A PKCβ inhibitor
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LY333531 (hydrochloride)

Item No. 13964

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(9S)-[(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, monohydrochloride
CAS Number
169939-93-9
Synonyms
  • Ruboxistaurin
Molecular Formula
C28H28N4O3 • HCl
Formula Weight
505.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/ml
SMILES
O=C(N1)C(C2=CN(CC[C@H]3CN(C)C)C4=C2C=CC=C4)=C(C5=CN(CCO3)C6=C5C=CC=C6)C1=O.Cl
InChi Code
InChI=1S/C28H28N4O3.ClH/c1-30(2)15-18-11-12-31-16-21(19-7-3-5-9-23(19)31)25-26(28(34)29-27(25)33)22-17-32(13-14-35-18)24-10-6-4-8-20(22)24;/h3-10,16-18H,11-15H2,1-2H3,(H,29,33,34);1H/t18-;/m0./s1
InChi Key
NYQIEYDJYFVLPO-FERBBOLQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $117

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    Product Description

    LY333531 is an inhibitor of PKCβ (IC50s = 4.7 and 5.9 nM for PKCβ1 and PKCβ2, respectively).1 It is selective for PKCβ1 and PKCβ2 over PKCα, -γ, -δ, -ε, -ζ, and -η (IC50s = 360, 300, 250, >100,000, and 52 nM, respectively). LY333531 also inhibits glycogen synthase kinase 3β (GSK3β; IC50 = 39.4 nM).2 It inhibits neutrophil extracellular trap (NET) formation induced by phorbol 12-myristate 13-acetate (PMA; Item No. 10008014) in primary human neutrophils when used at a concentration of 1 µM.3 LY333531 increases the mechanical nociceptive threshold in a rat model of diabetic hyperalgesia induced by streptozotocin (STZ; Item No. 13104).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jirousek, M.R., Gillig, J.R., Gonzalez, C.M., et al. (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 selective inhibitors of protein kinase Cβ. J. Med. Chem. 39(14), 2664-2671 (1996).

    2. Vignaux, P.A., Minerali, E., Foil, D.H., et al. Machine learning for discovery of GSK3b inhibitors. ACS Omega 5(41), 26551-26561 (2020).

    3. Gray, R.D., Lucas, C.D., MacKellar, A., et al. Activation of conventional protein kinase C (PKC) is critical in the generation of human neutrophil extracellular traps. J. Inflamm. (Lond) 10(1), 12 (2013).

    4. Kim, H., Sasaki, T., Maeda, K., et al. Protein kinase Cβ selective inhibitor LY333531 attenuates diabetic hyperalgesia through ameliorating cGMP level of dorsal root ganglion neurons. Diabetes 52(8), 2102-2109 (2019).