2. Signaling Pathways
  3. Epigenetics
    JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
    Stem Cell/Wnt
  4. JAK
  5. JAK1 Isoform
  6. JAK1 Inhibitor

JAK1 Inhibitor

JAK1 Inhibitors (99):

Cat. No. Product Name Effect Purity
  • HY-16755
    Solcitinib
    		Inhibitor 99.51%
    Solcitinib is an orally active, competitive, potent, selective JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of moderate-to-severe plaque-type psoriasis.
  • HY-151262
    JAK-IN-23
    		Inhibitor 98.90%
    JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD).
  • HY-19544
    JAK3-IN-1
    		Inhibitor 99.31%
    JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).
  • HY-101024
    PF-06263276
    		Inhibitor 99.38%
    PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively. PF-06263276 inhibits pSTAT3 and TYK2 pathway. PF-06263276 has a protective effect against ear skin inflammation.
  • HY-16997A
    Itacitinib adipate
    		Inhibitor 99.18%
    Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.
  • HY-50856S
    Deuruxolitinib
    		Inhibitor 99.18%
    Deuruxolitinib, a deuterated Ruxolitinib (HY-50856), is an orally active JAK1 and JAK2 inhibitor. Deuruxolitinib demonstrates significant hair regrowth effects. Deuruxolitinib can be used for the research of alopecia areata.
  • HY-19631B
    Ilginatinib hydrochloride
    		Inhibitor 98.92%
    Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
  • HY-111750
    JAK-IN-3
    		Inhibitor 98.92%
    JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively.
  • HY-18300A
    Filgotinib maleate
    		Inhibitor 99.88%
    Filgotinib maleate (GLPG0634 maleate) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib maleate can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values ​​of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib maleate also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib maleate can be used in the study of rheumatoid arthritis and inflammatory bowel disease.
  • HY-151385A
    (R,R)-VVD-118313
    		Inhibitor 99.54%
    (R,R)-VVD-118313 is the isomer of VVD-118313 (HY-151385). VVD-118313 is a selective JAK1 inhibitor and blocks JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer. (R,R)-VVD-118313 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-120469
    2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
    		Inhibitor 99.80%
    GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
  • HY-19631
    Ilginatinib maleate
    		Inhibitor 99.87%
    Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
  • HY-156961
    GLPG3667
    		Inhibitor 99.81%
    GLPG3667 is a reversible, ATP-competitive and orally active TYK2 inhibitor with an IC50 of 2.3 nM. GLPG3667 inhibits IFNα/pSTAT1, and the IC50 values ​​in human peripheral blood mononuclear cell (PBMC) and whole blood assays are 70 nM and 623 nM, respectively. GLPG3667 has the potential for the study of inflammatory and autoimmune diseases.
  • HY-131906
    JAK2-IN-7
    		Inhibitor 99.15%
    JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.
  • HY-139423
    JAK1-IN-8
    		Inhibitor
    JAK1-IN-8, a potent JAK1 inhibitor (IC50<500 nM), compound 28, extracted from patent WO2016119700A1.
  • HY-15814
    HG-7-85-01
    		Inhibitor 99.94%
    HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.
  • HY-143444
    JAK-IN-20
    		Inhibitor 99.63%
    JAK-IN-20 is a potent, pan and orally active JAK inhibitor with an IC50s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo.
  • HY-116505
    JAK1-IN-4
    		Inhibitor 99.26%
    JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM).
  • HY-13961
    GLPG0634 analog
    		Inhibitor 98.07%
    GLPG0634 analog (Compoun 176) is a broad spectrum JAK inhibitor with IC50 values of <100 nM against JAK1, JAK2 and JAK3.
  • HY-150720
    TYK2-IN-12
    		Inhibitor 98.81%
    TYK2-IN-12 (compound 30) is an orally active, potent and selective TYK2 (tyrosine kinase 2) inhibitor, with a Ki of 0.51 nM. TYK2-IN-12 inhibits IL-12 induced IFNγ, with IC50 values of 2.7 and 7.0 μM in human and mouse whole blood, respectively. TYK2-IN-12 can be used for psoriasis research.