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Results for "

JAK1+inhibitor

" in MedChemExpress (MCE) Product Catalog:

40

Inhibitors & Agonists

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-19569
    Upadacitinib
    Maximum Cited Publications
    26 Publications Verification

    ABT-494

    JAK Inflammation/Immunology
    Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research [1] .
    Upadacitinib
  • HY-107429
    Abrocitinib
    10+ Cited Publications

    PF-04965842

    JAK Inflammation/Immunology
    Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease [1].
    Abrocitinib
  • HY-18300
    Filgotinib
    20+ Cited Publications

    GLPG0634

    JAK HIV Cancer
    Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib 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 also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease [1] .
    Filgotinib
  • HY-107361
    Golidocitinib
    2 Publications Verification

    AZD4205

    JAK Cancer
    Golidocitinib (AZD4205) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM) [1].
    Golidocitinib
  • HY-126294

    AZD4604; JAK1-IN-7

    JAK Inflammation/Immunology
    Londamocitinib (AZD4604) is a potent and selective JAK1 inhibitor with IC50 at 0.54 nM. Londamocitinib has anti-inflammatory activity [1] .
    Londamocitinib
  • HY-145588

    INCB54707

    JAK Inflammation/Immunology
    Povorcitinib (INCB54707) is a potent and selective JAK1 inhibitor that effectively reduces abscesses and inflammatory nodules. Povorcitinib is used to study cutaneous lupus erythematosus (CLE) and lichen planus (LP) [1] .
    Povorcitinib
  • HY-145551

    JAK Interleukin Related Inflammation/Immunology
    Atinvicitinib is an orally active and selective JAK1 inhibitor. Atinvicitinib blocks signaling of JAK1-dependent pruritogenic and pro-inflammatory cytokines, including those in the IL-31, IL-4, and IL-13 pathways. Atinvicitinib can be used for the researches of pruritus associated with allergic dermatitis and canine atopic dermatitis [1].
    Atinvicitinib
  • HY-16755
    Solcitinib
    3 Publications Verification

    GSK-2586184; GLPG-0778

    JAK Inflammation/Immunology
    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.
    Solcitinib
  • HY-19569R
    Upadacitinib (Standard)
    1 Publications Verification

    ABT-494 (Standard)

    Reference Standards JAK Inflammation/Immunology
    Upadacitinib (Standard) is the analytical standard of Upadacitinib. This product is intended for research and analytical applications. Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research [1] .
    Upadacitinib (Standard)
  • HY-18300A
    Filgotinib maleate
    20+ Cited Publications

    GLPG0634 maleate

    JAK HIV Inflammation/Immunology
    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 [1] .
    Filgotinib maleate
  • HY-151385

    JAK STAT IFNAR Interleukin Related Cancer
    VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer [1]. 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.
    VVD-118313
  • HY-151385A

    STAT Interleukin Related IFNAR JAK Cancer
    (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 [1]. (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.
    (R,R)-VVD-118313
  • HY-152080

    TUL01101

    JAK Inflammation/Immunology
    Blovacitinib (TUL01101) is a potent, selective and orally active JAK1 inhibitor, with an IC50s of 3, 37, 1517 and 36 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Blovacitinib can be used for the research of rheumatoid arthritis [1].
    Blovacitinib
  • HY-W727879
    Upadacitinib-15N,d2
    1 Publications Verification

    ABT-494-15N,d2

    Isotope-Labeled Compounds Others
    Upadacitinib- 15N,d2 (ABT-494- 15N,d2) is the deuterium-labeled Upadacitinib (HY-19569). Upadacitinib- 15N,d2 (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib- 15N,d2 (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib- 15N,d2 (ABT-494) can be used for several autoimmune disorders research [1] .
    Upadacitinib-15N,d2
  • HY-139837

    JAK Inflammation/Immunology
    GDC-4379 is a JAK1 inhibitor that can be used for the research of asthma [1].
    GDC-4379
  • HY-116505

    JAK Cancer
    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) [1].
    JAK1-IN-4
  • HY-16997A
    Itacitinib adipate
    20+ Cited Publications

    JAK Cancer
    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.
    Itacitinib adipate
  • HY-139423

    JAK Inflammation/Immunology Cancer
    JAK1-IN-8, a potent JAK1 inhibitor (IC50<500 nM), compound 28, extracted from patent WO2016119700A1 [1].
    JAK1-IN-8
  • HY-145588A

    INCB54707 phosphate

    JAK Inflammation/Immunology
    Povorcitinib (INCB54707) phosphate is a potent and selective JAK1 inhibitor that effectively reduces abscesses and inflammatory nodules. Povorcitinib phosphate can be used to study cutaneous lupus erythematosus (CLE) and lichen planus (LP) (information extracted from patent WO2021076124A1) [1].
    Povorcitinib phosphate
  • HY-18300R

    GLPG0634 (Standard)

    Reference Standards JAK Cancer
    Filgotinib (Standard) is the analytical standard of Filgotinib. This product is intended for research and analytical applications. Filgotinib (GLPG0634) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
    Filgotinib (Standard)
  • HY-19569A

    ABT-494 tartrate tetrahydrate

    JAK Inflammation/Immunology
    Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib tartrate tetrahydrate displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research [1] .
    Upadacitinib tartrate tetrahydrate
  • HY-107429R

    PF-04965842 (Standard)

    Reference Standards JAK Inflammation/Immunology
    Abrocitinib (Standard) is the analytical standard of Abrocitinib. This product is intended for research and analytical applications. Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease [1].
    Abrocitinib (Standard)
  • HY-19569S1

    ABT-494-d5

    Isotope-Labeled Compounds JAK Inflammation/Immunology
    Upadacitinib-d5 (ABT-494-d5) is the deuterium labeled Upadacitinib (HY-19569). Upadacitinib (ABT-494) is a potent, orally active and selective JAK1 inhibitor (IC50 = 43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research [1] .
    Upadacitinib-d5
  • HY-144440

    JAK Cancer
    JAK1-IN-9 (compound 23a) is a potent and selective JAK1 inhibitor with an IC50 of 72 nM. JAK1-IN-9 shows selective against other JAKs by 12 times or more [1].
    JAK1-IN-9
  • HY-18300S

    GLPG0634-d4

    JAK Cancer
    Filgotinib-d4 is the deuterium labeled Filgotinib. Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
    Filgotinib-d4
  • HY-112442

    JAK Cancer
    AZ-3 is a potent and selective JAK1 inhibitor with an IC50 of 34 nM.
    AZ-3
  • HY-162031

    JAK Metabolic Disease
    MMT3-72-M2 is an MMT3-72 metabolite. MMT3-72-M2 is a selective JAK1 inhibitor. MMT3-72-M2 inhibits JAK1, JAK2, TYK2, and JAK3 with IC50 values of 10.8 nM, 26.3 nM, 91.6 nM, 328.7 nM, respectlly [1].
    MMT3-72-M2
  • HY-178282

    JAK Inflammation/Immunology
    JAK1-IN-19 (Compound 18) is a potent JAK1 inhibitor with IC50s of 0.02, 0.5, 91 and 0.2 nM against JAK1, JAK2, JAK3 and TYK2. JAK1-IN-19 exhibits improved rat and human intrinsic clearance. JAK1-IN-19 can be used for the studies of atopic dermatitis and other autoimmune diseases [1].
    JAK1-IN-19
  • HY-18300AR

    GLPG0634 maleate (Standard)

    JAK HIV Reference Standards Inflammation/Immunology
    Filgotinib (maleate) (Standard) is the analytical standard of Filgotinib (maleate). This product is intended for research and analytical applications. 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 [1] .
    Filgotinib maleate (Standard)
  • HY-143885

    JAK Inflammation/Immunology
    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 [1].
    JAK1/TYK2-IN-3
  • HY-153566

    JAK Cancer
    JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, is a potent and selective JAK1 inhibitor [1].
    JAK1-IN-10
  • HY-139807

    JAK Inflammation/Immunology
    JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC50 of <5 μM. JAK-IN-14 is >8-fold more selective for JAK1 than JAK2 and JAK3 (Patent WO2016119700A1, compound 16) [1].
    JAK-IN-14
  • HY-145588S

    INCB54707-d6

    Isotope-Labeled Compounds JAK Inflammation/Immunology
    Povorcitinib-d6 (INCB54707-d6) is the deuterium labeled Povorcitinib (HY-145588). Povorcitinib (INCB54707) is a potent and selective JAK1 inhibitor that effectively reduces abscesses and inflammatory nodules. Povorcitinib is used to study cutaneous lupus erythematosus (CLE) and lichen planus (LP) [1] .
    Povorcitinib-d6
  • HY-161139

    JAK Inflammation/Immunology
    JAK1-IN-14 (Compound 12a) is a potent and selective JAK1 inhibitor. JAK1-IN-14 inhibits JAK1 and JAK2 with an IC50 value of 12.6 nM and 135 nM. JAK1-IN-14 suppresses hepatic fibrosis levels and can be used for the research of liver fibrosis and inflammatory diseases [1].
    JAK1-IN-14
  • HY-176793

    JAK Infection Inflammation/Immunology Cancer
    JAK1-IN-18 (Example 2) is a selective JAK1 inhibitor with an IC50 of 0.15  nM for JAK1 over JAK2 and JAK3. JAK1-IN-18 significantly reduces inflammation in DSS (HY-116282C)-induced ulcerative colitis (UC) mouse models and DNBS(HY-W324435)-induced Crohn's disease (CD) rat models. JAK1-IN-18 can be used for autoimmune diseases (such as inflammatory bowel disease), viral infections (such as HBV infection) and cancers (such as blood cancer) research [1].
    JAK1-IN-18
  • HY-W635076

    JAK Inflammation/Immunology
    oJak-989 is a selective JAK1 inhibitor with a Ki of 2.8 nM for JAK1, 110 nM for JAK3, and 31 nM for TYK2. oJak-989 is applicable to the research of inflammatory diseases [1].
    oJak-989
  • HY-107361R

    AZD4205 (Standard)

    Reference Standards JAK Cancer
    Golidocitinib (Standard) (AZD4205 (Standard)) is the analytical standard of Golidocitinib (HY-107361). This product is intended for research and analytical applications. Golidocitinib (AZD4205) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM) [1].
    Golidocitinib (Standard)
  • HY-181872

    JAK Interleukin Related STAT Inflammation/Immunology
    JAK1-IN-20 (Compound 38) is a gut-restricted, orally active, selective JAK1 inhibitor with an IC50 of <0.5 nM. JAK1-IN-20 inhibits the enzymatic activity of JAK1, reduces the production of proinflammatory cytokines (TNF-α, IL-6), and suppresses the phosphorylation of STAT3. JAK1-IN-20 ameliorates ulcerative colitis. JAK1-IN-20 can be used for the research of inflammatory bowel disease [1].
    JAK1-IN-20
  • HY-182359

    JAK STAT Inflammation/Immunology
    YYSW001 is a selective and orally acrive JAK1 inhibitor with an IC50 of 6 nM and a Kd of 32.32 μM. YYSW001 blocks JAK1-dependent phosphorylation of STAT6, as well as IL-6-induced phosphorylation of STAT3. YYSW001 suppresses pro-inflammatory cytokine levels, reduces paw swelling, lowers clinical arthritis scores, alleviates joint damage and decreases bone loss. YYSW001 is applicable for the research of rheumatoid arthritis [1].
    YYSW001
  • HY-181663

    PD-1/PD-L1 JAK Cancer
    PJ27 is a dual PD-1/PD-L1/JAK1 inhibitor, with an IC50 of 414 nM against PD-1/PD-L1, an IC50 of 786 nM against JAK1, a Ka of 294 nM for human PD-1/PD-L1, and a Ka of 473 nM for murine PD-1/PD-L1. PJ27 promotes the infiltration of CD3 +CD8 + and CD3 +CD4 + cells into the tumor microenvironment and exerts a significant immune activation effect. PJ27 inhibits tumor growth in a dose-dependent manner in the LLC lung cancer mouse model. PJ27 is applicable to relevant research on lung cancer [1].
    PJ27

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