Home TGF-beta/Smad PKC inhibitor Ruboxistaurin (LY333531) HCl For research use only.

Ruboxistaurin (LY333531) HCl

Synonyms: Ruboxistaurin hydrochloride, LY333531 hydrochloride

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.

Ruboxistaurin (LY333531) HCl Chemical Structure

Ruboxistaurin (LY333531) HCl Chemical Structure

CAS No. 169939-93-9

Purity & Quality Control

Products often used together with Ruboxistaurin (LY333531) HCl

gp91ds-tat

Ruboxistaurin (LY333531) HCl and gp91ds-tat combined with therapeutic hypothermia substantially accelerate human brain microvascular endothelial cells (HBMEC) wound closure.

Kadir RRA, et al. Metab Brain Dis. 2021 Oct;36(7):1817-1832.

GLP-1 (7-37)

Ruboxistaurin HCl and GLP-1 (7-37) combination enhances the reduction of NOX4 expression via PKCβ inhibition.

Pujadas G, et al. Endocrine. 2016 Nov;54(2):396-410.

Ruboxistaurin (LY333531) HCl Related Products

Signaling Pathway

PKC Signaling Pathways

PKC Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLM13 Apoptosis assay Induction of apoptosis in human MOLM13 cells, IC50=0.7 μM 18077363
MV4-11 Apoptosis assay Induction of apoptosis in human MV4-11 cells, IC5=1.5 μM 18077363
endothelial cells Function assay Effective dose against plasminogen activator activity stimulated by phorbol ester in endothelial cells, ED50=7.5μM 8709095
MV4-11 Function assay 1 uM Reduction of BAD phosphorylation in human MV4-11 cells at 1 uM by Western blot 18077363
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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)		 Click to View More Targets
4.7 nM 5.9 nM 0.052 μM 0.25 μM 0.3 μM
In vitro
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AMPKα1 / AMPKα1 / p-MARCKS 27784766
In Vivo
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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00297401 Completed
Diabetes Mellitus Type 1
Chromaderm Inc.|Heart and Stroke Foundation of Canada
 March 2006 Phase 3
NCT00190970 Completed
Diabetic Neuropathy
Chromaderm Inc.
 October 2004 Phase 2
NCT00482976 Completed
Diabetes Mellitus
Chromaderm Inc.|Joslin Diabetes Center
 December 2003 Phase 2

Chemical Information & Solubility

Molecular Weight 505.01 Formula

C28H28N4O3.HCl
CAS No. 169939-93-9 SDF Download Ruboxistaurin (LY333531) HCl SDF
Smiles CN(C)CC1CCN2C=C(C3=CC=CC=C32)C4=C(C5=CN(CCO1)C6=CC=CC=C65)C(=O)NC4=O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (198.01 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Tech Support

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