Molecular structure of BX-912, CAS Number: 702674-56-4
BX-912 (CAS 702674-56-4)
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Alternate Names:
N-(3-(4-(2-(1H-imidazol-5-yl)ethylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide
Application:
BX-912 is a potent and selective PDK-1 inhibitor that induces apoptosis
CAS Number:
702674-56-4
Purity:
≥97%
Molecular Weight:
471.35
Molecular Formula:
C20H23BrN8O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
BX-912 is a 3-Phosphoinositide-dependent Kinase-1 (PDK-1) inhibitor. BX-912 suppresses growth in a number of cell lines and also induces apoptosis. Cell lines with elevated levels of AKT are >30-fold more sensitive to PDK1 inhibition by BX-912. This compound is a competitive inhibitor of PDK1, indicating that it binds to the ATP-binding pocket to inhibit phosphorylation. BX-912 accomplishes this due to the fact that the aminopyrimidine backbone, which adopts a similar conformation to ATP in the active site of PDK1. BX-912 potently inhibits the growth of PC-3 cells in soft agar, displaying an IC50 of 320 nM.
BX-912 (CAS 702674-56-4) References
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- Designing New Kinase Inhibitor Derivatives as Therapeutics Against Common Complex Diseases: Structural Basis of Microtubule Affinity-Regulating Kinase 4 (MARK4) Inhibition. | Naz, F., et al. 2015. OMICS. 19: 700-11. PMID: 26565604
- Phosphoinositide-dependent protein kinase 1 is a potential novel therapeutic target in mantle cell lymphoma. | Maegawa, S., et al. 2018. Exp Hematol. 59: 72-81.e2. PMID: 29287939
- Effects of inhibiting PDK‑1 expression in bone marrow mesenchymal stem cells on osteoblast differentiation in vitro. | Bai, Y., et al. 2021. Mol Med Rep. 23: PMID: 33300048
- Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration. | Drewry, DH., et al. 2022. J Med Chem. 65: 1313-1328. PMID: 34333981
- Clinical significance and immune landscape of cuproptosis-related lncRNAs in kidney renal clear cell carcinoma: a bioinformatical analysis. | Li, D., et al. 2022. Ann Transl Med. 10: 1235. PMID: 36544675
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Inhibitor of:
PDK1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
BX-912, 2 mg | sc-364451 | 2 mg | $124.00 | |||
BX-912, 5 mg | sc-364451A | 5 mg | $260.00 |