化合物GSK2334470 T2348

Product Introduction
Bioactivity


英文名: GSK2334470

描述: GSK2334470是一种高效的、特异性的PDK1抑制剂，IC50=10 nM。

细胞实验: GSK2334470 is dissolved in DMSO and diluted with appropriate medium before use. To study the inhibitory effect of GSK2334470 on mTOR-S6K pathway, non-resistant cells and the resistant sublines are treated with GSK2334470 at 5 μM for 1.5 and 12 h in 10 % FBS medium with/without MK-2206 (5 μM)[2].

激酶实验: FGFR1-4 Biochemical Assays: FGFR kinase inhibition assays are performed at KM for ATP. Picomolar to low nanomolar concentrations of FGFR proteins are incubated in 1× Kinase Reaction Buffer (KRB) with 1 μM of CSKtide and 50 to 250 of μM ATP at 25°C for 90 minutes in the presence or absence of a dosed concentration series of inhibitor. All reactions are terminated by the addition of Stop buffer, and plates are read on a Caliper EZReader2. IC50 values are fit with a four-parameter log[Inhibitor] versus response model with floating Hill Slope.

体内活性: The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 is tested in newborn BrafV600E::Pten?/?mice subjected to systemic administration of 4-HT. Twice weekly administration of PDK1 results in marked inhibition of pigmented lesions and concomitant melanomagenesis, as well as significant inhibition of lung metastases, seen by H&E staining-based quantification (~80%), and lymph node metastases as by S100 immunostaining, similar to the phenotype seen upon genetic ablation of Pdk1[4].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 83 mg/mL (179.4 mM)
DMSO : 83 mg/mL (179.4 mM)


关键字: GSK-2334470 | Inhibitor | GSK 2334470 | PDK-1 | inhibit | GSK2334470

相关产品: RS1-PDK1 inhibitor | Polyphyllin I | δ-Tocotrienol | Dehydroabiethylamine | PS10 | BX-912 | Rabusertib | PS 48 | PS47 | KPLH1130

相关库: Neuronal Differentiation Compound Library | Anti-Metabolism Disease Compound Library | Antidepressant Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Obesity Compound Library | Highly Selective Inhibitor Library | Anti-Pancreatic Cancer Compound Library | Reprogramming Compound Library | NO PAINS Compound Library

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