Ruboxistaurin (LY333531) HCl

Catalog No.S7663 Batch:S766301

Technical Data

Formula	C₂₈H₂₈N₄O₃.HCl
Molecular Weight	505.01	CAS No.	169939-93-9
Solubility (25°C)*	In vitro	DMSO	50 mg/mL (99.0 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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)	View More
4.7 nM	5.9 nM	0.052 μM	0.25 μM	0.3 μM	View More

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].

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].

Protocol (from reference)

Cell Assay:^{^[3]}	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.

Cell Assay:^{^[3]}

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.

References

Selleck's Ruboxistaurin (LY333531) HCl has been cited by 17 publications

Ginsenoside Rg1 attenuates diabetic vascular endothelial dysfunction by inhibiting the calpain-1/ROS/PKC-β axis [ Life Sci, 2023, 329:121972]	PubMed: 37482213
Dynamic Plasticity Systems Direct Early Adaptation to Treatment in Neuroblastoma [ bioRxiv, 2023, 10.1101/2023.12.07.570359]	PubMed: none
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization [ Cell Rep Methods, 2023, 3(10):100599]	PubMed: 37797618
Enhanced neutrophil extracellular trap formation in COVID-19 is inhibited by the protein kinase C inhibitor ruboxistaurin [ ERJ Open Res, 2022, 8(2)00596-2021]	PubMed: 35382002
Thioesterase superfamily member 1 undergoes stimulus-coupled conformational reorganization to regulate metabolism in mice [ Nat Commun, 2021, 12(1):3493]	PubMed: 34108467
Mechanism by which Huoxue Tongluo Qiwei Decoction improves the erectile function of rats with diabetic erectile dysfunction [ J Ethnopharmacol, 2021, 283:114674]	PubMed: 34560214
Essential role of protein kinase C βI in icariin-mediated protection against atherosclerosis [ J Pharm Pharmacol, 2021, rgab040]	PubMed: 33822184
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19]	PubMed: 32645325
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19]	PubMed: 32645325
circ-CBFB upregulates p66Shc to perturb mitochondrial dynamics in APAP-induced liver injury [ Cell Death Dis, 2020, 11(11):953]	PubMed: 33159035

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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