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

BioE-1115, PASKi

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: PASK
532306
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1268863-35-9C₁₉H₁₈FN₃O₂

Products

Catalogue NumberPackaging Qty/Pack
5323060001 Glass bottle 10 mg
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®
SynonymsPASK Inhibitor, 2-(4-Fluorophenyl)-3-(isopropyl(methyl)amino)quinoxaline-6-carboxylic acid, BioE1115, Per-Arnt-Sim Domain Kinase Inhibitor, PAS Domain Kinase 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
Catalogue Number GTIN
5323060001 04055977287196

Documentation

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

Title

Safety Data Sheet (SDS) 

References

Reference overview
Wu, X., et al. 2014. Cell Rep. 8, 242.

Technical Info

Title
White Paper: Further considerations of antibody validation and usage.
Data Sheet

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