1. Epigenetics
    TGF-beta/Smad
  2. PKC
  3. Ruboxistaurin

Ruboxistaurin (Synonyms: LY333531)

Cat. No.: HY-10195 Purity: 98.03%
Handling Instructions

Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin inhibits PKC beta II with an IC50 of 5.9 nM.

For research use only. We do not sell to patients.

Ruboxistaurin Chemical Structure

Ruboxistaurin Chemical Structure

CAS No. : 169939-94-0

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5 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Ruboxistaurin:

Top Publications Citing Use of Products

    Ruboxistaurin purchased from MCE. Usage Cited in: Biosci Rep. 2018 Sep 7;38(5):BSR20171459.

    Western blots analysis showing protein expression level of phosphorylated p-PKC βII over total PKC βII and total H3Cit over total H3 in wounds 12 days post wounding
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    Description

    Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin inhibits PKC beta II with an IC50 of 5.9 nM[1][2].

    IC50 & Target[1]

    PKC-βI

    4.7 nM (IC50)

    PKC-βII

    5.9 nM (IC50)

    PKCη

    52 nM (IC50)

    PKCδ

    250 nM (IC50)

    PKCγ

    300 nM (IC50)

    PKCα

    360 nM (IC50)

    PKCε

    600 nM (IC50)

    In Vitro

    Ruboxistaurin is a selective and ATP-competitive PKCβ inhibitor, with IC50s of 4.7 and 5.9 nM for PKCβI and PKCβII, shows less potent inhibition on PKCη (IC50, 52 nM), PKCα (IC50, 360 nM), PKCγ (IC50, 300 nM), PKCδ (IC50, 250 nM), and has no effect on PKCζ (IC50, >100 μM)[1]. Ruboxistaurin (10 and 400 nM) dramatically inhibits glucose-induced monocyte adherence to levels that are not different from baseline adherence of monocytes to endothelial cells under NG conditions. Ruboxistaurin (10 and 400 nM) dose not alter the endothelial expression of adhesion molecules or modify endothelial cell growth[2]. Ruboxistaurin (LY333531; 10 nM) reduces high-glucose (HG)-induced human renal glomerular endothelial cells (HRGECs) viability, and inhibits the increases in swiprosin-1 in HRGECs incubated with HG[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Ruboxistaurin (1 mg/kg; 8 weeks) markedly reduces GEC apoptosis as well as swiprosin-1 upregulation, and ameliorates renal glomerular injury in the diabetic mice. Ruboxistaurin also potently attenuates the expression of PARP, cleaved-caspase9, cleaved-caspase3, and the Bax/Bcl-2 ratio, in diabetic mice[3]. Ruboxistaurin (0.1, 1.0, or 10.0 mg/kg; p.o.) dramatically reduces the number of leukocytes trapped in the retinal microcirculation of diabetic rats[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Rats[4]
    Dosage: 0.1, 1.0, or 10.0 mg/kg
    Administration: P.o.
    Result: Dramatically reduced the number of leukocytes trapped in the retinal microcirculation of diabetic rats.
    Molecular Weight

    468.55

    Formula

    C₂₈H₂₈N₄O₃

    CAS No.
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (106.71 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1342 mL 10.6712 mL 21.3424 mL
    5 mM 0.4268 mL 2.1342 mL 4.2685 mL
    10 mM 0.2134 mL 1.0671 mL 2.1342 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Ruboxistaurin
    Cat. No.:
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