货号 | 4143/50 |
别名 | (3S,6R)-1-[6-(3-Amino-1H-indazol-6- |
供应商 | Tocris |
生物活性 | Potent 3-phosphoinositide-dependent protein kinase (PDPK1) inhibitor (IC50 ~ 10 nM). Exhibits no effect on other kinases including Aurora, ROCK, p38 MAPK and PI 3-K. Suppresses T-loop phosphorylation and subsequent activation of PDK1 substrates S6K1, SGK and RSK in vitro; exhibits limited inhibitory effect on Akt activation. Delays melanomagenesis and metastasis in BrafV600E::Pten(-/-)mice. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 462.59 |
分子式 | C25H34N8O |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
参考文献 | Scortegagnaet al (2014) Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of BrafV600E::Pten(-/-) melanoma. Oncogene 33 4330. PMID: 24037523. Najafovet al (2011) Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem.J. 433 357. PMID: 21087210. |