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Submit ReviewBX 795
说明： PDPK1 (PDK1) inhibitor
化学名： N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide
纯度： ≥98% (HPLC)
生物活性 for BX 795
BX 795 is an inhibitor of 3-phosphoinositide-dependent kinase 1 (PDPK1). Inhibits Akt phosphorylation at Thr308 in PC3 cells; also inhibits anchorage-independent growth of PC3 and MDA-MB-468 cells. Exhibits activity at other kinases, including TANK-binding kinase 1 (TBK1), Aurora B and IκB kinase ε (IKKε). Also enhances lentiviral transduction of natural killer (NK) cells by around 3.8-fold.
技术数据 for BX 795
| 分子量 | 591.47 |
| 公式 | C23H26IN7O2S |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 702675-74-9 |
| PubChem ID | 10077147 |
| InChI Key | VAVXGGRQQJZYBL-UHFFFAOYSA-N |
| Smiles | IC1=C(NCCCNC(C4=CC=CS4)=O)N=C(NC2=CC(NC(N3CCCC3)=O)=CC=C2)N=C1 |
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 BX 795
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 59.15 | 100 | |
| ethanol | 59.15 | 100 |
制备储备液 for BX 795
以下数据基于产品分子量 591.47。 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 |
|---|---|---|---|
| 1 mM | 1.69 mL | 8.45 mL | 16.91 mL |
| 5 mM | 0.34 mL | 1.69 mL | 3.38 mL |
| 10 mM | 0.17 mL | 0.85 mL | 1.69 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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产品说明书 for BX 795
参考文献 for BX 795
参考文献是支持产品生物活性的出版物。
Feldman et al (2005) Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J.Biol.Chem. 280 19867 PMID: 15772071
Clark et al (2009) Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IκB kinase ε: a distinct upstream kinase mediates Ser-172 phosphorylation and activati J.Biol.Chem. 284 14136 PMID: 19307177
Tamguney et al (2008) Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cells. Exp.Cell Res. 314 2299 PMID: 18514190
Sutlu et al (2012) Inhibition of intracellular antiviral defense mechanisms augments lentiviral transduction of human natural killer cells: implications for gene therapy. Hum. Gene Ther. 23 1090 PMID: 22779406
If you know of a relevant reference for BX 795, please let us know.
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关键词: BX 795, BX 795 supplier, BX795, pdk1, inhibitors, inhibits, 3-phosphoinositide-dependent, kinase-1, TBK1, TANK-binding, kinase, 1, Aurora, B, IkBe, IkappaBepsilon, IκBε, multi-kinase, PDPK1, enhances, enhancers, viral, transduction, Phosphoinositide-dependent, Kinase, PDK1, TANK, binding, (TBK), Viral, Transduction, Enhancers, 4318, Tocris Bioscience
3 篇 BX 795 的引用文献
引用文献是使用了 Tocris 产品的出版物。 BX 795 的部分引用包括：
Johnson et al (2019) Aspirin inhibits platelets from reprogramming breast tumor cells and promoting metastasis. Blood Adv 3 198 PMID: 30670536
Anne et al (2021) Chemotherapy-induced transposable elements activate MDA5 to enhance haematopoietic regeneration. Nat Cell Biol 23 704-717 PMID: 34253898
Pillai et al (2015) Tank binding kinase 1 is a centrosome-associated kinase necessary for microtubule dynamics and mitosis. Nat Commun 6 10072 PMID: 26656453
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