Art. -Nr.: HY-10195

Ruboxistaurin

(Synonyms: LY333531)

14 Cited Publications

Kundenbewertung

Based on 14 publication(s) in Google Scholar

Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (K_i=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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.97%
CAS. Nr.: 169939-94-0
Formel: C₂₈H₂₈N₄O₃
Molecular Weight:468.55

Speicherung:

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

Ruboxistaurin Chemical Structure

CAS. Nr.: 169939-94-0

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle PKC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-13	IC₅₀	0.7 μM Compound: LY-333531	Induction of apoptosis in human MOLM13 cells Induction of apoptosis in human MOLM13 cells	[PMID: 18077363]
MV4-11	IC₅₀	1.5 μM Compound: LY-333531	Induction of apoptosis in human MV4-11 cells Induction of apoptosis in human MV4-11 cells	[PMID: 18077363]

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].

MedChemExpress (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].

MedChemExpress (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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 169939-94-0
Appearance Solid
Molecular Weight 468.55
Formel C₂₈H₂₈N₄O₃
Color Brown to reddish brown
SMILES

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

LY333531
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (14)

All WB

Sort by:

Journal Impact Factor

Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Acta Pharm Sin B

HBXIP blocks myosin-IIA assembly by phosphorylating and interacting with NMHC-IIA in breast cancer metastasis. [Abstract]

2023 Mar;13(3):1053-1070. PMID: 36970214
Adv Sci (Weinh)

Inhibition of Calcium-Dependent Lipid Droplets Relocation of ACSL4-PKCβ-ALOX15 Complex Alleviates Ferroptosis and Acute Pancreatitis. [Abstract]

2026 Apr;13(19):e15768. PMID: 41589658
Cell Biosci

Integrin αIIbβ3 outside-in signaling activates human platelets through serine 24 phosphorylation of Disabled-2. [Abstract]

2021 Feb 8;11(1):32. PMID: 33557943
ACS Omega

Machine Learning for Discovery of GSK3β Inhibitors. [Abstract]

2020 Oct 12;5(41):26551-26561. PMID: 33110983
PLoS Pathog

HCMV encoded UL84 hijacks FHL2 to suppress type I interferon production and enhance viral replication. [Abstract]

2026 Jan 26;22(1):e1013895. PMID: 41587224
Rheumatology (Oxford)

Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]

2025 Aug 13:keaf437. PMID: 40802538
Biosci Rep

Specific PKC βII inhibitor: one stone two birds in the treatment of diabetic foot ulcers. [Abstract]

2018 Sep 7;38(5):BSR20171459. PMID: 29440456

Ruboxistaurin 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
FASEB J

DNA hypomethylation of Syk induces oxidative stress and apoptosis via the PKCβ/P66shc signaling pathway in diabetic kidney disease. [Abstract]

2024 Mar 31;38(6):e23564. PMID: 38522019
Endocrinology

Inhibition of A-Type K+ Channels by Urotensin-II Induces Sensory Neuronal Hyperexcitability Through the PKCα-ERK Pathway. [Abstract]

2018 May 1;159(5):2253-2263. PMID: 29648633
Diabetes Metab Syndr Obes

Essential Role Of High Glucose-Induced Overexpression Of PKCβ And PKCδ In GLP-1 Resistance In Rodent Cardiomyocytes. [Abstract]

2019 Nov 4;12:2289-2302. PMID: 31807042
In Vitro Cell Dev Biol Anim

PKCβ expression contributes to M1 macrophage-induced impairment in the osteogenic differentiation of periodontal ligament stem cells. [Abstract]

2025 Jun;61(6):635-643. PMID: 40526258
bioRxiv

2024 June 29.
Trop J Pharm Res

2022; 21(12): 2508.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (53.36 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

THF : < 1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 1.67 mg/mL (3.56 mM); Suspended solution

This protocol yields a suspended solution of ≥ 1.67 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Jirousek MR, et al. (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. J Med Chem. 1996;39(14):2664-2671. [Content Brief]

[2]. Ruboxistaurin: LY 333531. Drugs R D. 2007;8(3):193-199. [Content Brief]

[3]. Kunt T, et al. The beta-specific protein kinase C inhibitor ruboxistaurin (LY333531) suppresses glucose-induced adhesion of human monocytes to endothelial cells in vitro. J Diabetes Sci Technol. 2007 Nov;1(6):929-35. [Content Brief]

[4]. Nonaka A, et al. PKC-beta inhibitor (LY333531) attenuates leukocyte entrapment in retinal microcirculation of diabetic rats. Invest Ophthalmol Vis Sci. 2000 Aug;41(9):2702-6. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	2.1342 mL	10.6712 mL	21.3424 mL	53.3561 mL
	5 mM	0.4268 mL	2.1342 mL	4.2685 mL	10.6712 mL
	10 mM	0.2134 mL	1.0671 mL	2.1342 mL	5.3356 mL
	15 mM	0.1423 mL	0.7114 mL	1.4228 mL	3.5571 mL
	20 mM	0.1067 mL	0.5336 mL	1.0671 mL	2.6678 mL
	25 mM	0.0854 mL	0.4268 mL	0.8537 mL	2.1342 mL
	30 mM	0.0711 mL	0.3557 mL	0.7114 mL	1.7785 mL
	40 mM	0.0534 mL	0.2668 mL	0.5336 mL	1.3339 mL
	50 mM	0.0427 mL	0.2134 mL	0.4268 mL	1.0671 mL

Keywords

Ruboxistaurin

14 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Ruboxistaurin

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Anti-diabetic Compound Library

Macrocyclic Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Neurodegenerative Disease-related Compound Library

Targeted Diversity Library

Human Metabolite Library

Cancer Stem Cells Compound Library

Coagulation and Anti-coagulation Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Ruboxistaurin

Alle PKC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ruboxistaurin Related Classifications

HY-10195 Related Classifications