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Ruboxistaurin hydrochloride

Catalog No. T3689 CAS 169939-93-9

Synonyms: Ruboxistaurin, LY333531 HCl, LY 333531 hydrochloride

Ruboxistaurin hydrochloride (LY 333531 hydrochloride) is an Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50values are 0.052, 0.25, 0.30, 0.36, 0.60 and <100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src).

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Ruboxistaurin hydrochloride Chemical Structure

Ruboxistaurin hydrochloride, CAS 169939-93-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 65.00
2 mg	In stock	$ 94.00
5 mg	In stock	$ 159.00
10 mg	In stock	$ 270.00
25 mg	In stock	$ 540.00
50 mg	In stock	$ 779.00
100 mg	In stock	$ 1,090.00
500 mg	In stock	$ 2,180.00
1 mL * 10 mM (in DMSO)	In stock	$ 212.00

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Purity: 99.22%

Purity: 98.44%

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Storage & Solubility Information

Description	Ruboxistaurin hydrochloride (LY 333531 hydrochloride) is an Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src).
Targets&IC50	PKCη:0.052 μM, PKCβ2:5.9 nM, PKCδ:0.25 μM, PKCγ:0.3 μM, PKCβ1:4.7 nM
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	A significant up-regulation of TGF-b1, Smad2 and Smad3 mRNA expression was observed in diabetic rats, which was alleviated by administration of ruboxistaurin.
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)

Synonyms	Ruboxistaurin, LY333531 HCl, LY 333531 hydrochloride
Molecular Weight	505.01
Formula	C28H28N4O3·HCl
CAS No.	169939-93-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10.1 mg/mL (20 mM)

References and Literature

1. Jirousek MR, et al. J Med Chem. 1996, 39(14):2664-71. 2. Lei S, et al. Diabetes. 2013, 62(7):2318-28. 3. Wang SS, et al. Pharmazie. 2011, 66(11):881-7.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library TGF-beta/Smad Compound Library Bioactive Compound Library Kinase Inhibitor Library Bioactive Compounds Library Max Clinical Compound Library Human Metabolite Library

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Keywords

Ruboxistaurin hydrochloride 169939-93-9 Chromatin/Epigenetic Cytoskeletal Signaling PKC Ruboxistaurin Hydrochloride LY 333531 LY333531 Ruboxistaurin LY-333531 LY-333531 Hydrochloride LY 333531 Hydrochloride LY333531 HCl Inhibitor LY 333531 hydrochloride inhibit LY333531 Hydrochloride Protein kinase C inhibitor

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