janus kinase

Pyridone 6 (JAK Inhibitor)(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.

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

Deucravacitinib (BMS-986165) inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases. Which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain.

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.

Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.

Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.

Fosifidancitinib is a potent inhibitor of JAK 1 and JAK 3.

JAK-IN-5 is a JAK inhibitor.

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.

Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.

Solcitinib (GLPG-0778) (GSK2586184, GLPG0778) is a JAK1 inhibitor. Solcitinib may be potentially used for the treatment of psoriasis, ulcerative colitis, and systemic lupus erythematosus.

SB1317 (TG02) is a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3).

CEP-33779 is a novel and selective inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.

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

Peficitinib (ASP015K) (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.

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

1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide-I significantly sensitizes the res

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).

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

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

AG490 (Tyrphostin B42) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn, Lck, Syk, Btk, and Src.

RO8191 (CDM-3008) (CDM-3008) is an agonist of interferon (IFN) receptor.

LFM-A13（IC50=2.5 μM）, a specific Bruton's tyrosine kinase (BTK), is more than 100-fold specificity than other protein kinases, such as JAK1, JAK2, HCK, EGFR, and IRK.

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.

Itacitinib (INCB039110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity.

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

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

AZ960 is an effective ATP competitive JAK2 inhibitor (IC50/Ki: <3 nM and0.45 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.

WP1066 is a inhibitor of JAK2 (IC50: 2.30 μM) and STAT3 (IC50: 2.43 μM) in HEL cells; shows activity to JAK2, STAT3/5, and ERK1/2, not JAK1 and JAK3. WP1066 has been used in trials studying the treatment of Melanoma, Brain Cancer, Solid Tumors, and Central Nervous System Neoplasms.

Upadacitinib (ABT-494) (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 nM.

Tubulin/JAK2-IN-1 (compound 7g) serves as a potent dual inhibitor targeting both Janus kinase 2 (JAK2) and microtubules, demonstrating significant antiproliferative effects against cancer cells [1].

INCB032304 is an important pharmaceutical intermediate. It can be used in the preparation of Ruxolitinib phosphate (I008849), a janus kinase inhibitor, and in the preparation of Barretinib.

JAK-IN-33 (Compound 3 (R)) is a selective inhibitor of the Janus kinase (JAK) family [1].

Nimucitinib is a Janus kinase (JAK) inhibitor that can be used to treat dry eye and promote tear production.

Povorcitinib phosphate is a selective JAK1 inhibitor and can be used in studies about the treatment of cutaneous lupus erythematosus and Lichen planus.

JAK2 inhibitor G5-7 (JAK2 inhibitor G5-7) is an orally active JAK2 inhibitor, selectively inhibits JAK2–mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 has the potential for glioma study

Delgocitinib (JTE-052) is a specific JAK (Janus kinase) inhibitor with IC50 values of 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2 respectively. Delgocitinib is involved in various inflammatory and autoimmune diseases through JAK-dependent cytokines, and can effectively suppress multiple cytokine signaling while inhibiting itching caused by cytokines. It is widely used to treat various inflammatory diseases, including autoimmune diseases and hypersensitivity reactions.

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].

TK4g is a potent Janus kinase (JAK) inhibitor, demonstrating IC50 values of 12.61 nM and 15.80 nM against JAK2 and JAK3, respectively. It holds promise for research focused on lymphoid-derived diseases and leukemia cancer [1].

Pumecitinib is a Janus kinase (JAK) inhibitor. Pumecitinib exhibits anti-inflammatory activity.

DTP3 is a selective MKK7/GADD45β inhibitor, which inhibits cancer-selective NF-κB survival pathway.

Rovadicitinib is a Janus kinase inhibitor, also known as a JAK inhibitor. Rovadicitinib has potential for anti-inflammatory applications.

Tetramethylcurcumin is a novel curcumin analog, is an effective inhibitors of STAT3 phosphorylation, DNA binding activity, and transactivation in vitro.it also inhibits colony formation in soft agar, cell invasion, and exhibit synergy with the anti-cancer drug doxorubicin against breast cancer cells.

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

Nezulcitinib (TD-0903) is an inhaled, lung-selective inhibitor of pan-Janus kinase (JAK) that can be used to study COVID-19-associated acute lung injury and impaired oxygenation.

Brepocitinib (PF-06700841) is a potent dual JAK1/TYK2 inhibitor (IC50s: 17 nM/23 nM). Brepocitinib also inhibits JAK2/3 (IC50s: 77 nM/6.49 μM).

TK4b can be used in the research of leukemia cancer and lymphoid-derived diseases. TK4b is a Janus kinase (JAK) inhibitor with the IC50 values of 18.42 nM and 19.40 nM for JAK3 and JAK2, respectively [1].

Oclacitinib maleate (PF-03394197 maleate) is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, which did not inhibit a panel of 38 non-JAK kinases.

DTP3 TFA (1809784-29-9 free base) (DTP3 TFA) is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor.