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IRAK4 inhibitor

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110

Inhibitors & Agonists

1

Click Chemistry

3

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-145483
    KT-474
    1 Publications Verification

    KYM-001; PROTAC IRAK4 degrader-7

    PROTACs IRAK Apoptosis Cancer
    KT-474 (KYM-001; PROTAC IRAK4 degrader-7) is an orally active PROTAC IRAK4 degrader with anti-tumor effects. KT-474 inhibits the cell cycle and induces apoptosis. KT-474 induces tumor regression in a xenograft model of MYD88-mutated ABC DLBCL. KT-474 is a click chemistry reagent, containing an alkyne group, which can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing azide groups .
    KT-474
  • HY-103490
    Takinib
    25+ Cited Publications

    EDHS-206

    MAP3K Apoptosis Infection Inflammation/Immunology Cancer
    Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
    Takinib
  • HY-19836
    Zimlovisertib
    5+ Cited Publications

    PF-06650833

    IRAK Inflammation/Immunology
    Zimlovisertib (PF-06650833) is a potent, selective and orally active inhibitor of interleukin-1 receptor associated kinase 4 (IRAK4) with IC50s of 0.2 and 2.4 nM in the cell and PBMC assay, respectively. Zimlovisertib is used to treat diseases such as rheumatoid arthritis, lupus, and lymphomas .
    Zimlovisertib
  • HY-14721
    Tepotinib
    5+ Cited Publications

    EMD-1214063

    c-Met/HGFR Autophagy Cancer
    Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation and induces autophagy. Tepotinib has antitumor effects .
    Tepotinib
  • HY-18992

    IRAK Inflammation/Immunology
    AS2444697 is an orally active IRAK-4 inhibitor with an IC50 of 21 nM . AS2444697 potently inhibits human and rat IRAK-4 activity. AS2444697 exhibits renoprotective effects through anti-inflammatory action .
    AS2444697
  • HY-50937
    ST 2825
    Maximum Cited Publications
    70 Publications Verification

    MyD88 Inflammation/Immunology
    ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity .
    ST 2825
  • HY-153368

    KT-413

    PROTACs IRAK NF-κB IFNAR Cancer
    Zomiradomide is an orally active PROTAC degrader for IRAK4 (DC50=6 nM), thereby inhibiting the NF-κB signaling pathway. Zomiradomide acts also as a molecular glue, recruiting Ikaros and Aiolos, and mediating their degradation (DC50 for Ikaros is 1 nM), thereby activating the type I IFN signaling pathway . (Pink: target protein ligand PROTAC IRAK4 ligand-5 (HY-168311), Blue: E3 ligase ligand Thalidomide-4-Br (HY-W039116), Black: linker (HY-168313))
    Zomiradomide
  • HY-139374
    Zabedosertib
    2 Publications Verification

    BAY 1834845

    IRAK Inflammation/Immunology
    Zabedosertib (BAY 1834845) is a selective, orally active IRAK4 inhibitor with immunomodulatory potential, IC50 is 3.55 nM. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors . Zabedosertib exhibits anti-inflammatory property against IL-β, LPS (HY-D1056) and Imiquimod (HY-B1080) induced inflammation .
    Zabedosertib
  • HY-103017A
    JH-X-119-01
    5+ Cited Publications

    IRAK Infection Inflammation/Immunology Cancer
    JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice . JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM .
    JH-X-119-01
  • HY-111101

    IRAK Cancer
    AZ1495, a weak base, is a potent orally active interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor. AZ1495 has a favorable physicochemical and kinase selectivity for IRAK4 and IRAK1 with IC50 values of 0.005 μM and 0.023 μM, respectively. AZ1495 has IRAK4 inhibition with a Kd value of 0.0007 μM. AZ1495 can be used for the research of diffuse large B-cell lymphoma (DLBCL) .
    AZ1495
  • HY-160487

    IRAK Apoptosis Cancer
    KME-2780 is the orally active inhibitor for IRAK1 and IRAK4 with IC50s of 19 nM and 0.5 nM. KME-2780 can be used for research of dysregulation of innate immune signaling and hematologic malignancies .
    KME-2780
  • HY-114181
    IRAK4-IN-4
    1 Publications Verification

    IRAK Cyclic GMP-AMP Synthase Inflammation/Immunology
    IRAK4-IN-4 (Compound 15) is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor, with an IC50 of 2.8 nM. IRAK4-IN-4 also inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM. IRAK4-IN-4 can be used for research of autoimmune diseases .
    IRAK4-IN-4
  • HY-101922

    IRAK Inflammation/Immunology
    IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.
    IRAK4-IN-1
  • HY-135317
    Emavusertib
    5+ Cited Publications

    CA-4948

    IRAK Apoptosis FLT3 NF-κB MyD88 Inflammation/Immunology Cancer
    Emavusertib is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib exhibits antitumor activity in mouse model
    Emavusertib
  • HY-138742

    MAP4K Cancer
    HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1 .
    HPK1-IN-7
  • HY-109585

    IRAK Inflammation/Immunology Cancer
    IRAK4-IN-7 is a selective, potent and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor, extracted from patent WO2015104688 (example 1). IRAK4-IN-7 has the potential for cancer and inflammatory diseases treatment .
    IRAK4-IN-7
  • HY-13275

    IRAK Inflammation/Immunology
    IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 3.801 μM, and >10 μM, respectively.
    IRAK inhibitor 1
  • HY-77048

    IRAK Inflammation/Immunology
    IRAK-4 protein kinase inhibitor 2 (compound 1) is a potent inhibitor of interleukin-1 (IL-1) receptor-associated kinase-4 (IRAK-4), with an IC50 of 4 μM. IRAK-4 protein kinase inhibitor 2 can be used for the research of inflammatory and immune-related conditions or disorders .
    IRAK-4 protein kinase inhibitor 2
  • HY-147264

    GS-5718

    IRAK Inflammation/Immunology
    Edecesertib (GS-5718) is a selective, potent, orally active IRAK-4 inhibitor. Edecesertib has anti-inflammatory activity. Edecesertib can be used for rheumatoid arthritis (RA) and lupus erythematosus (LE) research .
    Edecesertib
  • HY-153224

    IRAK Inflammation/Immunology
    GLPG2534 is an orally active and selective IRAK4 inhibitor, with IC50 values of 6.4 nM and 3.5 nM for human and mouse IRAK4. GLPG2534 can be used for the research of inflammatory skin diseases .
    GLPG2534
  • HY-148238

    IRAK Inflammation/Immunology
    GNE-2256 (molecule 19), a chemical probe, is an orally active IRAK4 (Interleukin 1 receptor associated kinase 4) inhibitor (IRAK4 Ki=1.4 nM; IL-6 IC50=190 nM) .
    GNE-2256
  • HY-123854

    IRAK Inflammation/Immunology
    PF-06426779 is a potent and selective inhibitor of interleukin 1 receptor associated kinase 4 (IRAK4), with an IC50 of 0.3 nM .
    PF-06426779
  • HY-174455

    PROTACs IRAK Interleukin Related Inflammation/Immunology
    APH02174 is a highly selective and orally active IRAK4 PROTAC degrader with the DC50 of 4.01 nM in THP-1 cells. APH02174 blocks inflammatory signals by inhibiting IL-6 release. APH02174 can be used for research on inflammatory conditions such as psoriasis vulgaris and rheumatoid arthritis .
    APH02174
  • HY-14721R

    EMD-1214063 (Standard)

    Reference Standards c-Met/HGFR Autophagy Cancer
    Tepotinib (Standard) is the analytical standard of Tepotinib. This product is intended for research and analytical applications. Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation. Tepotinib has antitumor effects .
    Tepotinib (Standard)
  • HY-W014223

    Ultraviolet absorber UV-0

    Environmental Pollutants Toll-like Receptor (TLR) NF-κB Reactive Oxygen Species (ROS) MyD88 IRAK Inflammation/Immunology
    2,4′-Dihydroxybenzophenone (Ultraviolet absorber UV-0) occupies the hydrophobic pocket of MD2 and blocks the dimerization of TLR4. 2,4′-Dihydroxybenzophenone inhibits the LPS induced mtROS production, and LPS induced inflammatory response by downregulating pro-inflammatory mediators and decreasing the expression of MyD88, p-IRAK4, and NF-κB. 2,4′-Dihydroxybenzophenone is also a UV absorber .
    2,4′-Dihydroxybenzophenone
  • HY-150735

    IRAK Inflammation/Immunology
    IRAK4-IN-20 (Compound BAY-1834845) is an orally active IRAK4 inhibitor with an IC50 of 3.55 nM. IRAK4-IN-20 can be used for acute respiratory distress syndrome (ARDS) research .
    IRAK4-IN-20
  • HY-151363

    IRAK Inflammation/Immunology
    IRAK4-IN-21 (compound 17) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 5 and 56 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.17 μM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis .
    IRAK4-IN-21
  • HY-151365

    IRAK Inflammation/Immunology
    IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis .
    IRAK4-IN-22
  • HY-146112

    IRAK Cancer
    IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC50 of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib .
    IRAK4-IN-14
  • HY-179094

    PROTACs IRAK NF-κB Enolase Inflammation/Immunology Cancer
    PSP-0119 is a highly efficient and effective PROTAC degrader targeting IRAK4 (IC50 = 2.83 nM). PSP-0119 can inhibit IRAK4 kinase activity, NF-κβ activity, and IL-1β-induced IRAK4 phosphorylation. PSP-0119 degrades IRAK4 in FLT3-mutant AML cell lines, sparing FLT3-wild-type AML cells, FLT3-wild-type samples, and normal bone marrow. PSP-0119 downregulates alpha-enolase (eNOS) of MOLM-13 cells. PSP-0119 can be used for the study of Acute Myeloid Leukemia (AML) .
    PSP-0119
  • HY-159953

    IRAK FLT3 Inflammation/Immunology Cancer
    IRAK1/4/pan-FLT3 Kinase-IN-1 is an orally active, potent and selective IRAK/pan-FLT3 kinase inhibitor with IC50s of 5 nM, 0.6 nM and <0.5 nM against IRAK1, IRAK4 and FLT3, respectively. IRAK1/4/pan-FLT3 Kinase-IN-1 can be used for research on AML .
    IRAK1/4/pan-FLT3 Kinase-IN-1
  • HY-134911

    IRAK CDK Inflammation/Immunology Cancer
    HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC50 values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity .
    HS-243
  • HY-162359

    IRAK Neurological Disease Inflammation/Immunology
    BIO-7488 is an orally active, selective and blood-brain barrier permeable IRAK4 inhibitor, with an IC50 value of 0.5 nM. BIO-7488 inhibits the production of pro-inflammatory cytokines (IL-1β, TNFα, IL-6) and demonstrates anti-inflammatory effects in both LPS (HY-D1056) and distal hypoxic-middle cerebral artery occlusion (DH-MCAO) ischemic stroke model. BIO-7488 can be used for the study of neuroinflammatory-related diseases, particularly ischemic stroke .
    BIO-7488
  • HY-153673

    IRAK PROTACs Cancer
    PROTAC IRAK4 degrader-8 (Compound 2) is a PROTAC IRAK4 degrader (IC50: 15.5 nM). PROTAC IRAK4 degrader-8 degrades IRAK4 in THP-1 cells (DC50: 1.8 nM)。PROTAC IRAK4 degrader-8 also inhibits L-6 production in human whole blood and LPS-induced human PBMC cells, with IC50s of 246 nM and 2.2 nM respectively .
    PROTAC IRAK4 degrader-8
  • HY-130253

    IRAK Cancer
    IRAK4-IN-6 is an orally efficacious and selective IRAK4 inhibitor with an IC50 of 4 nM, and targetes MyD88 L265P mutant diffuse large B cell lymphoma .
    IRAK4-IN-6
  • HY-175022

    PROTACs IRAK Toll-like Receptor (TLR) Interleukin Related Inflammation/Immunology
    PROTAC IRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader with DC50s of 0.86 and 1.1 nM for monocytes and lymphocytes in PBMCs, respectively. PROTAC IRAK4 degrader-13 significantly induces TIR signal activation, and inhibits the expression of circulating proinflammatory cytokines in Imiquimod (HY-B0180) induced psoriasis mice model. PROTAC IRAK4 degrader-13 can be used for TLR- and IL-1R-driven driven neutrophilic inflammation diseases like hidradenitis suppurativa (HS) and atopic dermatitis (AD) research . Pink: IRAK4 ligand; Blue: E3 ligase ligand; Black: linker
    PROTAC IRAK4 degrader-13
  • HY-148276

    PROTACs IRAK Cancer
    KTX-497 is an IRAK4 PROTAC degrader with a DC50 value of 3 nM. KTX-497 can be used for the research of oncology [1].(Pink:IRAK4 inhibitor (HY-150735); Black: linker; Blue: CRBN Ligand (HY-10984))
    KTX-497
  • HY-131903

    IRAK Inflammation/Immunology
    HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties .
    HS271
  • HY-14721A

    EMD-1214063 hydrochloride

    c-Met/HGFR Autophagy Cancer
    Tepotinib (EMD-1214063) hydrochloride is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib hydrochloride inhibits c-Met phosphorylation and induces autophagy. Tepotinib hydrochloride has antitumor effects .
    Tepotinib hydrochloride
  • HY-178012

    IRAK TNF Receptor Inflammation/Immunology
    GLPG4471 is a selective and orally active IRAK4 inhibitor with an IC50 of 1.7 nM. GLPG4471 exhibits potent inhibition of cytokine (TNFα and IFNα) secretion in cellular and whole blood phenotypic assays. GLPG4471 displays significant activity in a mouse model of collagen-induced arthritis. GLPG4471 can be used for the study of arthritis .
    GLPG4471
  • HY-13278
    IRAK inhibitor 4
    1 Publications Verification

    IRAK Inflammation/Immunology
    IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor.
    IRAK inhibitor 4
  • HY-13280

    IRAK Inflammation/Immunology
    IRAK inhibitor 6 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK-4) with IC50 of 160 nM.
    IRAK inhibitor 6
  • HY-177515

    IRAK STAT JAK NF-κB Inflammation/Immunology
    IRAK4 modulator-2 (Compound 5) is a selective dual Interleukin-1 Receptor Associated Kinase 4 (IRAK4) and IRAK1 inhibitor with IC50 values of 0.005 μM and 0.97 μM, erespectively. IRAK4 modulator-2 blocks IRAK-mediated signaling pathways (e.g., JAK-STAT, NF-κB pathways), reduces the production of pro-inflammatory cytokines (e.g., IL-1, TNF), and exerts anti-inflammatory activity. IRAK4 modulator-2 is promising for research of autoimmune diseases and inflammatory diseases, such as rheumatoid arthritis, psoriasis, inflammatory bowel disease .
    IRAK4 modulator-2
  • HY-179095

    Ligands for Target Protein for PROTAC IRAK NF-κB p38 MAPK Cancer
    UR241-2 is an IRAK4 inhibitor. UR241-2 suppresses IL-1–induced IRAK1/4 signaling, NF-κβ activation, and phosphorylation of p65 and p38. UR241-2 selectively inhibits leukemia stem cell clonogenicity. UR241-2 can serve as a ligand for target proteins for PROTAC, facilitating the development and design of PROTAC degraders for IRAK4. UR241-2 can be used in the research of acute myeloid leukemia .
    UR241-2
  • HY-W900240

    IRAK Inflammation/Immunology
    BMS-978299 is an IRAK4 inhibitor that can be used for the study of immune disorders .
    BMS-978299
  • HY-124995

    IRAK Toll-like Receptor (TLR) ERK NF-κB Interleukin Related Inflammation/Immunology
    BMS-986126 is a potent, selective, and orally active IRAK4 inhibitor (IC50 = 5.3 nM). BMS-986126 broadly inhibits MyD88-dependent signaling pathways. BMS-986126 demonstrates robust activity in the MRL/lpr and NZB/NZW murine models of lupus, inhibiting multiple pathogenic responses. BMS-986126 can be used for autoimmune diseases research, such as lupus erythematosus (SLE) .
    BMS-986126
  • HY-155132

    IRAK Inflammation/Immunology
    IRAK4-IN-28 (compound 42) is an orally active IRAK4 inhibitor (IC50=8.9 nM). IRAK4-IN-28 has binding affinity for IRAK4 with a Kd of 0.58 nM. IRAK4-IN-28 can be used in the research of inflammation and autoimmune diseases .
    IRAK4-IN-28
  • HY-155519

    IRAK Inflammation/Immunology
    IRAK4-IN-26 (Compound 21) is a IRAK4 inhibitor (IC50: 6.2 nM). IRAK4-IN-26 displays an oral bioavailability of 21%. IRAK4-IN-26 can be used for research of inflammatory and autoimmune disorders .
    IRAK4-IN-26
  • HY-143485

    IRAK Inflammation/Immunology Cancer
    IRAK4-IN-9 (compound 73) is a potent IRAK4 inhibitor with an IC50 of 1.5 nM. IRAK4-IN-9 blocks MyD88 dependent signaling. IRAK4-IN-9 has the potential for the research of inflammatory diseases, autoimmune diseases, and cancer .
    IRAK4-IN-9
  • HY-143231

    IRAK Infection
    IRAK4-IN-8 (VI-177) is a potent IRAK4 inhibitor .
    IRAK4-IN-8

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