Home TGF-beta/Smad PKC inhibitor Ruboxistaurin (LY333531) HCl

Ruboxistaurin (LY333531) HCl

Catalog No.S7663 Synonyms: Ruboxistaurin hydrochloride, LY333531 hydrochloride

For research use only.

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

CAS No. 169939-93-9

Selleck's Ruboxistaurin (LY333531) HCl has been cited by 12 Publications

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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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLM13 M{n6NmFxd3C2b4Ppd{Bie3OjeR?= MmfGTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCPT1zNNVMh[2WubIOsJGlEPTB;MD63JO69VQ>? NUnoclVERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwO|c{PjNpPkG4NFc4OzZ|PD;hQi=>
MV4-11 MljhRZBweHSxc3nzJIF{e2G7 MnnRTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCPVkStNVEh[2WubIOsJGlEPT1zLkWg{txO M3fXflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEe3N|Y{Lz5zOEC3O|M3OzxxYU6=
endothelial cells MlXLSpVv[3Srb36gZZN{[Xl? M4eydWVn\mWldHn2[UBld3OnIHHnZYlve3RicHzhd41qdm:pZX6gZYN1cX[jdH;yJIFkfGm4aYT5JJN1cW23bHH0[YQh[nlicHjvdoJwdCCnc4TldkBqdiCnbnTveIhmdGmjbDDj[YxteyxiRVS1NF04NjYQvF2= M{j6PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493Nzh5MEmwPVUoRjh5MEmwPVU9N2F-
MV4-11 MkT6SpVv[3Srb36gZZN{[Xl? NWrndmIxOSC3TR?= M2\NTHJm\HWldHnvckBw\iCEQVSgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF3WOE0yOSClZXzsd{BifCBzIIXNJIJ6KFenc4Tldo4h[myxdB?= M{PLb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEe3N|Y{Lz5zOEC3O|M3OzxxYU6=
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot p-AMPKα1 / AMPKα1 / p-MARCKS 27784766
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 Research:[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.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 505.01
Formula

C28H28N4O3.HCl
CAS No. 169939-93-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)CC1CCN2C=C(C3=CC=CC=C32)C4=C(C5=CN(CCO1)C6=CC=CC=C65)C(=O)NC4=O.Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00297401 Completed Drug: ruboxistaurin|Drug: placebo Diabetes Mellitus Type 1 Chromaderm Inc.|Heart and Stroke Foundation of Canada March 2006 Phase 3
NCT00190970 Completed Drug: Ruboxistaurin Diabetic Neuropathy Chromaderm Inc. October 2004 Phase 2
NCT00482976 Completed Drug: Ruboxistaurin|Drug: Placebo Diabetes Mellitus Chromaderm Inc.|Joslin Diabetes Center December 2003 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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