Baricitinib

SKU: orb1305415

Description

Baricitinib (INCB028050) is a JAK1 and JAK2 inhibitor (IC50=5.9/5.7 nM) with selective and oral activity. Baricitinib has potential anti-inflammatory, immunomodulatory and anti-tumor activity.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1187594-09-7
• MW: 371.42
• Purity: 99.97%
• Formula: C₁₆H₁₇N₇O₂S
• SMILES: CCS(=O)(=O)N1CC(CC#N)(C1)n1cc(cn1)-c1[nH]cnc2nccc12
• Target: Tyrosine Kinases,Chk,JAK
• Solubility: H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 250 mg/mL (673.09 mM), Sonication is recommended.

Bioactivity

• Target IC50:
  JAK3:> 400 nM|JAK2:5.7 nM|JAK1:5.9 nM|TYK2:53 nM
• In Vivo:
  METHODS: To investigat the potential therapeutic utility in autoimmune arthritis, Baricitinib (1-10 mg/kg) was administered orally to DBA/1j mice with collagen-induced arthritis (CIA) twice daily for 15 days. Results: Clinical signs of disease improved as early as 4 days after administration, and at study termination, clinical scores were reduced by 19%, 67%, and 61%, respectively in a dose-dependent manner compared to the vector control group.
• In Vitro:
  METHODS: PBMC cells were pre-incubated with Baricitinib (0-10,000 nM) for 10 min, an the cells were stimulated with IL-6 (10 ng/mL) for 48 h. Related factors were detected by ELISA assay. Results: In PBMC, Baricitinib inhibited IL-6-stimulated phosphorylation o the classical substratee STAT3 and subsequent production o the chemokine MCP-1 with IC50 Values of 44 nM and 40 nM, respectively METHODS: CD19+ B cells were treated with IgM antibody (1 µg/mL), sCD40L (250 ng/mL), IL-4 (100 ng/mL), and Baricitinib (0.05-5 µM) for 2-5 days, and gene expression levels were measured using real-time PCR. Results: After two days of stimulation, Baricitinib was found to significantly inhibi the expression level of Aicda in a dose-dependent manner, whil the expression level of Bcl6 was increased. After five days of stimulation the expression levels of Xbp1 and Irf4 were also significantly reduced. IgG production measured fro the supernatant unde the same conditions was significantly reduced depending o the increase in Baricitinib dose after two and five days of stimulation, respectively
• Cell Research:
  Baricitinib(INCB 028050) is dissolved in stock solutions, and then diluted with appropriate media before us. Human PBMCs are isolated by leukapheresis followed by Ficoll-Hypaque centrifugation. Fo the determination of IL-6-induced MCP-1 production, PBMCs are plated at 3. × 05 cells per well in RPMI 1640+10% FCS in the presence or absence of various concentration of INCB028050 (1 nM, 10 nM, 100 nM, 1 μM, and 10 μM). Following preincubation with compound for 10 min at room temperature, cells are stimulated by adding 10 ng mL human recombinant IL-6 to Each well. Cells are incubated for 48 h at 37℃, 5% CO2. Supernatants are Harvested and analyzed by ELISA for levels of human MCP-1 the ability of INCB028050 to inhibit IL-6-induced secretion of MCP-1 is reported a the concentration required for 50% Inhibition IC50 . Proliferation of Ba/F3-TEL-JAK3 cells is performed over 3 d using Cell-Titer Gl.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Chk2, Baricitinib, INCB028050, INCB-028050, INCB 028050, Janus kinase, JAK1, JAK2, JAK3, JAK, inhibit, Inhibitor, LY3009104, LY-3009104, LY 3009104, Tyk2, TyrosineKinases, Tyrosine Kinases

Compound Identifiers

PubChem CID

44205240