1. Epigenetics
    TGF-beta/Smad
  2. PKC

Ruboxistaurin hydrochloride (Synonyms: LY 333531 hydrochloride)

Cat. No.: HY-10195B Purity: 98.88%
Handling Instructions

Ruboxistaurin hydrochloride 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).

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

Ruboxistaurin hydrochloride Chemical Structure

Ruboxistaurin hydrochloride Chemical Structure

CAS No. : 169939-93-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 253 In-stock
Estimated Time of Arrival: December 31
1 mg USD 60 In-stock
Estimated Time of Arrival: December 31
5 mg USD 228 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
25 mg USD 490 In-stock
Estimated Time of Arrival: December 31
50 mg USD 650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1050 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Top Publications Citing Use of Products

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

    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
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Ruboxistaurin hydrochloride 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).

    IC50 & Target[1]

    PKCβI

    4.7 nM (IC50)

    PKCβII

    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 hydrochloride 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].

    In Vivo

    Ruboxistaurin (LY333531; 1 mg/kg/d for 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 (LY333531; 0.1, 1.0, or 10.0 mg/kg/d, po.o.) dramatically reduces the number of leukocytes trapped in the retinal microcirculation of diabetic rats[4].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : 6.8 mg/mL (13.47 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9802 mL 9.9008 mL 19.8016 mL
    5 mM 0.3960 mL 1.9802 mL 3.9603 mL
    10 mM 0.1980 mL 0.9901 mL 1.9802 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [2]

    The second passages of human umbilical vein endothelial cells (HUVEC) are grown to confluence in microtiter plates coated with gelatin. The medium contains 5.5 mM glucose. If endothelial cells are stimulated with 27.7 mM glucose for 4 days, they are seeded in the well at a calibrated higher cell concentration in order to achieve comparable cell density at the day adhesion assays are performed. Therefore, cell density in the wells is tested thoroughly in control wells of each glucose concentration prior to monocyte adhesion assays. If Ruboxistaurin is used in this assay, it is added to the cultures for the whole period[2].

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

    Animal Administration
    [4]

    Rats[4]
    Leukocyte entrapment is evaluated only once after a 4-week diabetic period in both groups of rats with and without Ruboxistaurin treatment, using one eye (right eye) of each rat. Ruboxistaurin is administered orally at dosages of 0.1 (n = 8), 1.0 (n = 16), and 10.0 mg/kg/d (n = 8) for 4 weeks, from the time streptozotocin is injected in the rats. Immediately before acridine orange digital fluorography, rats are anesthetized with a mixture (1:1) of xylazine hydrochloride (4 mg/kg) and ketamine hydrochloride (10 mg/kg). The pupils are dilated with 0.5% tropicamide and 2.5% phenylephrine hydrochloride. A contact lens is placed on the cornea to maintain transparency throughout the experiments. Each rat has a catheter inserted into the tail vein and is placed on a movable platform. Body temperature is maintained between 37°C and 39°C throughout the experiment[4].

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

    References
    Molecular Weight

    505.01

    Formula

    C₂₈H₂₉ClN₄O₃

    CAS No.

    169939-93-9

    SMILES

    O=C1NC(C(C2=CN(C3=CC=CC=C32)CCO[[email protected]](CN(C)C)CC4)=C1C5=CN4C6=CC=CC=C56)=O.[H]Cl

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 98.88%

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    Product Name:
    Ruboxistaurin hydrochloride
    Cat. No.:
    HY-10195B
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    Ruboxistaurin hydrochloride

    Cat. No.: HY-10195B