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-142662A
    PROTAC IRAK3 degrade-1 formic
    		Degrader 99.26%
    PROTAC IRAK3 degrader-1 formic is a potent and selective IRAK3 degrader with a DC50 of 0.002 μM. PROTAC IRAK3 degrader-1 formic induces proteasome-dependent degradation of IRAK3 via ternary complex formation with IRAK3 and CRBN. PROTAC IRAK3 degrader-1 formic can be used for cancer research.
    PROTAC IRAK3 degrade-1 formic
  • 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).
    Trimebutine
  • 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).
    Trimebutine maleate
  • HY-P5432
    IRAK-4 Peptide substrate
    		99.87%
    IRAK-4 Peptide substrate (IRAK-1 (360-380)) is a biological active peptide. (This is a substrate peptide for Interleukin-1 Receptor-Associated Kinase (IRAK) 4)
    IRAK-4 Peptide substrate
  • HY-101922
    IRAK4-IN-1
    		Inhibitor 99.62%
    IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.
    IRAK4-IN-1
  • HY-W722277A
    LCC-12 formate
    		Inhibitor 99.90%
    LCC-12 (formate) is a copper (II) chelator and a derivative of the biguanide metformin (HY-B0627). LCC-12 (formate) reduces its hydrogen peroxide-dependent oxidation of NADH to NAD+. LCC-12 (formate) reduces IL-1β, IL-2, IL-6, IL-8, and TNF-α levels, as well as JAK2, STAT2, and IL-1 receptor-associated kinase 4 (IRAK4) levels in primary human cytokine-activated monocyte-derived macrophages (MDMs). LCC-12 (formate) reduces the number of CD80+ and CD86+ cytokine-activated MDMs. LCC-12 LCC-12 (formate) improves survival in a mouse model of sepsis induced by LPS or cecal ligation and puncture.
    LCC-12 formate
  • HY-151363
    IRAK4-IN-21
    		Inhibitor 99.94%
    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-W014223
    2,4′-Dihydroxybenzophenone
    		Inhibitor 98.00%
    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-129966
    PROTAC IRAK4 degrader-1
    		Degrader 99.77%
    PROTAC IRAK4 degrader-1 (compound I-210) is a Cereblon-based IRAK4 PROTAC degrader.
    PROTAC IRAK4 degrader-1
  • HY-130253
    IRAK4-IN-6
    		Inhibitor 99.30%
    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-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.
    SB1-G-187
  • HY-148290
    KTX-951
    		Degrader 99.60%
    KTX-951 is an orally active IRAK4 and IMiD (Ikaros/Aiolos) substrates PROTAC degrader (Kd = 3.5 nM). KTX-951 has DC50s of 13 nM, 14 nM and 13 nM for IRAK4, Ikaros and Aiolos, respectively. KTX-951 has IC50 of 35 nM for OCl-Ly10 CTG. KTX-951 has antitumor activity.
    KTX-951
  • 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.
    HS-243
  • 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.
    IRAK1/4/pan-FLT3 Kinase-IN-1
  • HY-13277
    IRAK inhibitor 3
    		Modulator 98.86%
    IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2.
    IRAK inhibitor 3
  • HY-109585
    IRAK4-IN-7
    		Inhibitor 99.36%
    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-162359
    BIO-7488
    		Inhibitor 99.44%
    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-135382A
    PROTAC IRAK4 degrader-3
    		Degrader 98.24%
    PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on von Hippel-Lindau.
    PROTAC IRAK4 degrader-3
  • 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.
    Larotinib
  • HY-175022
    PROTAC IRAK4 degrader-13
    		Degrader 99.47%
    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
Cat. No. Product Name / Synonyms Application Reactivity
IRAK Isoform Comparison

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