Baricitinib [1187594-09-7]
Référence HY-15315-5mg
Conditionnement : 5mg
Marque : MedChemExpress
Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
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Baricitinib Chemical Structure
CAS No. : 1187594-09-7
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- M14 and A2058 cells are treated with IFN-γ (10 ng/mL) after Lac (100 μg/mL) or baricitinib (0.5 μM) for the indicated times. Whole cell lysates are subjected to western blotting.
- Western analysis of pJAK2, JAK2, pSTAT1, STAT1 and IRF1 protein in M14 and A2058 cells treated with IFN-g (10 ng/mL) after Lac (100 μg/mL) or baricitinib (0.5 μM) for the indicated times.
- An activator of Stat3, colivelin (0.1 or 1 µM), rescued Baricitinib-induced RANKL down-regulation in osteoblast cultures.
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Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively. | ||||
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In Vitro | In cell-based assays, Baricitinib (INCB028050) proves to be a potent inhibitor of JAK signaling and function. In PBMCs, Baricitinib inhibits IL-6-stimulated phosphorylation of the canonical substrate STAT3 (pSTAT3) and subsequent production of the chemokine MCP-1 with IC50 values of 44 nM and 40 nM, respectively. In isolated naive T-cells, INCB028050 also inhibits pSTAT3 stimulated by IL-23 (IC50=20 nM). Importantly, this inhibition prevented the production of two pathogenic cytokines (IL-17 and IL-22) produced by Th17 cells-a subtype of helper T cells with demonstrable inflammatory and pathogenic properties-with an IC50 value of 50 nM. In stark contrast, the structurally similar but ineffective JAK1/2 inhibitors INCB027753 and INCB029843 has no significant effect in any of these assays systems when tested at concentrations up to 10 μM. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. | |||
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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. MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement. |
Rats MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement. |
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[1]. Fridman JS, et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol. 2010 May 1;184(9):5298-307.
[2]. Jabbari A, et al. Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib. EBioMedicine. 2015 Feb 26;2(4):351-5.
[3]. Khan IM, et al. Intermuscular and perimuscular fat expansion in obesity correlates with skeletal muscle T cell and macrophage infiltration resistance. Int J Obes (Lond). 2015 Nov;39(11):1607-18.
* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.6924 mL | 13.4618 mL | 26.9237 mL | 67.3092 mL |
5 mM | 0.5385 mL | 2.6924 mL | 5.3847 mL | 13.4618 mL | |
10 mM | 0.2692 mL | 1.3462 mL | 2.6924 mL | 6.7309 mL | |
15 mM | 0.1795 mL | 0.8975 mL | 1.7949 mL | 4.4873 mL | |
20 mM | 0.1346 mL | 0.6731 mL | 1.3462 mL | 3.3655 mL | |
25 mM | 0.1077 mL | 0.5385 mL | 1.0769 mL | 2.6924 mL | |
30 mM | 0.0897 mL | 0.4487 mL | 0.8975 mL | 2.2436 mL | |
40 mM | 0.0673 mL | 0.3365 mL | 0.6731 mL | 1.6827 mL | |
50 mM | 0.0538 mL | 0.2692 mL | 0.5385 mL | 1.3462 mL | |
60 mM | 0.0449 mL | 0.2244 mL | 0.4487 mL | 1.1218 mL |
- Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
- JAK
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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
Baricitinib1187594-09-7LY3009104 INCB028050LY 3009104LY-3009104INCB028050INCB 028050INCB-028050JAKJanus kinaseInhibitorinhibitorinhibit
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- Nom du produit:
- Baricitinib
- Cat. No.:
- HY-15315
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