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PI3K/Akt/mTOR signaling PDK BX795

BX795

Catalog No. T1830   CAS 702675-74-9

BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.

BX795, CAS 702675-74-9
Pack Size Availability Price/USD Quantity
5 mg In stock 60.00
10 mg In stock 111.00
25 mg In stock 245.00
50 mg In stock 400.00
100 mg In stock 600.00
1 mL * 10 mM (in DMSO) In stock 90.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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Description BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.
Targets&IC50 CDK2/CyclinE : ic50 430nM,   Chk1 : ic50 510nM,   c-Kit : ic50 320nM,   PDK1 : ic50 6nM,  
Kinase Assay Kinase assays: PDK1 is assayed in a direct kinase assay and a coupled assay format measuring PDK1- and PtdIns-3,4-P2-mediated activation of AKT2. For the coupled assay, the final assay mixture (60 μL) contained: 15 mM MOPS, pH 7.2, 1 mg/mL bovine serum albumin, 18 mM β-glycerol phosphate, 0.7 mM dithiothreitol, 3 mM EGTA, 10 mM MgOAc, 7.5 μM ATP, 0.2 μCi of [γ-33P]ATP, 7.5 μM biotinylated peptide substrate (biotin-ARRRDGGGAQPFRPRAATF), 0.5 μL of PtdIns-3,4-P2-containing phospholipid vesicles, 60 pg of purified recombinant human PDK1, and 172 ng of purified recombinant human AKT2. After incubation for 2 h at room temperature, the biotin-labeled peptide is captured from 10 μl of the assay mixture on streptavidin-coated SPA beads, and product formation is measured by scintillation proximity in a Wallac MicroBeta counter. The product formed is proportional to the time of incubation and to the amount of PDK1 and inactive AKT2 added. PDK1 is added at suboptimal levels so that the assay could sensitively detect inhibitors of AKT2 activation as well as direct inhibitors of PDK1 or AKT2. To measure PDK1 activity directly, the final assay mixture (60 μL) contained 50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 0.1 mM EDTA, 0.1% β-mercaptoethanol, 1 mg/mL bovine serum albumin, 10 mM MgOAc, 10 μM ATP, 0.2 μCi of [γ-33P]ATP, 7.5 μM substrate peptide (H2N-ARRRGVTTKTFCGT), and 60 ng of purified recombinant human PDK1. After 4 h at room temperature, we add 25 mM EDTA and spotted a portion of the reaction mixture on Whatman P81 phosphocellulose paper. The filter paper is washed three times with 0.75% phosphoric acid and once with acetone. After drying, the filter-bound labeled peptide is quantified using a Fuji phosphorimager.
Cell Research
Cells seeded at a low density (1,500–3,000 cells/well, 0.1 mL/well, 96-well plates) are incubated overnight. Compound treatments are made by adding 10 μL/well of the compound in 1% dimethyl sulfoxide and growth medium (final concentration of dimethyl sulfoxide, 0.1%), followed by brief shaking. Treated cells are incubated for 72 hours, and viability is measured by the addition of 10 μL of the metabolic dye WST-1. The WST-1 signal is read in a plate reader at 450 nm, and a no cell, or zero time cell, background is subtracted to calculate the net signal. Results are reported as the average ± S.E. of two or more replicates.(Only for Reference)
Cell lines: MDA-468, PC-3, HCT-116 and MiaPaca cells
Molecular Weight 591.47
Formula C23H26IN7O2S
CAS No. 702675-74-9

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 59.2 mg/mL (100 mM)

Ethanol: 59.2 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL

Citations

References and Literature
1. Feldman RI, et al. J Biol Chem. 2005, 280(20), 19867-119874. 2. Clark K, et al. J Biol Chem. 2009, 284(21), 14136-14146. 3. Dangelmaier C, et al. Thromb Haemost. 2013,111(4).

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library PI3K-AKT-mTOR Compound Library Tyrosine kinase inhibitor library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Anti-Cardiovascular Disease Compound Library Anti-cancer Metabolism Compound Library Preclinical Compound Library Cell cycle related Compound Library

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