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JAK

The JAK-STAT signalling pathway is a chain of interactions between proteins in a cell, and is involved in processes such as immunity, cell division, cell death and tumour formation. There are 4 JAK proteins: JAK1, JAK2, JAK3 and TYK2. JAKs contains a FERM domain (approximately 400 residues), an SH2-related domain (approximately 100 residues), a kinase domain (approximately 250 residues) and a pseudokinase domain (approximately 300 residues). The kinase domain is vital for JAK activity, since it allows JAKs to phosphorylate (add phosphate groups to) proteins.

  • Fedratinib
    T1995936091-26-8
    Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.
    • $45
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  • Ruxolitinib
    T1829941678-49-5
    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.
    • $53
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  • Kurarinone
    T5S099334981-26-5
    Kurarinone, a flavanoid derived from shrub Sophora flavescens,Kurarinone exhibits anti-tumor, estrogenic, and anti-inflammatory activities, it also shows strong inhibitory effect on immune responses. Kurarinone may ameliorate chronic inflammatory skin diseases through the suppression of pathogenic CD4(+) T-cell differentiation and the overall immune response.
    • $39
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  • Ritlecitinib
    T53821792180-81-4
    Ritlecitinib (PF-06651600) is a potent JAK3-selective inhibitor (IC50: 33.1 nM).
    • $39
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  • Ruxolitinib phosphate
    T30431092939-17-7
    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.
    • $44
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  • Cucurbitacin I
    TQ01962222-07-3
    Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.
    • $78
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  • TAK-901
    T2709934541-31-8
    TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.
    • $66
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  • Fosifidancitinib
    T386241237168-58-9
    Fosifidancitinib is a potent inhibitor of JAK 1 and JAK 3.
    • $148
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  • JI069
    T77672850019-35-1
    JI069 (WAY-354189) is a potent STAT3 inhibitor that inhibits gp130 signaling by inducing dissociation between gp130 and JAK1.
    • $195
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  • JAK3i
    T276501918238-72-8In house
    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.
    • $350
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  • NVP-BSK805 2HCl (1092499-93-8(free base))
    T6294 In house
    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.
    • $53
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  • WDR5-0103 hydrochloride[890190-22-4(free base)]
    T5140
    WDR5-0103 hydrochloride[890190-22-4(free base)] (WD-Repeat Protein 5-0103) is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
    • $37
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  • JAK-IN-5
    T117102096999-92-5In house
    JAK-IN-5 is a JAK inhibitor.
    • $197
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  • TG-46
    T20743936091-15-5In house
    TG-46 (TG46) inhibits JAK2, FLT3, RET, JAK3 and can be used to study glaucoma.
    • $195
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  • GDC-0214
    T98261831144-46-7
    GDC-0214 is an inhaled small-molecule JAK1 inhibitor and reduces fractional exhaled nitric oxide (Feno).
    • $148
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  • WHI-P97 HCl
    T4657L
    WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinase inhibition assays. WHI-P97 effectively inhibited the in vitro invasiveness of EGFR-positive human cancer cells in a concentration-dependent manner.
    • $58
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  • JAK-STAT-IN-1
    T786071236666-76-4In house
    JAK-STAT-IN-1 is a specific JAK-STAT inhibitor indicated for the study of autoimmune diseases.
    • $195 TargetMol
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  • SB1317 hydrochloride (1204918-72-8(free base))
    T4227
    SB1317 hydrochloride (1204918-72-8(free base)) (TG-02 hydrochloride) is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).
    • $45
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  • JAK-IN-10
    T13571916741-98-5In house
    JAK-IN-10 is a JAK inhibitor. JAK-IN-10 can be used for the research of dry eye disorders.
    • $79
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  • Butyzamide
    T678941110767-45-7In house
    Butyzamide is an effective and oral Mpl activator. It is a novel non-peptide-based molecule with antagonistic effects on thrombopoietin (TPO) receptors, which promotes proliferation of human Mpl (hMpl) expression and mouse pro B cell line Ba/F3. The phosphorylation of JAK2, STAT3, STAT5 and MAPK is induced. Butyzamide has been shown to help increase platelet levels in mouse xenotransplantation trials.
    • $285
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  • GS-829845
    T679051257705-09-1In house
    GS-829845 is a JAK1 inhibitor, the main component of the active metabolite of Filgotinib, which is approximately 10-fold less potent and has a longer half-life than the parent.
    • $39
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  • JAK3/BTK-IN-1
    T98142674036-91-8In house
    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.
    • $1,330
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  • TG-89
    T20742936091-56-4In house
    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.
    • $56
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  • JAK-IN-5 hydrochloride
    T11710L2751323-21-2In house
    JAK-IN-5 hydrochloride is a JAK inhibitor [1].
    • $1,620
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  • JAK3/BTK-IN-2
    T98132674036-93-0In house
    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.
    • $1,330
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  • Izencitinib
    T358982051918-33-1In house
    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.
    • $88 TargetMol
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  • JAK-IN-11
    T12549916742-11-5In house
    JAK-IN-11 (R-348) is a potent and selective inhibitor of JAK, has the potential for the skin disorders treatment.
    • $497
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  • Momelotinib
    T18491056634-68-4
    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.
    • $32
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  • Solcitinib
    T36201206163-45-2
    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.
    • $31
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  • Peficitinib
    T6933944118-01-8
    Peficitinib (ASP015K) (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.
    • $110
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  • SB1317
    T26531204918-72-8
    SB1317 (TG02) is a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3).
    • $64
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  • Degrasyn
    T6300856243-80-6
    Degrasyn (WP1130) (WP1130), a specific deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor, also inhibits Bcr/Abl, which is a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT).
    • $58
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  • Pacritinib
    T6020937272-79-2
    Pacritinib (SB1518) (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
    • $34
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  • CEP-33779
    T61221257704-57-6
    CEP-33779 is a novel and selective inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
    • $38
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  • AZD-1480
    T3069935666-88-9
    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
    • $52
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  • Pyridone 6
    T3080457081-03-7
    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.
    • $75
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  • Atractylenolide I
    T5S016773069-13-3
    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
    • $36
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  • AT9283
    T3068896466-04-9
    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).
    • $39
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  • Mubritinib
    T6124366017-09-6
    Mubritinib (TAK-165) (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
    • $32
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  • Baricitinib
    T24851187594-09-7
    Baricitinib (INCB028050) is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.
    • $43
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  • Tofacitinib
    T6321477600-75-2
    Tofacitinib (Tasocitinib) is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
    • $30
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  • AG490
    T2600133550-30-8
    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.
    • $43
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  • Filgotinib
    T19291206161-97-8
    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.
    • $50
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  • WP1066
    T2156857064-38-1
    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.
    • $44
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  • Upadacitinib
    T75031310726-60-3
    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.
    • $39
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  • RO8191
    T22142691868-88-9
    RO8191 (CDM-3008) (CDM-3008) is an agonist of interferon (IFN) receptor.
    • $38
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  • PP2
    T6266172889-27-9
    PP2 (AG 1879,AGL 1879) is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
    • $39
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  • LFM-A13
    T6217244240-24-2
    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.
    • $31
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  • WHI-P97
    T4657211555-05-4
    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.
    • $32
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  • OICR-9429
    T69161801787-56-3
    OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro.
    • $31
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