AG-490 (Tyrphostin B42) is an inhibitor of EGFR, ErbB2 and JAK2 with IC50 of 0.1 μM, 13.5 μM, and ~10 μM, respectively.

FM-479 is the negative control of FM-381 and has no activity on JAK3 or other kinases.

Peficitinib (ASP015K) hydrochloride is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.

SJ1008030 (compound 8) is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 inhibits MHH–CALL-4 cells with an EC50 of 5.4 nM and an IC50 of 32.09 nM. SJ1008030 can be used for the research of leukemia.

Peficitinib (ASP015K) hydrobromide is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.

SD-1008 is a potent JAK inhibitor. SD-1008 inhibits tyrosyl phosphorylation of STAT3, JAK2 and Src. SD-1008 also reduces STAT3-dependent luciferase activity. SD-1008 enhances apoptosis induced by Paclitaxel in ovarian cancer cells via directly blocking the JAK-STAT3 signaling pathway.

Humanin (human) (1-24-Protein humanin (human)), a small mitochondrial-derived cytoprotective polypeptide encoded by mtDNA, exhibits protective effects in several cell types against cellular stress conditions and apoptosis through regulating various signaling mechanisms, such as JAK/STAT pathway and interaction of BCL-2 family of protein.

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).

CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.

NDI-031407 (NDI 031407) is a novel potent, selective TYK2 inhibitor with IC50 of 0.21 nM in radiometric assays, 20 fold selectivity over JAK3 (4.2 nM), 147 fold for JAK2 (31 nM), and 220 fold for JAK1 (46 nM).NDI-031407 has high potency in cell line and primary cell assays for TYK2-dependent cytokines (IL-12, IC50=118 nM) over TYK2-independent cytokines (GM-CSF).NDI-031407 blocks IL-23–induced STAT3 phosphorylation and IL-17A production in human CD4+ T cells.NDI-031407 inhibits disease progression in the SKG model of Spondyloarthritis (SpA).NDI-031407 suppresses systemic IL-23–induced type 3 immunity in vivo.

LAS194046 (LAS-194046) is a potent, selective pan-JAK inhibitor with IC50 of 5.46/0.4/ 2.07 nM against JAK1/2/3, less potent in TYK2 activity (IC50=21.8 nM).LAS194046 is effective at blocking cytokine signaling depending on JAK1/JAK3, both in lymphocytes and monocytes, and JAK2/JAK2 in monocytes with IC50 of 16 nM, 26 nM and 37 nM, respectively.LAS194046 reduces allergen-induced airway inflammation, late asthmatic response, and phosphor-STAT activation in the rat OVA model.

Flonoltinib maleate is a potent, highly selective, dual JAK2/FLT3 inhibitor with IC50 of 0.8, 1.4, and 15 nM for JAK2, JAK2V617F, and FLT3, respectively.

Tofacitinib Prodrug-1 is an effective and oral active prodrug to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib Prodrug-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib Prodrug-1 is a potential drug candidate for the treatment of ulcerative colitis.

JAK-IN-19 is a potent JAK inhibitor (PBMC IFNγ pIC50=7.2 and HLF Eotaxin pIC50=7.7). JAK-IN-19 has good retentive properties in the lung via mitigating being metabolized by Aldehyde Oxidase (AO), with diminished VEGFR2 selectivity (VEGFR2 pIC50=7.0, Aurora B pIC50=5.8).

JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells.

JAK2/TYK2-IN-2 is a potent and selective TYK2 inhibitor with IC50 values of 9 and 157 nM for TYK2 and JAK2, respectively. JAK2/TYK2-IN-2 has anti-inflammatory activity.

Baricitinib phosphate(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2,showed potent activity against COVID-19(SARS-COV-2).

WHI-P97 is a rationally designed potent inhibitor of JAK-3.

LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.

Merck 5 is a potent and reversible ATP-competitive inhibitor of the JAK kinases (JAK1, JAK2, JAK3, and Tyk2). It also blocks IL2 and IL4 dependent proliferation of CTLL cells and inhibits the phosphorylation of STAT5.

GDC-4379 is a JAK1 inhibitor that can be used for the research of asthma.

A potent and highly selective JAK3 inhibitor with IC50 of 0.15 nM.

PF-06700841 is an inhibitor of JAK1 and TYK2 kinases. PF-06700841 has been investigated for the treatment of psoriasis and lupus.

Povorcitinib is a potent and selective inhibitor of JAK1. Povorcitinib has the potential for the research of disease selected from cutaneous lupus erythematosus (CLE) and Lichen planus (LP) (extracted from patent WO2021076124A1).

JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and JAK1 (IC50 = 29 and 41 nM respectively).

GLPG0634 (analog) is a pan JAK inhibitor with IC50s of 50-200 nM for JAK1/JAK2/JAK3; more information can be found in the reference patents.

BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.

Janex 1 selectively inhibits the tyrosine kinase activity of JAK3 with an IC50 value of 78 µM without affecting the enzymatic activity of JAK1, JAK2, or other protein tyrosine kinases (IC50 ≥350 µM).

Ten01 has 5.0 nM activity against JAK1 kinase.

Lorpucitinib is a Gut-Restricted JAK Inhibitor for the research of Inflammatory Bowel Disease.