BX 795

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Cat.No. 4318 - BX 795 | C23H26IN7O2S | CAS No. 702675-74-9
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)
Datasheet
Citations (2)
Reviews
Literature (1)

Biological Activity

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

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 Data

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

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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

Feldman et al (2005) Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J.Biol.Chem. 280 19867 PMID: 15772071

Clark et al (2009) 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. 284 14136 PMID: 19307177

Tamguney et al (2008) Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cells. Exp.Cell Res. 314 2299 PMID: 18514190

Sutlu et al (2012) Inhibition of intracellular antiviral defense mechanisms augments lentiviral transduction of human natural killer cells: implications for gene therapy. Hum. Gene Ther. 23 1090 PMID: 22779406


If you know of a relevant reference for BX 795, please let us know.

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View all Phosphoinositide-dependent Kinase 1 Inhibitors

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2 Citations for BX 795

Citations are publications that use Tocris products. Selected citations for BX 795 include:

Pillai et al (2015) Tank binding kinase 1 is a centrosome-associated kinase necessary for microtubule dynamics and mitosis. Nat Commun 6 10072 PMID: 26656453

Johnson et al (2019) Aspirin inhibits platelets from reprogramming breast tumor cells and promoting metastasis. Blood Adv 3 198 PMID: 30670536


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Literature in this Area

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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases