LY 333531 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

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.

Background References

1. Effects of protein kinase C inhibitors on thromboxane production by thrombin-stimulated platelets.
   Samokhin et al.
   Eur.J.Pharmacol., 1999;386:297
2. Synthesis and Characterization of the Selective, Reversible PKC� Inhibitor (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, Ruboxistaurin (LY333531)
   Lewin et al.
   A.C.S.Chem.Neurosci., 2019;10:246
3. (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
4. Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCβ.
   Faul et al.
   Bioorg.Med.Chem.Lett., 2003;13:1857

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