2. Epigenetics TGF-beta/Smad
  3. PKC
  4. Ruboxistaurin mesylate

Ruboxistaurin mesylate  (Synonyms: LY333531 mesylate)

Cat. No.: HY-10195A Purity: 99.87%
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Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes.

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

Ruboxistaurin mesylate Chemical Structure

Ruboxistaurin mesylate Chemical Structure

CAS No. : 192050-59-2

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 248 In-stock
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10 mM * 1 mL in DMSO USD 248 In-stock
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10 mg USD 350 In-stock
25 mg USD 700 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Ruboxistaurin mesylate:

Ruboxistaurin mesylate Related Antibodies

Top Publications Citing Use of Products

    Ruboxistaurin mesylate purchased from MedChemExpress. Usage Cited in: Biosci Rep. 2018 Sep 7;38(5):BSR20171459.  [Abstract]

    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) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes[1][2][3][4].

    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 mesylate inhibits PKC isozymes with IC50 values of 0.36, 0.0047, 0.0059, 0.30, 0.25, 0.60 and 0.052 μM for PKCα, PKCβI, PKCβII, PKCγ, PKCδ, PKCε and PKCη, respectively[1].
    Ruboxistaurin mesylate inhibits Ca calmodulin and Rat Brain PKC with IC50 values of 6.2 and 0.32 μM, respectively[1].
    Ruboxistaurin mesylate (10 and 400 nM; 4 days) significantly suppresses glucose-induced monocyte adherence under normoglycemic (NG) conditions[3].

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

    Ruboxistaurin mesylate Related Antibodies
    In Vivo

    Ruboxistaurin mesylate (0.1, 1.0 and 10.0 mg/kg; oral administration, once daily for 4 weeks) decreases the increasing of leukocyte entrapment in the retinal microcirculation during the early diabetes period[4].

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

    Animal Model: Male long-evans rats with streptozotocin induced diabetes[4]
    Dosage: 0.1, 1.0 and 10.0 mg/kg
    Administration: Oral administration; 0.1, 1.0 and 10.0 mg/kg, once daily for 4 weeks
    Result: Significantly decreased the number of leukocytes in the retinal microcirculation of rats with streptozotocin induced diabetes.
    Clinical Trial
    Molecular Weight

    564.65

    Formula

    C29H32N4O6S
    CAS No.
    Appearance

    Solid

    Color

    Orange to red

    SMILES

    O=C1NC(C(C2=CN(C3=CC=CC=C32)CCO[C@H](CN(C)C)CC4)=C1C5=CN4C6=CC=CC=C56)=O.CS(=O)(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (88.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7710 mL 8.8550 mL 17.7101 mL
    5 mM 0.3542 mL 1.7710 mL 3.5420 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7710 mL 8.8550 mL 17.7101 mL 44.2752 mL
    5 mM 0.3542 mL 1.7710 mL 3.5420 mL 8.8550 mL
    10 mM 0.1771 mL 0.8855 mL 1.7710 mL 4.4275 mL
    15 mM 0.1181 mL 0.5903 mL 1.1807 mL 2.9517 mL
    20 mM 0.0886 mL 0.4428 mL 0.8855 mL 2.2138 mL
    25 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.7710 mL
    30 mM 0.0590 mL 0.2952 mL 0.5903 mL 1.4758 mL
    40 mM 0.0443 mL 0.2214 mL 0.4428 mL 1.1069 mL
    50 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.8855 mL
    60 mM 0.0295 mL 0.1476 mL 0.2952 mL 0.7379 mL
    80 mM 0.0221 mL 0.1107 mL 0.2214 mL 0.5534 mL
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    Ruboxistaurin mesylate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Ruboxistaurin192050-59-2LY333531LY 333531LY-333531PKCProtein kinase CselectivePKCβIATPdependentcompetitivePKCβIIInhibitorinhibitorinhibit

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