JAK3-IN-1 |
| Catalog No.GC33046 |
JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1805787-93-2
Sample solution is provided at 25 µL, 10mM.
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JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, also inhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM).IC50 value: 4.8 nM [1]Target: JAK3in vitro: JAK3-IN-1 provides a set of useful tools to pharmacologically interrogate JAK3-dependent biology. JAK3-IN-1 completely inhibits IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibits IFNβ-induced p-STAT1 at a concentration of 5.0 μM. In a similar way, JAK3-IN-1 exhibits consistent potency and selectivity for JAK3 in leukemia cancer cell lines: TALL-1 and OCL-AML5. [1]in vivo: JAK3-IN-1 demonstrates reasonable pharmacokinetic properties, with moderate T1/2 of 1.4 h, area under the curve (AUC) value of 795 ng.h/mL following a 10 mg/kg oral dose and good oralbioavailability of 66%. [1]
[1]. Tan L, et al. Development of Selective Covalent Janus Kinase 3 Inhibitors. J Med Chem. 2015 Aug 27;58(16):6589-6606.
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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