Ruboxistaurin (LY333531) HCl

製品コードS7663 バッチS766303

印刷

化学情報

Chemical Structure Synonyms Ruboxistaurin hydrochloride, LY333531 hydrochloride Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C28H28N4O3.HCl
分子量 505.01 CAS No. 169939-93-9
Solubility (25°C)* 体外 DMSO 100 mg/mL (198.01 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 5.000mg/ml (9.90mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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 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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human umbilical vein endothelial cell (HUVEC)
濃度 200 nM
反応時間 48 h
実験の流れ 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.
動物実験 動物モデル Male Sprague-Dawley rats
投薬量 1 mg/kg/day
投与方法 by oral gavage

参考

  • https://pubmed.ncbi.nlm.nih.gov/8709095/
  • https://pubmed.ncbi.nlm.nih.gov/23474486/
  • https://pubmed.ncbi.nlm.nih.gov/22204135/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A genome-wide association study identified PRKCB as a causal gene and therapeutic target for Mycobacterium avium complex disease [ Cell Rep Med, 2025, S2666-3791(24)00694-3] PubMed: 39848245
Map2k6 is a potent genetic modifier of arterial rupture in vascular Ehlers-Danlos syndrome mice [ JCI Insight, 2025, 10(5)e187315] PubMed: 39836470
Spatial transcriptomics of a parasitic flatworm provides a molecular map of drug targets and drug resistance genes [ Nat Commun, 2024, 15(1):8918] PubMed: 39414795
Parkinson's disease gene, Synaptojanin1, dysregulates the surface maintenance of the dopamine transporter [ NPJ Parkinsons Dis, 2024, 10(1):148] PubMed: 39117637
Ginsenoside Rg1 attenuates diabetic vascular endothelial dysfunction by inhibiting the calpain-1/ROS/PKC-β axis [ Life Sci, 2023, 329:121972] PubMed: 37482213
Dynamic Plasticity Systems Direct Early Adaptation to Treatment in Neuroblastoma [ bioRxiv, 2023, 10.1101/2023.12.07.570359] PubMed: none
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization [ Cell Rep Methods, 2023, 3(10):100599] PubMed: 37797618
Enhanced neutrophil extracellular trap formation in COVID-19 is inhibited by the protein kinase C inhibitor ruboxistaurin [ ERJ Open Res, 2022, 8(2)00596-2021] PubMed: 35382002
Thioesterase superfamily member 1 undergoes stimulus-coupled conformational reorganization to regulate metabolism in mice [ Nat Commun, 2021, 12(1):3493] PubMed: 34108467
Mechanism by which Huoxue Tongluo Qiwei Decoction improves the erectile function of rats with diabetic erectile dysfunction [ J Ethnopharmacol, 2021, 283:114674] PubMed: 34560214

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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