Ruboxistaurin hydrochloride

SKU: orb1693357

Description

Ruboxistaurin hydrochloride

Research Area

Epigenetics & Chromatin, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 169939-93-9
• MW: 505.01
• Purity: 95.97% (May vary between batches)
• Formula: C₂₈H₂₈N₄O₃·HCl
• SMILES: Cl.CN(C)CC1CCn2cc(C3=C(C(=O)NC3=O)c3cn(CCO1)c1ccccc31)c1ccccc21
• Target: PKC
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:1 mg/mL (1.98 mM);DMSO:55 mg/mL (108.91 mM)

Bioactivity

• Target IC50:
  PKCη:0.052 μM|PKCβ2:5.9 nM|PKCδ:0.25 μM|PKCγ:0.3 μM|PKCβ1:4.7 nM|PKCα:360 nM|PKCε:600 nM
• In Vivo:
  A significant up-regulation of TGF-b1, Smad2 and Smad3 mRNA expression was observed in diabetic rats, which was alleviated by administration of ruboxistaurin.
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• In Vitro:
  Ruboxistaurin strikingly decreases the chance of HUVEC survival and the effect of Ruboxistaurin 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, Ruboxistaurin reduces the ratio of Bcl-2/Bax. Ruboxistaurin 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.
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• Cell Research:
  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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PKC, PKCβ2, PKCγ, PKCβ1, PKCδ, PKCη, LY 333531, LY 333531 hydrochloride, LY333531, LY-333531, LY333531 HCl, LY333531 Hydrochloride, LY-333531 Hydrochloride

Compound Identifiers

PubChem CID

9892365