Ruboxistaurin (LY333531 HCl)

Catalog No.S7663 Synonyms: Ruboxistaurin

Ruboxistaurin (LY333531 HCl) Chemical Structure

Molecular Weight(MW): 505.01

LY333531 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.

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Biological Activity

Description LY333531 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)
4.7 nM 5.9 nM 0.052 μM 0.25 μM 0.3 μM
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

Cell Research:[3]
+ Expand
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 50 mg/mL (99.0 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 505.01
Formula

C28H28N4O3.HCl

CAS No. 169939-93-9
Storage powder
in solvent
Synonyms Ruboxistaurin

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02769611 Recruiting Heart Failure Children''s Hospital Medical Center Cincinnati|The Christ Hospital June 28 2017 Phase 1|Phase 2
NCT02769611 Recruiting Heart Failure Children''s Hospital Medical Center Cincinnati|The Christ Hospital June 28 2017 Phase 1|Phase 2
NCT00297401 Completed Diabetes Mellitus Type 1 Chromaderm Inc.|Heart and Stroke Foundation of Canada March 2006 Phase 3
NCT00297401 Completed Diabetes Mellitus Type 1 Chromaderm Inc.|Heart and Stroke Foundation of Canada March 2006 Phase 3
NCT00266695 Completed Diabetic Retinopathy Chromaderm Inc. January 2006 Phase 3
NCT00266695 Completed Diabetic Retinopathy Chromaderm Inc. January 2006 Phase 3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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PKC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID