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S6 kinase&PKD-1

BX-912 (702674-56-4)

BX912 is a selective potent PDK1 inhibitor with IC50 of 12 nM. BX912 blocks PDK1/Akt signaling in tumor cells and suppresses the anchorage-dependent growth of avariety of tumor cell lines (such as PC-3 cells) in culture or induces apoptosis.

Not Intended for Therapeutic Use. For research use only.

CAS: 702674-56-4 Category

BX-912 (702674-56-4) Description:

3-Phosphoinositide-dependent protein kinase (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC.1 BX-912 is a potent, ATP-competitive inhibitor of PDK1 (IC50 = 26 nM). It less effectively inhibits a panel of related serine-threonine kinases.BX-912 has been used to evaluate the role of PDK1 in kinase activation and cell survival.

BX-912 (702674-56-4) Specifications:

Product Name BX-912
Synonym BX912; BX 912; BX912
Chemical Name N-(3-((4-((2-(1H-imidazol-4-yl)ethyl)amino)-5-bromopyrimidin-2-yl)amino)phenyl)pyrrolidine-1-carboxamide
Drug Class PDK1 inhibitor
Purity ≥98% (HPLC)
CAS Number 702674-56-4
Molecular Formula C20H23BrN8O
Molecular Weight 471.35
Monoisotopic Mass 470.118 g/mol
MDL number MFCD10565925
InChIKey DMMILYKXNCVKOJ-UHFFFAOYSA-N
InChi Code InChI=1S/C20H23BrN8O/c21-17-12-24-19(28-18(17)23-7-6-16-11-22-13-25-16)26-14-4-3-5-15(10-14)27-20(30)29-8-1-2-9-29/h3-5,10-13H,1-2,6-9H2,(H,22,25)(H,27,30)(H2,23,24,26,28)
SMILES O=C(N1CCCC1)NC2=CC=CC(NC3=NC=C(Br)C(NCCC4=CNC=N4)=N3)=C2
Form Powder
Color White solid
Solubility  Soluble in DMSO (93 mg/mL at 25 °C), water (<1 mg/mL at 25 °C), and ethanol (3 mg/mL at 25 °C).
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application PDK1 inhibitor

 


RIDADR NONH for all modes of transport

References:

[1]. Mashukova A, Forteza R, Wald FA, Salas PJ. PDK1 in apical signaling endosomes  participates in the rescue of the polarity complex atypical PKC by intermediate filaments in intestinal epithelia. Mol Biol Cell. 2012 May;23(9):1664-74. Epub 2012 Mar 7. PubMed PMID: 22398726; PubMed Central PMCID: PMC3338434.

[2]. Feldman, R.I., Wu, J.M., Polokoff, M.A., et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1 The Journal of Biological Chemisty 280(20), 19867-19874 (2005).

[3]. Kloo, B., Nagel, D., Pfeifer, M., et al. Critical role of PI3K signaling for NF-κB-dependent survival in a subset of activated B-cell-like diffuse large B-cell lymphoma cells Proceedings of the National Academy of Sciences of the United States of America 108(1), 272-277 (2011).

[4]. Mashukova, A., Forteza, R., Wald, F.A., et al. PDK1 in apical signaling endosomes participates in the rescue of the polarity complex atypical PKC by intermediate filaments in intestinal epithelia Molecular Biology of the Cell 23(9), 1664-1674 (2012).

[5]. Shibata, E., Kanno, T., Tsuchiya, A., et al. Free fatty acids inhibit protein tyrosine phosphatase 1B and activate Akt Cell Physiology and Biochemistry32(4), 871-879 (2013).