2. Signaling Pathways
  3. Immunology/Inflammation
  4. IRAK
  5. IRAK1 Isoform

IRAK1

Interleukin-1 receptor-associated kinase 1 (IRAK1) is a serine-threonine kinase that mediates signaling downstream of Toll-like receptors (TLRs) and interleukin-1 receptor (IL-1R) complexes, promoting innate immune and inflammatory responses[1][2]. Mechanistically, IRAK1 interacts with the adaptor protein MyD88 and is recruited to the myddosome, where it undergoes phosphorylation and contributes to the activation of NF-κB and MAPK pathways[2][3]. Compared with its paralog IRAK4, IRAK1 exhibits distinct roles in hematologic malignancies, being preferentially expressed and required for maintaining viability and progenitor function in myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML)[4][5]. IRAK1 also regulates cancer stemness and chemoresistance in hepatocellular carcinoma through the IRAK1/IRAK4/AP-1/AKR1B10 signaling cascade, influencing self-renewal and tumorigenicity[6]. Alternative splicing generates the IRAK1b isoform, which is kinase-inactive but stable, adding regulatory complexity to IL-1 signaling[7]. Pharmacologically, selective IRAK1 inhibitors, including dual IRAK1/4 compounds and covalent degraders, effectively suppress inflammatory responses, enhance chemotherapy sensitivity, and reduce leukemic or tumor-initiating cell function in preclinical models[8][9][10][5][11][12]. These findings underscore the importance of IRAK1 in innate immunity, oncogenesis, and as a target for therapeutic intervention, while differentiating its function and regulation from other IRAK family members[13][4][5].

References:

IRAK1 Related Products (28):

Cat. No. Product Name Effect Purity
  • HY-N0039
    Ginsenoside Rb1
    		Inhibitor 99.75%
    Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .
  • HY-147141
    HS-276
    		Inhibitor 98.93%
    HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 reduces the expression of TNF, IL-6, and IL-1β. HS-276 can be used for rheumatoid arthritis (RA) research.
  • HY-103017A
    JH-X-119-01
    		Inhibitor 99.65%
    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.
  • HY-160487
    KME-2780
    		Inhibitor 98.94%
    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.
  • HY-153188
    JNJ-1013
    		Degrader 99.97%
    JNJ-1013 is a potent and selective IRAK1 PROTAC degrader with an IC50s of 72, 443, 1071 nM for IRAK1, IRAK4, VHL FP respectively. JNJ-1013 induces apoptosis and increases the expression of cleavaged PARP. JNJ-1013 decreases the expression IRAK1, p-IKBα, pSTAT3(Tyr705) (Pink: ligand for target protein (HY-138834); black: linker (HY-Y1760); Blue: E3 ligase ligand (HY-112078)).
  • HY-159953A
    IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride
    		Inhibitor 98.46%
    IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride 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 hydrochloride can be used for research on AML.
  • HY-147141A
    HS-276 hydrochloride
    		Inhibitor
    HS-276 hydrochloride is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 hydrochloride shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 hydrochloride reduces the expression of TNF, IL-6, and IL-1β. HS-276 hydrochloride can be used for rheumatoid arthritis (RA) research.
  • HY-125142
    AP-24567
    		Inhibitor
    AP-24567 is a Ligands for Target Protein for PROTAC, which can be used for the synthesis of SB1-G-187 (HY-137342).
  • HY-111101
    AZ1495
    		Inhibitor 98.07%
    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).
  • HY-103017
    JH-X-119-01 hydrochloride
    		Inhibitor 99.14%
    JH-X-119-01 hydrochloride is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 hydrochloride ameliorates LPS-induced sepsis in mice.
  • HY-B0380
    Trimebutine
    		Inhibitor 99.42%
    Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
  • HY-B0380A
    Trimebutine maleate
    		Inhibitor 99.66%
    Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
  • HY-137342
    SB1-G-187
    		Degrader 98.70%
    SB1-G-187 is a multi-target kinase PROTAC degrader with activity against various kinases including GCK, YES1, IRAK1 and LYN. SB1-G-187 induces degradation of target kinases via a p97-dependent pathway, and forms ternary complexes with CRBN and specific functional kinases. SB1-G-187 can be used in tumor-related research.
  • HY-159953
    IRAK1/4/pan-FLT3 Kinase-IN-1
    		Inhibitor 99.25%
    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.
  • HY-153110
    Larotinib
    		Inhibitor 99.50%
    Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM.
  • HY-134911
    HS-243
    		Inhibitor 99.95%
    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.
  • HY-153224
    GLPG2534
    		Inhibitor 98.73%
    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.
  • HY-153110A
    Larotinib mesylate hydrate
    		Inhibitor 98.66%
    Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM.
  • HY-179095
    UR241-2
    		Inhibitor 99.68%
    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.
  • HY-N0039R
    Ginsenoside Rb1 (Standard)
    		Inhibitor
    Ginsenoside Rb1 (Standard) is the analytical standard of Ginsenoside Rb1. This product is intended for research and analytical applications. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .
Cat. No. Product Name / Synonyms Application Reactivity