BioE-1115

SKU: orb1309925

Description

BioE-1115 is a potent and selective inhibitor of PASK (serine-threonine protein kinase) with an IC50 of 4 nM, and it also inhibits CK2α at 10 μM. This small molecule is a valuable research tool for studying kinase signaling pathways in both cellular and biochemical assays.

Research Area

Cell Biology, Metabolism Research, Protein Biochemistry, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1268863-35-9
• MW: 339.36
• Purity: 97.54% (May vary between batches)
• Formula: C₁₉H₁₈FN₃O₂
• SMILES: CC(C)N(C)c1nc2cc(ccc2nc1-c1ccc(F)cc1)C(O)=O
• Target: Serine/threonin kinase,Casein Kinase,Serine Protease
• Solubility: 10% DMSO+90% Corn Oil:2.5 mg/mL (7.37 mM);DMSO:60 mg/mL (176.8 mM)

Bioactivity

• Target IC50:
  CK2α:10 μM
• In Vivo:
  In male Sprague-Dawley rats, BioE-1115 (10, 30 and 100 mg/kg) treatment shows a dose-dependent suppression of the expression of Gpat1, Fasn, and all other SREBP-1c target genes analyzed. SREBP-1 maturation in the liver is also suppressed in BioE-1115 treated rats. A calculated measure of insulin resistance, HOMA-IR, is decreased in a dose-dependent manner by BioE-1115 administration. Hepatic and serum TAG are decreased in a dose-dependent manner by BioE-1115 administration. BioE-1115 treatment causes a significant decrease in serum glucose. Both SREBP-1c and SREBP-1a mRNA are modestly decreased at the highest doses. Neither dose of BioE-1115 causes a significant change in either liver weight or body weight.
• In Vitro:
  In HepG2 cells, BioE-1115 (>10μM) treatment shows a significant reduction in SREBP activity, without any observable effects on cell morphology or growth rate. In HEK293 cells, BioE-1115 shows a dose-dependent loss of PASK phosphorylation (IC50 =1μM).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ser/Thr Protease, Serine endopeptidases, Serine kinase, serine threonine protein kinase, Serine proteases, threoninkinase, Serinekinase, threonin kinase, Threonine proteases, BioE 1115, BioE1115, BioE-1115, Casein Kinase, CaseinKinase, CK2α, inhibit, Inhibitor

Compound Identifiers

PubChem CID

50922674