BX795
Cat. No.：YN410009
CAS No. ：702675-74-9
| 产品名称: | BX795 |
| CAS No.: | 702675-74-9 |
| Chemical Name: | N-[3-[[5-iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide |
| Synonyms: | N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide;BX-795;1-Pyrrolidinecarboxamide, N-[3-[[5-iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-;BX 795;BX-795 (BX 79 |
| 分子量: | 591.47 |
| 分子式: | C₂₃H₂₆IN₇O₂S |
| SMILES: | O=C(NCCCNC1=C(C=NC(NC2=CC=CC(NC(N3CCCC3)=O)=C2)=N1)I)C4=CC=CS4 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | BX795 是一种有效的、选择性的PDK1抑制剂，IC50值为 6 nM。同时，BX795 为有效、相对特异性的TBK1和IKKɛ的抑制剂，IC50值分别为 6 和 41 nM。BX795 抑制 S6K1，Akt，PKCδ 和 GSK3β 的磷酸化。BX795 对 PKA，PKC，c-Kit，GSK3β 选择性较低。BX795 可调节自噬 (autophagy)。 |
| IC50和靶点: | [{name:"PDK1:6 nM (IC50)"},{name: "TBK1:6 nM (IC50)"},{name: "IKKε:41 nM (IC50)"}] |
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Feldman, R.I., Wu, J.M., Polokoff, M.A., et al.Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1J. Biol. Chem.280(20),19867-19874(2005)
Clark, K., Plater, L., Peggie, M., et al.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 activationJ. Biol. Chem.284(21),14136-14146(2009)
Tamgüney, T., Zhang, C., Fiedler, D., et al.Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cellsExp. Cell Res.314(11-12),2299-2312(2008)
