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PI3K/Akt/mTOR signaling PDK BX912

BX912

Catalog No. T1837   CAS 702674-56-4
Purity 99.00% Datasheet

BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC etc.

BX912, CAS 702674-56-4
Pack Size Availability Price/USD Quantity
2 mg In stock 81.00
5 mg In stock 134.00
10 mg In stock 242.00
25 mg In stock 435.00
50 mg In stock 580.00
100 mg Inquiry 782.00
1 mL * 10 mM (in DMSO) In stock 136.00
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Purity 99.00%
Biological Description
Chemical Properties
Storage & Solubility Information
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Description BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC etc.
Targets&IC50 CDK2/CyclinE :ic50 650nM,   Chk1 :ic50 830nM,   PDK1 :ic50 12nM,   PKA :ic50 110nM,   VEGFR2 (KDR) :ic50 410nM,  
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 hours 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 inhibitor BX912 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 hours at room temperature, 25 mM EDTA is added and a portion of the reaction mixture on P81 phosphocellulose paper is spotted. 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 phosphorimager.
Cell Research
Cells such as MDA-468, MDA-453 are seeded at a low density (1.5-3 × 103 cells/well, 0.1 mL/well, 96-well plates) and are incubated overnight. BX912 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. (Only for Reference)
Cell lines: MDA-468, MDA-453
Appearance solid
Molecular Weight 471.35
Formula C20H23BrN8O
CAS No. 702674-56-4

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 87 mg/mL (184.6 mM)

Ethanol: 87 mg/mL (184.6 mM)

Water: <1 mg/mL

( < 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), 19867-19874.

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 GPCR Compound Library Anti-cancer Clinical Compound Library Angiogenesis related Compound Library Anti-cancer Metabolism Compound Library Preclinical Compound Library Cell cycle related Compound Library

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Dicumarol BX795 BX912 PHT-427 Osu-03012 Sodium Dichloroacetate BX-517 Rabusertib

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