Millipore Sigma Vibrant Logo

532306 PAS Kinase Inhibitor, BioE-1115 - CAS 1268863-35-9 - Calbiochem

BioE-1115, PASKi

MSDS (material safety data sheet) o SDS, certificato d’analisi (CoA) e certificato di qualità (CoQ), dossier, brochure e altri documenti disponibili.

Sinonimi: 2-(4-Fluorophenyl)-3-(isopropyl(methyl)amino)quinoxaline-6-carboxylic acid, BioE1115, Per-Arnt-Sim Domain Kinase Inhibitor, PAS Domain Kinase Inhibitor, PASK Inhibitor

Primary Target: PASK
532306
Visualizza prezzi e disponibilità

Panoramica

Replacement Information

Tabella delle specifiche principali

CAS #Empirical Formula
1268863-35-9C₁₉H₁₈FN₃O₂

Prezzi e disponibilità

Numero di catalogo DisponibilitàConfezionamento Qtà/conf Prezzo Quantità
5323060001
Verifica della disponibilità in corso...
—
Disponibilità limitata Disponibilità limitata
A magazzino 
Fuori produzione
Disponibili quantità limitate
La disponibilità deve essere confermata
    Prodotti rimanenti: riceverà un nostro avviso
      Prodotti rimanenti: riceverà un nostro avviso
      Will advise
      Contatti il Servizio Clienti
      Contact Customer Service

      		 Bottiglia di vetro 10 mg
      Ricerca del prezzo in corso...
      Non è stato possibile trovare il prezzo
      La quantità minima deve essere un multiplo di
      Maximum Quantity is
      Al termine dell'ordine Maggiori informazioni
      Lei ha salvato ()
       
      —
      Richiedi il prezzo
      		 —
      Description
      OverviewA cell-permeable, orally available, non-toxic quinoxaline-carboxylic acid based compound that acts as a highly potent, selective, and reversible inhibitor of Per-Arnt-Sim Kinase (PASK; IC50 ~ 4 nM). Exhibits excellent selectivity over 49 other kinases (IC50 > 10 µM) and displays about 2,500-fold greater potency for PASK over casein kinase 2α. Blocks PASK autophosphorylation at Thr307 in a dose-dependent manner (IC50 ~ 1 µM) without affecting the insulin-induced phosphorylation of either Akt or S6K. Effectively blocks the maturation of SREBP-1 in hepatic tissue of high fructose fed wild-type Sprague-Dawley rats. Shown to normalize hepatic and serum triglyceride levels, reduce blood glucose levels, and partially reverse insulin resistance in animal models (30 mg/kg. p.o.).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number532306
      Brand Family Calbiochem®
      Synonyms2-(4-Fluorophenyl)-3-(isopropyl(methyl)amino)quinoxaline-6-carboxylic acid, BioE1115, Per-Arnt-Sim Domain Kinase Inhibitor, PAS Domain Kinase Inhibitor, PASK Inhibitor
      References
      ReferencesWu, X., et al. 2014. Cell Rep. 8, 242.
      Product Information
      CAS number1268863-35-9
      FormYellow powder
      Hill FormulaC₁₉H₁₈FN₃O₂
      Chemical formulaC₁₉H₁₈FN₃O₂
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPASK
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Numero di catalogo GTIN
      5323060001 04055977287196

      Documentation

      PAS Kinase Inhibitor, BioE-1115 - CAS 1268863-35-9 - Calbiochem MSDS

      Titolo

      Scheda di sicurezza (MSDS) 

      Riferimenti bibliografici

      Panoramica delle referenze
      Wu, X., et al. 2014. Cell Rep. 8, 242.

      Informazioni tecniche

      Titolo
      White Paper: Further considerations of antibody validation and usage.
      Scheda tecnica

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision28-January-2015 JSW
      Synonyms2-(4-Fluorophenyl)-3-(isopropyl(methyl)amino)quinoxaline-6-carboxylic acid, BioE1115, Per-Arnt-Sim Domain Kinase Inhibitor, PAS Domain Kinase Inhibitor, PASK Inhibitor
      DescriptionA cell-permeable quinoxaline-carboxylic acid compound that acts as a selective PAS kinase/PASK inhibitor (IC50 ~ 4 nM) with little or no potency against a panel of 49 other kinases (IC50 ≥ 10 µM) and effectively inhibits cellular PASK-T307 autophosphorylation (IC50 ~ 1 µM; 16 h drug treatment in PASK-transfected HEK293T cultures with 1% FBS). Similar to siRNA-mediated PASK knockdown, BioE-1115 treatment is shown to effectively prevent sterol regulatory element binding protein SREBP-1c maturation without affecting Akt/mTOR pathway signaling, resulting in impaired cellular SREBP transcription activity in HepG2 cultures (% inhibition/[drug] = 40%/30 µM & & 65%/50 µM by SRE-Luc reporter assay; overnight drug treatment prior to 100 nM insulin stimulation for 6 h). Oral administration is reported to effectively reduce high-frucose diet/HFrD-induced dyslipidemia (% reduction of liver triglyceride/serum triacylglyerol/dose = 48/26/30 mg kg-1 & 63/55/100 mg kg-1; Daily oral dosage administered in the last wk of a 3 wk HFrD period, followed by a 24 h fasting and a 12 refed period prior to tissue collection) and insulin resistance (% reduction of serum glucose/insulin/dose = 23/14/30 mg kg-1 & 28/31/100 mg kg-1) in rats by selectively suppressing SREBP-1 maturation and thereby inhibiting SREBP-1c, but not SRREBP-2, target genes transcription in liver, but not in abdominal fat or gastrocnemius muscle in vivo (% Gpat1/Fasn/Scd1/Acc1/Fae mRNA reduction/plasma [BioE-1115] in µg/mL/dose = 40/34/36/27/34/2.07/10 mg kg-1, 59/56/51/48/54/7.65/30 mg kg-1, 76/5967/62/74/42.2/100 mg kg-1) without affecting liver or body weight.
      FormYellow powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1268863-35-9
      Chemical formulaC₁₉H₁₈FN₃O₂
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesWu, X., et al. 2014. Cell Rep. 8, 242.