Overview

  • Product name

    BX-795, PDK1 inhibitor
  • Description

    PDK1 inhibitor. Potent TBK1 and IKKε inhibitor
  • Biological description

    PDK1 inhibitor. Potent TBK1 and IKKε inhibitor. Blocks PDK1/Akt signaling. Inhibits anchorage-dependent growth of tumor cells. Blocks phosphorylation, nuclear translocation, and transcriptional activity of interferon regulatory factor 3. Induces G2/M cell cycle arrest.
  • Purity

    > 97%
  • CAS Number

    702675-74-9
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    N-(3-(5-Iodo-4-(3-(thiophene-2-carboxamido)propylamino)pyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide
  • Molecular weight

    591.47
  • Molecular formula

    C23H26IN7O2S
  • PubChem identifier

    10077147
  • Storage instructions

    Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
  • Solubility overview

    Soluble in ethanol to 100 mM and in DMSO to 100 mM
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    C1CCN(C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)NCCCNC(=O)C4=CC=CS4)I
  • Source

    Synthetic

  • Research areas

References

This product has been referenced in:

  • Clark K  et al. Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IkappaB kinase epsilon: a distinct upstream kinase mediates Ser-172 phosphorylation and activation. J Biol Chem 284:14136-46 (2009). Read more (PubMed: 19307177) »
  • Tamgüney T  et al. Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cells. Exp Cell Res 314:2299-312 (2008). Read more (PubMed: 18514190) »
  • Feldman RI  et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem 280:19867-74 (2005). Read more (PubMed: 15772071) »

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