Catalog Number: 4738
Alternate Names: Ruboxistaurin
Chemical Name: (9S)-9-[(Dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione hydrochloride
Biological Activity
Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50 values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src).
Technical Data
  • M.Wt:
    505.01
  • Formula:
    C28H28N4O3.HCl
  • Solubility:
    Soluble to 20 mM in DMSO
  • Storage:
    Store at -20°C
  • CAS No:
    169939-93-9
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16,21-dimetheno-1H,13H-dibenzo[e,k]]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-dione (LY333531) and related analogues: isozyme selec
    Jirousek et al.
    J.Med.Chem., 1996;39:2664
  2. Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCβ.
    Faul et al.
    Bioorg.Med.Chem.Lett., 2003;13:1857
  3. Effects of protein kinase C inhibitors on thromboxane production by thrombin-stimulated platelets.
    Samokhin et al.
    Eur.J.Pharmacol., 1999;386:297
Citations:

The citations listed below are publications that use Tocris products. Selected citations for LY 333531 hydrochloride include:

2 Citations: Showing 1 - 2
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  1. N-cadherin adhesive interactions modulate matrix mechanosensing and fate commitment of mesenchymal stem cells.
    Authors: Cosgrove
    Nature Materials 2016;15:1297
  2. Targeting a cell state common to triple-negative breast cancers.
    Authors: Muellner Et al.
    ASN Neuro 2015;11:789

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