Ruboxistaurin
Based on 14 publication(s) in Google Scholar
Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.97%
- No. CAS: 169939-94-0
- Fòrmula: C28H28N4O3
- Peso molecular:468.55
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Ruboxistaurin
More- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Acta Pharm Sin B. 2023 Mar;13(3):1053-1070. [Abstract]
- Adv Sci (Weinh). 2026 Apr;13(19):e15768. [Abstract]
- Cell Biosci. 2021 Feb 8;11(1):32. [Abstract]
- ACS Omega. 2020 Oct 12;5(41):26551-26561. [Abstract]
- PLoS Pathog. 2026 Jan 26;22(1):e1013895. [Abstract]
- Rheumatology (Oxford). 2025 Aug 13:keaf437. [Abstract]
- Biosci Rep. 2018 Sep 7;38(5):BSR20171459. [Abstract]
- FASEB J. 2024 Mar 31;38(6):e23564. [Abstract]
- Endocrinology. 2018 May 1;159(5):2253-2263. [Abstract]
- Diabetes Metab Syndr Obes. 2019 Nov 4:12:2289-2302. [Abstract]
- In Vitro Cell Dev Biol Anim. 2025 Jun;61(6):635-643. [Abstract]
- bioRxiv. 2024 June 29.
- Trop J Pharm Res. 2022; 21(12): 2508.
Customer Validation & Images
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IF
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WB
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Histological Imaging/Staining
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IP
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WB
Actividad biológica
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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) |
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Cell Line
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Type | Value | Description | References |
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| MOLM-13 | IC50 |
0.7 μM
Compound: LY-333531
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Induction of apoptosis in human MOLM13 cells
Induction of apoptosis in human MOLM13 cells
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[PMID: 18077363] |
| MV4-11 | IC50 |
1.5 μM
Compound: LY-333531
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Induction of apoptosis in human MV4-11 cells
Induction of apoptosis in human MV4-11 cells
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[PMID: 18077363] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[4]
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Dosage:0.1, 1.0, or 10.0 mg/kg
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Administration:P.o.
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Result:Dramatically reduced the number of leukocytes trapped in the retinal microcirculation of diabetic rats.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 169939-94-0
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Appearance Solid
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Peso molecular 468.55
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Fòrmula C28H28N4O3
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Color Brown to reddish brown
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SMILES
O=C1NC(C(C2=CN(C3=CC=CC=C32)CCO[C@H](CN(C)C)CC4)=C1C5=CN4C6=CC=CC=C56)=O
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Synonyms
LY333531
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (14)
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Journal Impact Factor
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Most Recent
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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
Ruboxistaurin purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Mar;13(3):1053-1070. [Abstract]
The spatial distribution patterns of NMHC-IIA (red) and nuclei (DAPI) were detected in the indicated stable cells transiently treated with si-PKCβII or 10 μmol/L LY333531 by IF.
Ruboxistaurin purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Mar;13(3):1053-1070. [Abstract]
WB analysis showed Triton X-insoluble fractions of the stable cells transiently treated with si-PKCβII or 10 μmol/L LY333531 (left panel) and quantification of the relation to the total lysate group (right panel).
Ruboxistaurin purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Mar;13(3):1053-1070. [Abstract]
H&E and IHC staining of metastatic foci in lung paraffin sections from tail vein-injected BALB/c nude mice (n = 8) with MCF-7 or MCF-7-OE-HBXIP cells for 55 days treated with saline or LY333531 (10 μM).
Ruboxistaurin purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Mar;13(3):1053-1070. [Abstract]
Co-IP analysis of the phosphorylation level of Flag-EATR. Before treatment with 10 μmol/L LY333531 for 24 h.
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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
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
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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 -
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Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (281 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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. 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 |
Ruboxistaurin Related Classifications
HY-10195 Related Classifications
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