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Biological Description

Description: Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.

Targets&IC50: JAK2:5.7 nM, JAK1:5.9 nM, Tyk2:53 nM, JAK3:>400 nM

Kinase Assay: Enzyme assays are performed using a homogeneous time-resolved fluorescence assay with recombinant epitope tagged kinase domains (JAK1, 837-1142; JAK2, 828-1132; JAK3, 718-1124; Tyk2, 873-1187) or full-length enzyme (cMET and Chk2) and peptide substrate. Each enzyme reaction is performed with or without test compound (11-point dilution), JAK, cMET, or Chk2 enzyme, 500 nM (100 nM for Chk2) peptide, ATP (at the Km specific for each kinase or 1 mM), and 2.0% DMSO in assay buffer. The calculated IC50 value is the compound concentration required for inhibition of 50% of the fluorescent signal. Additional kinase assays are performed at Cerep using standard conditions at 200 nM. Enzymes tested included: Abl, Akt1, AurA, AurB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKα, IKKβ, JNK1, Lck, MEK1, p38α, p70S6K, PKA, PKCα, Src, and ZAP70.

Cell Research: Baricitinib(INCB 028050) is dissolved in stock solutions, and then diluted with appropriate media before use. Human PBMCs are isolated by leukapheresis followed by Ficoll-Hypaque centrifugation. For the determination of IL-6-induced MCP-1 production, PBMCs are plated at 3.3×105 cells per well in RPMI 1640+10% FCS in the presence or absence of various concentrations 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°C, 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 as the concentration required for 50% inhibition (IC50). Proliferation of Ba/F3-TEL-JAK3 cells is performed over 3 d using Cell-Titer Glo.

Chemical Properties

Molecular Weight: 371.42

Formula: C16H17N7O2S

CAS No.: 1187594-09-7

Storage & Solubility Information

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

Ethanol: <1 mg/mL

DMSO: 69 mg/mL (185.8 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Catalog #: T2485

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References and Literature

1. Fridman JS, et al. J Immunol, 2010, 184(9), 5298-5307.

2. Kontzias A, et al. Curr Opin Pharmacol, 2012, 12(4), 464-470.

3. Norman P, et al. Expert Opin Ther Pat, 2012, 22(10), 1233-1249.

4. Norman P, et al. Expert Opin Ther Pat, 2012, 22(9), 1105-1109.

5. Kvacskay P, Yao N, Schnotz J H, et al. Increase of aerobic glycolysis mediated by activated T helper cells drives synovial fibroblasts towards an inflammatory phenotype: new targets for therapy?[J]. Arthritis Research & Therapy. 2021, 23(1): 1-15.