Ruboxistaurin mesylate
Based on 14 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.87%
- No. CAS: 192050-59-2
- Fòrmula: C29H32N4O6S
- Peso molecular:564.65
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Almacenamiento:
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)
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Publications Citing Use of MedChemExpress (MCE) Ruboxistaurin mesylate
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) |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male long-evans rats with streptozotocin induced diabetes[4]
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Dosage:0.1, 1.0 and 10.0 mg/kg
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Administration:Oral administration; 0.1, 1.0 and 10.0 mg/kg, once daily for 4 weeks
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Result:Significantly decreased the number of leukocytes in the retinal microcirculation of rats with streptozotocin induced diabetes.
Chemical Information
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No. CAS 192050-59-2
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Appearance Solid
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Peso molecular 564.65
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Fòrmula C29H32N4O6S
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Color Orange to red
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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.CS(=O)(O)=O
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Synonyms
LY333531 mesylate
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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)
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 mesylate 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 mesylate 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 mesylate 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 mesylate 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 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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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 : 50 mg/mL (88.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (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 |
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| 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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