JAK3-IN-11 (Compound 12) exhibits potent, noncytotoxic, irreversible, orally active JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile (>588-fold compared to other JAK isoforms), covalently binds to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T-cell proliferation which is a promising tool for studying autoimmune diseases [1].

JAK3/ BTk-in-2 is a potent JAK3/BTK inhibitor. JAK3/ BTk-in-2 inhibits both BTK and JAK3, which are two important targets IN autoimmune diseases. JAK3/ BTk-in-2 simultaneously inhibits the BTK/JAK3 signaling pathway, showing a synergistic effect. JAK3/ BTk-in-2 has the potential to treat diseases associated with abnormal JAK3 and BTK activity.

JAK3-IN-14 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively.

JAK3/ BTk-in-1 is a dual JAK3/BTK inhibitor that specifically targets and inhibits Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK), two important targets in autoimmune diseases. JAK3/ BTk-in-1 simultaneously inhibited the BTK/JAK3 signaling pathway, showing a synergistic effect. JAK3/ BTK-in-1 is a potential compound for the treatment of immune-related diseases, such as autoimmune diseases, certain types of cancer (including lymphoma and leukemia), and other diseases that may be characterized by an unbalanced immune response.

JI6 (JAK3 Inhibitor VI) is a potent, selective and orally active FLT3 inhibitor. JI6 exhibits IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits c-Kit and JAK3, with IC50s of ∼500 and ∼250 nM, respectively. JI6 has research value in acute myeloid leukemia.

JAK3/BTK-IN-5 is a potent inhibitor of JAK3/BTK. where BTK and JAK3 are two key targets in autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway has a synergistic effect and JAK3/BTK-IN-5 has potential research value for JAK3 kinase and/or BTK-related diseases.

JAK3/BTK-IN-3 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets in autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway has a synergistic effect and JAK3/BTK-IN-3 has shown potential for the investigation of JAK3 kinases and/or BTK-related diseases.

JAK3-IN-9 is a potent and orally active inhibitor of the Janus kinase 3 (JAK3) enzyme, displaying an impressive IC50 value of 1.7 nM. It exhibits high selectivity towards the JAK3 signaling pathway, making it a valuable tool for studying autoimmune diseases. Additionally, JAK3-IN-9 possesses desirable characteristics such as low toxicity and excellent oral bioavailability. It also demonstrates promising anti-arthritis activity, thus enhancing its potential as a therapeutic agent [1].

JAK3/BTK-IN-4 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets in autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signaling pathway has a synergistic effect and JAK3/BTK-IN-4 has potential for JAK3 kinase and/or BTK-related diseases.

JAK3 Covalent Inhibitor-1 is a compound characterized by its potent and selective inhibition of Janus kinase 3 (JAK3), possessing an IC50 of 11 nM and demonstrating a 246-fold selectivity compared to other JAKs.

JAK3-IN-13 is a potent, selective, orally active JAK3 inhibitor that acts on NK1 (IC50: 4728 nM), JNK2 (IC50: 2039 nM), JNK3 (IC50: 8 nM), and Tyk2 (IC50: 365 nM). JAK3-IN-13 exhibits anti-tumor effects.

JAK3-IN-6 is irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM

JAK3-IN-1 is a selective and orally active JAK3 inhibitor (IC50: 4.8 nM). JAK3-IN-1 displays over 180-fold more selective for JAK3 than JAK1 (IC50: 896 nM) and JAK2 (IC50: 1050 nM).

JAK3-IN-12 (compound 15k) is a potent inhibitor of JAK3 (IC50: 9.5 nM) and can be used in the study of rheumatoid arthritis.

JAK3/BTK-IN-6 is a potent dual inhibitor of BTK (IC50: 0.6 nM) and JAK3 (IC50: 0.4 nM).JAK3/BTK-IN-6 exhibits good metabolic stability in human liver microsomes.JAK3/BTK-IN-6 can be used to study blood and immune diseases.

JAK3-IN-7 is a potent and selective JAK3 inhibitor (IC50<0.01 μM) for the treatment of rejection in organ transplantation, graft-versus-host reaction after organ transplantation, autoimmune disorders, allergic diseases, and chronic myeloproliferative disorders.

JANEX-1 (Jak3 inhibitor I) is a cell-permeable, reversible, effective, ATP-competitive, and selective inhibitor of JAK3 (IC50: 78 μM); little inhibitory against JAK1/2, or Zap/Syk or SRC tyrosine kinases.

WHI-P154 (Jak3 inhibitor ii) is a potent JAK3 inhibitor.

JAK3i is a selective covalent inhibitor of JAK3 kinase. JAK3i reveals two distinct temporal waves of STAT5 phosphorylation and more potently targets the second wave, which is required for cell cycle progression and T cell proliferation.

JAK 3 inhibitor IV (ZM 39923 hydrochloride) is a JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase.

ZM39923 hydrochloride (JAK3 Inhibitor IV) is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase.

Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

Ritlecitinib (PF-06651600) is a potent JAK3-selective inhibitor (IC50: 33.1 nM).

Ruxolitinib phosphate (INCB018424)(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.

TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.

NVP-BSK805 2HCl (1092499-93-8(free base)) (BSK 805)(IC50=0.5 nM), a specific and effective ATP-competitive JAK2 inhibitor, is more than 20-fold specificity over JAK1, JAK3 and TYK2.

TG-46 (TG46) inhibits JAK2, FLT3, RET, JAK3 and can be used to study glaucoma.

Izencitinib (JNJ-8398) is an orally active and gut-selective JAK inhibitor with potential anti-inflammatory activity for the study of ulcerative colitis and Crohn;s disease.

TG-89 is an inhibitor of JAK2, JAK3, RET and FLT3, and has an IC50 value of 11.2 μM against JAK2, showing anticancer activity in the treatment of ovarian and cervical cancer.

AZD1480 is a novel ATP-competitive JAK2 inhibitor (IC50: 0.26 nM), selectivity act against Tyk2 and JAK3, and to a smaller extent against JAK1. AZD1480 has been used in trials studying the treatment of Solid Malignancies, Post-Polycythaemia Vera, Primary

Pacritinib (SB1518) (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).

Baricitinib (INCB028050) is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.

AT9283 (J-504568) is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).

Tofacitinib (Tasocitinib) is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.

WHI-P97 is a rationally designed potent inhibitor of JAK-3. IC50 value: Target: JAK3 Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcepsilonRI crosslinking by >90% at low micromolar concentrations. WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal.

SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).

Filgotinib (GLPG0634) is a selective JAK1 inhibitor. The IC50 values against JAK1, JAK2, JAK3, and TYK2 are 10 nM, 28 nM, 810 nM, and 116 nM, respectively.

FM-479, an FM-381 structural analog, exhibits no inhibitory potency against JAK3 or other kinases when used at the FM-381 effective dosing range (100-300 nM). FM-479 is used as a negative control for FM-381.

JAK-2/3-IN-1 is a highly effective inhibitor targeting both JAK-2 and JAK-3 isoforms. It exhibits remarkable potency, with Ki values below 250 nM for both isoforms.

JAK2-IN-6, a polysubstituted aminothiazole derivative, is a potent and selective inhibitor of JAK2 (ic50 at 22.86 μg/mL). Jak2-in-6 inhibits the activity of JAK2 enzymes by interfering with Jak2-related signaling pathways, thereby producing therapeutic effects on the specific disease IN which JAK2 is dysregulated, and does not show activity on JAK1 and JAK3. JAK2 is a protein involved in signaling pathways that regulate cell growth and division. Abnormal activation of JAK2 has been linked to a variety of diseases, including some types of cancer and inflammatory diseases. JAK2-IN-6 has antiproliferative activity against cancer cells.

JAK-IN-34 (compound 11n) is a potent inhibitor of Janus kinases (JAKs), demonstrating IC50 values of 0.40 nM for JAK1, 0.83 nM for JAK2, 2.10 nM for JAK3, and 1.95 nM for TYK2. It effectively reduces joint swelling while maintaining a good safety profile [1].

Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, has an IC50 of 0.755-1.02 nM for BTK.

Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable inhibitor of JAK2.

JAK-IN-27, also known as compound 1, is an orally active, potent inhibitor of the JAKS family kinases, displaying inhibitory concentrations (IC50s) of 3.0 nM for TYK2, 7.7 nM for JAK1, and 629.6 nM for JAK3. Moreover, JAK-IN-27 impedes IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells with an IC50 of 23.7 nM [1].

JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC 50 of <5 μM. JAK-IN-14 is more than 8-fold selective for JAK1 than JAK2 and JAK3 [1].

PF-00956980 is a reversible pan-JAK inhibitor, exhibiting IC50 values of 2.2 μM for JAK1, 23.1 μM for JAK2, and 59.9 μM for JAK3. It is utilized in the study of lung and skin inflammatory diseases.

JAK2-IN-4 is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.

PF-06263276 is an effective and selective inhibitor of pan-JAK. It also has IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3, and TYK2, respectively.

AFN941 is a staurosporine analog, acting as a Jak3-specific inhibitor.

SJ10542, a phenyl glutarimide (PG)-PROTAC, demonstrates potent and selective activity against JAK2/3 by exhibiting DC50 values of 14, 11, and 24 nM for JAK2, JAK3, and JAK2-fusion ALL, respectively. It employs a PG ligand for cereblon (CRBN) recruitment [1].