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BX-912

Cat. No. M2311

All AbMole products are for research use only, cannot be used for human consumption.

BX-912 Structure
Size Price Availability Quantity
1mg USD 70 In stock
5mg USD 100 In stock
10mg USD 180 In stock
25mg USD 360 In stock
50mg USD 630 In stock
100mg USD 850 In stock
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Quality Control & Documentation
Biological Activity

BX912 is a selective potent PDK1 inhibitor with an IC50 of 12 nM. BX912 also inhibits other kinases such as ChcK1, PKA, c-kit, and KDR with IC50 of 0.83, 0.11, 0.85, and 0.41 μM, resepectively. BX912 potently prevents PDK1 enzyme activity in a direct kinase assay format, although BX912 fails to block preactivated AKT2 activity (IC50 < 10 μM). BX912 is a competitive inhibitor of PDK1 activity with respect to its substrate, ATP. BX912 promotes a pronounced increase in the population of MDA-468 cells with 4 N DNA content, indicative of a block at the G2/M phase of the cell cycle. BX912 also potently inhibits the growth of HCT-116 cells in soft agar, showing a 96% inhibitory effect at a dose of 1 μM.

Chemical Information
Molecular Weight 471.35
Formula C20H23BrN8O
CAS Number 702674-56-4
Solubility (25°C) DMSO 60 mg/mL
Ethanol 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Yiguang Bai, et al. Effects of inhibiting PDK‑1 expression in bone marrow mesenchymal stem cells on osteoblast differentiation in vitro

[2] Saori Maegawa, et al. Phosphoinositide-dependent protein kinase 1 is a potential novel therapeutic target in mantle cell lymphoma

[3] Farha Naz, et al. Evaluation of human microtubule affinity-regulating kinase 4 inhibitors: fluorescence binding studies, enzyme, and cell assays

[4] Farha Naz, et al. Designing New Kinase Inhibitor Derivatives as Therapeutics Against Common Complex Diseases: Structural Basis of Microtubule Affinity-Regulating Kinase 4 (MARK4) Inhibition

[5] Richard I Feldman, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1

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  Catalog
Abmole Inhibitor Catalog




Keywords: BX-912 supplier, PDK1, inhibitors, activators

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