BX 795

Name: BX 795
Brand: Tocris Bioscience
SKU: 4318

Tocris Bioscience, part of Bio-Techne | Catalog # 4318

Citations (16)

COA / SDS

PDPK1 (PDK1) inhibitor

Key Product Details

Description:	PDPK1 (PDK1) inhibitor
Chemical Name:	N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	591.47

View Full Technical Details for BX 795

Technical Data
Citations

Biological Activity for BX 795

BX 795 is an inhibitor of 3-phosphoinositide-dependent kinase 1 (PDPK1). Inhibits Akt phosphorylation at Thr308 in PC3 cells; also inhibits anchorage-independent growth of PC3 and MDA-MB-468 cells. Exhibits activity at other kinases, including TANK-binding kinase 1 (TBK1), Aurora B and IκB kinase ε (IKKε). Also enhances lentiviral transduction of natural killer (NK) cells by around 3.8-fold.

Technical Data for BX 795

M. Wt	591.47
Formula	C₂₃H₂₆IN₇O₂S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	702675-74-9
PubChem ID	10077147
InChi Key	VAVXGGRQQJZYBL-UHFFFAOYSA-N
Smiles	IC1=C(NCCCNC(C4=CC=CS4)=O)N=C(NC2=CC(NC(N3CCCC3)=O)=CC=C2)N=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for BX 795

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	59.15	100
	ethanol	59.15	100

Preparing Stock Solutions for BX 795

The following data is based on the product molecular weight 591.47.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.69 mL	8.45 mL	16.91 mL
5 mM	0.34 mL	1.69 mL	3.38 mL
10 mM	0.17 mL	0.85 mL	1.69 mL
50 mM	0.03 mL	0.17 mL	0.34 mL

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References for BX 795

References are publications that support the biological activity of the product.

Sutlu Inhibition of intracellular antiviral defense mechanisms augments lentiviral transduction of human natural killer cells: implications for gene therapy. Hum. Gene Ther. 2012 PMID: 22779406
Clark Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IκB kinase ε: a distinct upstream kinase mediates Ser-172 phosphorylation and activati J.Biol.Chem. 2009 PMID: 19307177
Tamguney Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cells. Exp.Cell Res. 2008 PMID: 18514190
Feldman Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J.Biol.Chem. 2005 PMID: 15772071