2. Signaling Pathways
  3. Immunology/Inflammation
  4. IRAK

IRAK

Interleukin-1 receptor associated kinase; IL-1R associated kinase

IRAK

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Interleukin-1 receptor-associated kinases (IRAKs), are serine/threonine kinases, play critical roles in initiating innate immune responses against foreign pathogens and other types of dangers through their role in Toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) mediated signaling pathways. The four different IRAK-like molecules have been identified: two active kinases, IRAK-1 and IRAK-4, and two inactive kinases, IRAK-2 and IRAK-M. All IRAKs mediate activation of nuclear factor-kappaB (NF-κB) and mitogen-activated protein kinase (MAPK) pathways.

Toll-like receptors transduce their signals through the adaptor molecule MyD88 and members of the IL-1R-associated kinase family (IRAK-1, 2, M and 4). IRAK-1 and IRAK-2, known to form Myddosomes with MyD88-IRAK-4, mediate TLR7-induced TAK1-dependent NF-κB activation. IRAK-M is known to function as a negative regulator that prevents the dissociation of IRAKs from MyD88, thereby inhibiting downstream signalling.

IRAK Isoform Specific Products:

IRAK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-160787
    NCGC1481
    		Inhibitor
    NCGC1481 is an inhibitor of FLT3, IRAK1, and IRAK4, with IC50 values of <0.5 nM, 22.6 nM, and 0.8 nM, respectively. NCGC1481 can effectively overcome the adaptive resistance of leukemia cells to FLT3 inhibitors and has antileukemic activity.
    NCGC1481
  • HY-135317F
    Emavusertib phosphate
    		Inhibitor
    Emavusertib phosphate (CA-4948 phosphate) is the phosphate salt form of Emavusertib (HY-135317). Emavusertib phosphate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib phosphate 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 phosphate exhibits antitumor activity in mouse model.
    Emavusertib phosphate
  • HY-101922R
    IRAK4-IN-1 (Standard)
    		Inhibitor
    IRAK4-IN-1 (Standard) is the analytical standard of IRAK4-IN-1 (HY-101922). This product is intended for research and analytical applications. IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.
    IRAK4-IN-1 (Standard)
  • HY-180908
    IRAK4-IN-34
    		Inhibitor
    IRAK4-IN-34 (compound 19) is a potent, selective, and orally active Interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC50 of 0.73 nM. IRAK4-IN-34 exhibits good selectivity vs both hERG and other kinases. IRAK4-IN-34 shows favorable in vivo PK properties. IRAK4-IN-34 can be used for inflammatory diseases research.
    IRAK4-IN-34
  • HY-135317E
    Emavusertib maleate
    		Inhibitor
    Emavusertib maleate (CA-4948 maleate) is the maleate salt form of Emavusertib (HY-135317). Emavusertib maleate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib maleate 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 maleate exhibits antitumor activity in mouse model.
    Emavusertib maleate
  • HY-117622
    ND-2110
    		Inhibitor
    ND-2110 is a selective IRAK4 inhibitor (Ki: 7.5 nM). ND-2110 binds to the ATP pocket of IRAK4. ND-2110 targets the subset of activated B cell-like (ABC) subtype of diffuse large B cell lymphoma (DLBCL) cell lines with MYD88 L265P mutations,. ND-2110 inhibits LPS-induced TNF production, alleviates collagen-induced arthritis, and blocks gout formation in mouse models.
    ND-2110
  • HY-135317C
    Emavusertib tosylate
    		Inhibitor
    Emavusertib tosylate (CA-4948 tosylate) is the tosylate salt form of Emavusertib (HY-135317). Emavusertib tosylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib tosylate 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 tosylate exhibits antitumor activity in mouse model.
    Emavusertib tosylate
  • HY-103017AR
    JH-X-119-01 (Standard)
    		Inhibitor
    JH-X-119-01 (Standard) is the analytical standard of JH-X-119-01 (HY-103017A). This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0380R
    Trimebutine (Standard)
    		Inhibitor
    Trimebutine (Standard) is the analytical standard of Trimebutine (HY-B0380). This product is intended for research and analytical applications. 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).
    Trimebutine (Standard)
  • HY-174843
    IRAK4-IN-32
    		Inhibitor
    IRAK4-IN-32 (Compound 10) is a potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an enzymatic IC50 value of 18.86 nM and a cellular IC50 value of 6.19 nM. IRAK4-IN-32 is promising for research of inflammatory and autoimmune diseases.
    IRAK4-IN-32
  • HY-135317D
    Emavusertib mesylate
    		Inhibitor
    Emavusertib mesylate (CA-4948 mesylate) is the mesylate salt form of Emavusertib (HY-135317). Emavusertib mesylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib mesylate 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 mesylate exhibits antitumor activity in mouse model.
    Emavusertib mesylate
Cat. No. Product Name / Synonyms Application Reactivity
IRAK Isoform Comparison

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