Ruboxistaurin hydrochloride
Based on 14 publication(s) in Google Scholar
Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 169939-93-9
- Formula: C28H29ClN4O3
- Molecular Weight:505.01
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Ruboxistaurin hydrochloride
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
Biological Activity
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PKCβI 4.7 nM (IC50) |
PKCβII 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 hydrochloride 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.
Chemical Information
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CAS No. 169939-93-9
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Appearance Solid
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Molecular Weight 505.01
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Formula C28H29ClN4O3
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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.[H]Cl
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Synonyms
LY333531 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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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Solvent & Solubility
DMSO : 25 mg/mL (49.50 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)
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). 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). 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: ≥ 2.5 mg/mL (4.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.95 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Protocol
The second passages of human umbilical vein endothelial cells (HUVEC) are grown to confluence in microtiter plates coated with gelatin. The medium contains 5.5 mM glucose. If endothelial cells are stimulated with 27.7 mM glucose for 4 days, they are seeded in the well at a calibrated higher cell concentration in order to achieve comparable cell density at the day adhesion assays are performed. Therefore, cell density in the wells is tested thoroughly in control wells of each glucose concentration prior to monocyte adhesion assays. If Ruboxistaurin is used in this assay, it is added to the cultures for the whole period[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[4]
Leukocyte entrapment is evaluated only once after a 4-week diabetic period in both groups of rats with and without Ruboxistaurin treatment, using one eye (right eye) of each rat. Ruboxistaurin is administered orally at dosages of 0.1 (n = 8), 1.0 (n = 16), and 10.0 mg/kg/d (n = 8) for 4 weeks, from the time streptozotocin is injected in the rats[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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). 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 | 1.9802 mL | 9.9008 mL | 19.8016 mL | 49.5040 mL |
| 5 mM | 0.3960 mL | 1.9802 mL | 3.9603 mL | 9.9008 mL | |
| 10 mM | 0.1980 mL | 0.9901 mL | 1.9802 mL | 4.9504 mL | |
| 15 mM | 0.1320 mL | 0.6601 mL | 1.3201 mL | 3.3003 mL | |
| 20 mM | 0.0990 mL | 0.4950 mL | 0.9901 mL | 2.4752 mL | |
| 25 mM | 0.0792 mL | 0.3960 mL | 0.7921 mL | 1.9802 mL | |
| 30 mM | 0.0660 mL | 0.3300 mL | 0.6601 mL | 1.6501 mL | |
| 40 mM | 0.0495 mL | 0.2475 mL | 0.4950 mL | 1.2376 mL |
Ruboxistaurin hydrochloride Related Classifications
HY-10195B Related Classifications
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