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Cat. No. Product Name CAS No. Information



FM-381 (FM381) is a potent, specific, reversible and covalent inhibitor of JAK3 with IC50 of 127 pM, 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and Tyk2, respectively; targets the unique Cys909 at the gatekeeper position +7 in JAK3; blocks IL2-stimulated (JAK3/JAK1 dependent) STAT5 phosphorylation at 100 nM, but not JAK3 independent IL6-stimulated (JAK1/2/TYK dependent) STAT3 signalling in Human CD4+ T cells.


AZD 4205


AZD 4205 (AZD4205) is a potent, selective JAK1 inhibitor IC50 of 73 nM and Ki of 2.8 nM, shows high selectivity against JAK2 and JAK3 with IC50 of 13,233 nM and >30,000 nM respectively; shows potent inhibition of p-STAT3 in a cell based assay of JAK1 activity with an IC50 of 128 nM and excellent selectivity across the kinome; reduces residual disease and prolongs the benefit of Osimertinib in lung cancer patients with EGFR activating mutations both in vitro and in vivo.

Lung Cancer

Phase 2 Clinical




PF-06700841 is a potent, selective TYK2/JAK1 kinase inhibitor that reduces IL-23 expression and directly attenuates IL-23 signaling via TYK2; is under investigation for the treatment of plaque psoriasis and lupus erythematosus.


Phase 2 Clinical


AS 2553627


AS 2553627 (AS2553627) is a novel potent, selective pan-JAK inhibitor with IC50 of 0.46, 0.30, 0.14 and 2.0 nM for JAK1, JAK2, JAK3 and TYK2, respectively; displays no inhibitory activity against a panel of protein kinases, including SYK and ZAP70 at 1 uM; inhibits proliferation of IL-2 stimulated human and rat T cells with IC50 of 2.4 and 4.3 nM, respectively, inhibits the proliferation of TF-1 cells stimulated with EPO with IC50 of 12 nM; effectively prevents chronic rejection in rat cardiac allografts in rat cardiac transplant model alone or co-administration with tacrolimus.




PF-04965842 (Abrocitinib, PF04965842) is a potent, selective, orally bioavailable JAK1 inhibitor with IC50 of 29 nM; exhibits good selective inhibition profile for JAK1 versus other JAK family enzymes (IC50=803/>10,000/1250 nM for JAK2/JAK3/TYK2, respectively); demonstrates efficacy in a rat adjuvant-induced arthritis (rAIA) model.


Phase 3 Clinical



Delgocitinib (JTE-052, LEO 124249) is a potent, selective, orally active, pan-JAK inhibitor with IC50 of 2.8, 2.6, 13 and 58 nM for JAK1,2,3 and Tyk2, respectively; does not inhibit a broad panel of kinases with exception of ROCK-II (IC50=140 nM); inhibits cytokine signaling evoked by IL-2, IL-6, IL-23, granulocyte/macrophage CSF, and IFN-α in vitro; potently suppresses the IL-2-induced IFN-γ production in mice (ED50=1.1 mg/kg), suppresses inflammatory responses in collagen-induced arthritis model.
Phase 2 Clinical



PF-06263276 (PF06263276, PF 6263276) is a potent, selective pan JAK inhibitor with IC50 of 2.2, 23.1, 59.9 and 29.7 nM for JAK1, JAK2, JAK3, and TYK2, respectively; demonstrates good JAK potency and kinase selectivity, exhibts inhibitory potency in human whole blood versus various stimulatory cytokines (IFNα, IL-23, IL-4, IL-6 and GM-CSF) with IC50 of 0.6-5.2 uM; suitable for inhaled and topical delivery in vivo.


Phase 1 Discontinued

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