Ruboxistaurin HCl (LY333531 HCl)

For research use only.

Catalog No.S7663 Synonyms: Ruboxistaurin hydrochloride, LY333531 hydrochloride

4 publications

Ruboxistaurin HCl (LY333531 HCl) Chemical Structure

Molecular Weight(MW): 505.01

Ruboxistaurin HCl (LY333531 HCl) is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively.

Size Price Stock Quantity  
EUR 95 In stock
EUR 223 In stock
EUR 881 In stock
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Ruboxistaurin HCl (LY333531 HCl) has been cited by 4 publications

Purity & Quality Control

Choose Selective PKC Inhibitors

Biological Activity

Description Ruboxistaurin HCl (LY333531 HCl) is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively.
Targets
PKCβ1 [1]
(Cell-free assay)		 PKCβ2 [1]
(Cell-free assay)		 PKCη [1]
(Cell-free assay)		 PKCδ [1]
(Cell-free assay)		 PKCγ [1]
(Cell-free assay)
4.7 nM 5.9 nM 0.052 μM 0.25 μM 0.3 μM
In vitro

LY333531 strikingly decreases the chance of HUVEC survival and the effect of LY333531 on apoptotic cell death in HUVEC significantly increases compared with the AGEs group. Blockade of PKC-beta up-regulates the expression of Bax and Bad proteins and down-regulates the expression of Bcl-2 protein. Moreover, LY333531 reduces the ratio of Bcl-2/Bax. LY333531 can further prompt AGEs-induced endothelial cells apoptosis. The increased expression of Bax, Bad and decreased expression of Bcl-2 and Bcl-2/Bax ratio are associated with the apoptotic process[3].
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLM13 NGfSS5hCeG:ydH;zbZMh[XO|YYm= NWH4bGhlUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDNU2xOOTNiY3XscJMtKEmFNUC9NE44KM7:TR?= MnfBNVgxPzd|NkO=
MV4-11 NUDiVG9mSXCxcITvd4l{KGG|c3H5 M{[wc2lv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iTW[0MVEyKGOnbHzzMEBKSzV;MT61JO69VQ>? MU[xPFA4PzN4Mx?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-AMPKα1 / AMPKα1 / p-MARCKS ; 

PubMed: 27784766     


HUVECs were pre-treated with the indicated concentrations of LY333531 for 1 h prior to stimulation with VEGF (10 ng/ml, 5 min) or PMA (1 µmol/l, 20 min). Cell lysates were prepared and analysed by immunoblotting with the antibodies indicated.

27784766
In vivo LY333531 treatment (for a duration of 4 weeks) prevents excessive PKCb2 activation and attenuates cardiac diastolic dysfunction in rats with streptozotocin-induced diabetes. LY333531 suppresses the decreased expression of myocardial NO, Cav-3, phosphorylated (p)-Akt, and p-eNOS and also mitigates the augmentation of O2-, nitrotyrosine, Cav-1, and iNOS expression[2].

Protocol

Cell Research:[3]
- Collapse
  • Cell lines: Human umbilical vein endothelial cell (HUVEC)
  • Concentrations: 200 nM
  • Incubation Time: 48 h
  • Method: HUVECs are seeded into 96-well plates in low glucose DMEM with 10% FBS for 12 h. Afterwards, HUVECs are starved for 12 h and incubated with BSA (200 μg/ml), AGEs (200 μg/ml) and LY333531 (200 nM)+AGEs (200 μg/ml) for 48 h. Then, the medium is replaced with 0.5 mg/ml MTT and at 37 ◦C in a 95% air/5% CO2 incubator for 4 h. Finally, the medium containing MTT is aspirated and replaced by dimethyl sulphoxide (DMSO). OD is measured with a Microplate spectrophotometer. AGEs:advanced glycation end products.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 50 mg/mL (99.0 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 505.01
Formula

C28H28N4O3.HCl
CAS No. 169939-93-9
Storage powder
in solvent
Synonyms Ruboxistaurin hydrochloride, LY333531 hydrochloride
Smiles CN(C)CC1CCN2C=C(C3=CC=CC=C32)C4=C(C5=CN(CCO1)C6=CC=CC=C65)C(=O)NC4=O.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00297401 Completed Drug: ruboxistaurin|Drug: placebo Diabetes Mellitus Type 1 Chromaderm Inc.|Heart and Stroke Foundation of Canada March 2006 Phase 3
NCT00190970 Completed Drug: Ruboxistaurin Diabetic Neuropathy Chromaderm Inc. October 2004 Phase 2
NCT00482976 Completed Drug: Ruboxistaurin|Drug: Placebo Diabetes Mellitus Chromaderm Inc.|Joslin Diabetes Center December 2003 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field
selleck catalog

PKC Signaling Pathway Map

Related PKC Products

  • SD-208 New

    SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.

  • LDN-214117 New

    LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.

  • Staurosporine

    Staurosporine (CGP 41251) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.

  • Sotrastaurin

    Sotrastaurin (AEB071) is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay; inactive to PKCζ. Phase 2.

    Features:Unlike former PKC inhibitors, Sotrastaurin does not enhance apoptosis of murine T-cell blasts in a model of activation-induced cell death.

  • Go 6983

    Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ.

  • Enzastaurin (LY317615)

    Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM in cell-free assays, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3.

  • Bisindolylmaleimide I (GF109203X)

    Bisindolylmaleimide I (GF109203X) is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor.

    Features:Greater selectivity than PKC inhibitor staurosporine. GF109203X is a chemical probe for studying PKC signal transduction pathways. Potential for use in a variety of cancers.

  • Go6976

    Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.

  • Bisindolylmaleimide IX (Ro 31-8220 Mesylate)

    Bisindolylmaleimide IX (Ro 31-8220 Mesylate) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively, and also shows potent inhibition against MAPKAP-K1b, MSK1, GSK3β and S6K1.

Tags: buy Ruboxistaurin HCl (LY333531 HCl) | Ruboxistaurin HCl (LY333531 HCl) supplier | purchase Ruboxistaurin HCl (LY333531 HCl) | Ruboxistaurin HCl (LY333531 HCl) cost | Ruboxistaurin HCl (LY333531 HCl) manufacturer | order Ruboxistaurin HCl (LY333531 HCl) | Ruboxistaurin HCl (LY333531 HCl) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID