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Highly potent JAK1 and JAK2 inhibitor (IC50 values are 5.9 and 5.7 nM, respectively). Also inhibits Tyk2 (IC50 = 53 nM). Displays >100-fold selectivity for JAK1/2 over JAK3 (IC50 = 53 nM for JAK3). Binds AAK1, BIKE, GAK and MPSK1 in vitro (Kd values are 17.2, 39.8, 134.4 and 68.5 nM, respectively). Inhibits IL-6-induced STAT phosphorylation and subsequent pro-inflammatory chemokine (MPC-1) and cytokine (IL-17 and IL-22) production in PBMCs and T-cells. Displays anti-inflammatory and disease modifying effects in the rat adjuvant arthritis model. In silico modelling predicts inhibition of SARS-CoV-2 cell entry.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 371.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.69 mL||13.46 mL||26.92 mL|
|5 mM||0.54 mL||2.69 mL||5.38 mL|
|10 mM||0.27 mL||1.35 mL||2.69 mL|
|50 mM||0.05 mL||0.27 mL||0.54 mL|
References are publications that support the biological activity of the product.
Fridman et al (2010) Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J.Immunol. 184 5298 PMID: 20363976
Sorrell et al (2016) Family-wide structural analysis of human numb-associated protein kinases. Structure. 24 401 PMID: 26853940
Richardson et al (2020) Baricitinib as potential treatment for 2019-nCoV acute respiratory disease. Lancet. 395 e30 PMID: 32032529
If you know of a relevant reference for Baricitinib, please let us know.
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