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Ruboxistaurin (LY333531) HCl

Name: Ruboxistaurin (LY333531) HCl
Brand: Selleck Chemicals
SKU: S7663
Rating: 5 (20 reviews)

Synonyms: Ruboxistaurin hydrochloride, LY333531 hydrochloride

Catalog No.S7663 Purity:99.65%

Ruboxistaurin (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.

Ruboxistaurin (LY333531) HCl Chemical Structure

CAS No. 169939-93-9

Purity & Quality Control

Batch: Purity: 99.65%

99.65

Products often used together with Ruboxistaurin (LY333531) HCl

gp91ds-tat

Ruboxistaurin (LY333531) HCl and gp91ds-tat combined with therapeutic hypothermia substantially accelerate human brain microvascular endothelial cells (HBMEC) wound closure.

Kadir RRA, et al. Metab Brain Dis. 2021 Oct;36(7):1817-1832.

GLP-1 (7-37)

Ruboxistaurin HCl and GLP-1 (7-37) combination enhances the reduction of NOX4 expression via PKCβ inhibition.

Pujadas G, et al. Endocrine. 2016 Nov;54(2):396-410.

Ruboxistaurin (LY333531) HCl Related Products

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Signaling Pathway

PKC Signaling Pathway

Cell Data

Cell Lines	Assay Type	Concentration	Activity Description	PMID
MOLM13	Apoptosis assay		Induction of apoptosis in human MOLM13 cells, IC50=0.7 μM	18077363
MV4-11	Apoptosis assay		Induction of apoptosis in human MV4-11 cells, IC5=1.5 μM	18077363
endothelial cells	Function assay		Effective dose against plasminogen activator activity stimulated by phorbol ester in endothelial cells, ED50=7.5μM	8709095
MV4-11	Function assay	1 uM	Reduction of BAD phosphorylation in human MV4-11 cells at 1 uM by Western blot	18077363
Click to View More Cell Line Experimental Data

Biological Activity

Description

Ruboxistaurin (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)	Click to View More Targets
4.7 nM	5.9 nM	0.052 μM	0.25 μM	0.3 μM	Click to View More Targets

In vitro
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 Research	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.
Experimental Result Images	Methods	Biomarkers	Images	PMID
Experimental Result Images	Western blot	p-AMPKα1 / AMPKα1 / p-MARCKS		27784766

In Vivo
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].

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00297401	Completed	Diabetes Mellitus Type 1	Chromaderm Inc.\|Heart and Stroke Foundation of Canada	March 2006	Phase 3
NCT00190970	Completed	Diabetic Neuropathy	Chromaderm Inc.	October 2004	Phase 2
NCT00482976	Completed	Diabetes Mellitus	Chromaderm Inc.\|Joslin Diabetes Center	December 2003	Phase 2

References

Chemical Information & Solubility

Molecular Weight	505.01	Formula	C₂₈H₂₈N₄O₃.HCl
CAS No.	169939-93-9	SDF	Download Ruboxistaurin (LY333531) HCl SDF
Smiles	CN(C)CC1CCN2C=C(C3=CC=CC=C32)C4=C(C5=CN(CCO1)C6=CC=CC=C65)C(=O)NC4=O.Cl
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (198.01 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

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:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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