4054, Tocris Bioscience
2 篇 PEP 005 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PEP 005 的部分引用包括：
Oliver et al (2022) High-content phenotyping of Parkinson's disease patient stem cell-derived midbrain dopaminergic neurons using machine learning classification. Stem Cell Reports 17 2349-2364 PMID: 36179692
Jiang et al (2015) Synergistic reactivation of latent HIV expression by Ingenol-3-Angelate, PEP005, targeted NF-kB signaling in combination with JQ1 induced p-TEFb activation. PloS Pathog. 11 e1005066 PMID: 26225771
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