[CAS NO. 169939-93-9] Ruboxistaurin (LY333531) HCl
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PRODUCTS SPECIFICATIONS [169939-93-9]
Store
Catalog
SLK-S7663
Brand
Selleck
CAS
169939-93-9
DESCRIPTION [169939-93-9]
Overview
| MDL | MFCD00940226 |
|---|---|
| Molecular Weight | 505.01 |
| Molecular Formula | C28H28N4O3.HCl |
| SMILES | O=C1NC(C(C2=CN(C3=CC=CC=C32)CCO[C@H](CN(C)C)CC4)=C1C5=CN4C6=CC=CC=C56)=O.[H]Cl |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9802 mL | 9.9008 mL | 19.8016 mL |
| 5 mM | 0.3960 mL | 1.9802 mL | 3.9603 mL |
| 10 mM | 0.1980 mL | 0.9901 mL | 1.9802 mL |
| 50 mM | 0.0396 mL | 0.1980 mL | 0.3960 mL |
Description
Ruboxistaurin (LY333531) HCl is a inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively.
Targets
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.
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.
References
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