1. PI3K/Akt/mTOR
    Apoptosis
  2. PDK-1
    Apoptosis
  3. BX-912

BX-912 

Cat. No.: HY-11005 Purity: 98.94%
Handling Instructions

BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.

For research use only. We do not sell to patients.

BX-912 Chemical Structure

BX-912 Chemical Structure

CAS No. : 702674-56-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 178 In-stock
Estimated Time of Arrival: December 31
5 mg USD 162 In-stock
Estimated Time of Arrival: December 31
50 mg USD 648 In-stock
Estimated Time of Arrival: December 31
100 mg USD 972 In-stock
Estimated Time of Arrival: December 31
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Based on 4 publication(s) in Google Scholar

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Description

BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis[1].

IC50 & Target

IC50: 26 nM (PDK1)[1]

In Vitro

BX-912 promotes a block at the G2/M phase of the cell cycle in MDA-468 cells[1].
BX-912 binds to the ATP binding site of PDK1, and is 9-fold selective for PDK1 relative to PKA. BX-912 blocks PDK1 activity in PTEN-negative PC-3 cells. PTEN-negative PC-3 cells display constitutive activation of Akt which is reflected in high levels of the PDK1 product, phospho-Thr308-Akt[1].
BX-912 is identified in a coupled assay measuring PDK1- and PtdIns-3,4-P2-mediated Akt activation, which can detect inhibitors of PDK1, AKT2, or other steps critical for activation of AKT2[1].

Molecular Weight

471.35

Formula

C₂₀H₂₃BrN₈O

CAS No.

702674-56-4

SMILES

BrC1=C(NCCC2=CNC=N2)N=C(NC3=CC(NC(N4CCCC4)=O)=CC=C3)N=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (212.16 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1216 mL 10.6078 mL 21.2157 mL
5 mM 0.4243 mL 2.1216 mL 4.2431 mL
10 mM 0.2122 mL 1.0608 mL 2.1216 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (5.83 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (5.83 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (5.83 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

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) contains: 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 can sensitively detect inhibitors of AKT2 activation as well as direct inhibitors of PDK1 or AKT2[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

The cell lines MDA-468, MDA-453, HCT-116, U87-MG, U2OS, PC-3, B16F10, and MiaPaCa; LOX amelanotic human melanoma cells; and HeLa 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 BX-912 (1, 10, 100 and 1000 nM) in 1% DMSO and growth medium (final concentration of DMSO, 0.1%), followed by brief shaking. Treated cells are incubated for 72 h, 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

BX-912BX912BX 912PDK-1ApoptosisPhosphoinositide dependent protein kinase-1Inhibitorinhibitorinhibit

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Product name:
BX-912
Cat. No.:
HY-11005
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