69 products were found matching "K11218"!

PF-06651600 is a covalent inhibitor of JAK3 (IC50 = 33.1 nM). It is selective for JAK3 over JAK1, JAK2, and tyrosine kinase 2 (TYK2, IC50s = >10,000 for all) and a panel of 304 other kinases at 1 µM. PF-06651600 inhibits STAT5, STAT6, and STAT3 phosphorylation induced by IL-2, IL-4, or IL-21, respectively, in...

Soluble in DMSO at 100 mg/mL, soluble in ethanol at 100 mg/mL, very poorly soluble in water, maximum solubility in plain water is estimated to be about 10-20 µM, buffers, serum, or other additives may increase or decrease the aqueous solubility

The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Human JAK3. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Human JAK3. Next,...

The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Rat JAK3. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Rat JAK3. Next,...

JAK3-IN-2 is an inhibitor of JAK3 (Ki = 0.07 nM). It is selective for JAK3 over JAK1 and JAK2 (Kis = 320 and 740 nM, respectively). JAK3-IN-2 inhibits IL-2-induced STAT5 gene expression in a reporter assay (IC50 = 70 nM). In vivo, JAK3-IN-2 (100, 300, and 600 mg/kg) reduces paw swelling and ankle bone loss in a rat...

Off-white to pale yellow solid. Soluble in DMSO or ethanol. Potent cell permeable JAK3 inhibitor (IC50 = 1nM). Shows also JAK-1 inhibitory activity, Immunosuppressive and anti-inflammatory agent, Inhibits signaling through heterodimeric receptors associated with JAK3, JAK1, or both of them, with functional...

Tofacitinib is a potent, cell-permeable inhibitor of all JAK isoforms (IC50s = 6.1, 12, and 8 nM for JAK1, JAK2, and JAK3, respectively). It is selective for JAK1-3 over ROCK2 and Lck (IC50s = 3,400 and 3,870 nM, respectively) as well as 28 additional kinases in enzyme assays (IC50s = >10,000 nM). It inhibits...

Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. JAK1 mostly activates IL-6, whereas JAK1 and JAK3 trigger IL-2 and IL-4 and JAK1 and JAK2 stimulates IFN-gamma. JAK Inhibitor I is a pyridine-containing...

VX-509 is a selective inhibitor of Janus kinase 3 (JAK3) with a Ki value of 2.5 nM in enzyme assays and an IC50 value of 50-170 nM in cellular assays dependent on JAK3 activity with no measurable activity against other JAK isotypes. At 10-100 mg/kg, it has been shown to dose dependently reduce proinflammatory...

Janus kinase 3 (JAK3) is a cytoplasmic protein tyrosine kinase that functions in the initiation of cytokine-triggered signal transduction by catalyzing the phosphorylation of signal transduction and activators of transcription (STATs). JAK3 is abundantly expressed in normal lymphoid cells as well as human...

ZM 39923 is an inhibitor of JAK3 (IC50 = 79 nM) that less potently inhibits epidermal growth factor receptor, JAK1, and cyclin-dependent kinase 4 (IC50s = 2.4, 40, and 10 µM, respectively). In the absence of the reducing agent dithiothreitol, ZM 39923 also inhibits human tissue transglutaminase 2 (TGM2) and the...

FM-381 is a potent inhibitor of JAK3 (IC50 = 127 pM). It is 400-, 2,700-, and 3,600-fold selective for JAK3 over JAK1, JAK2, and TYK3 and only inhibits 11 kinases by less than 50 percent in a panel of 410 kinases when used at a concentration of 500 nM. FM-381 (1 µM) blocks JAK3-dependent STAT5 phosphorylation but...