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  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. Nombre del producto Efecto Pureza Chemical Structure
  • HY-146111
    IRAK4-IN-13
    		Inhibitor
    IRAK4-IN-13 (compound 21) is a potent and selective IRAK4 inhibitor with an IC50 of 0.6 nM. IRAK4-IN-13 shows high metabolic clearance with human liver microsomes (HLM) intrinsic clearance is 96 µL/min/mg.
    IRAK4-IN-13
  • HY-176197
    IRAK4-IN-31
    		Inhibitor
    IRAK4-IN-31 (Compound II) is a crystalline IRAK4 inhibitor. IRAK4-IN-31 can be used in myelodysplastic syndrome (MDS) research.
    IRAK4-IN-31
  • HY-180579
    IRAK4-IN-33
    		Inhibitor
    IRAK4-IN-33 (Compound 22) is a selective, potent and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC50 0.36 nM. IRAK4-IN-33 can block the pro-inflammatory signaling pathway mediated by IRAK4 and inhibit the release of TNFα and IFNα. IRAK4-IN-33 shows weak inhibition for hERG channel (IC50 > 30 μM). IRAK4-IN-33 can be used for the research of inflammation and immunology, such as rheumatoid arthritis.
    IRAK4-IN-33
  • HY-183800
    JH-l-25-NH2
    		Ligand
    JH-l-25-NH2 is an IRAK1/4 inhibitor analog derived from JH-I-25 and serves as the IRAK4-binding moiety for synthesizing VHL-recruiting and CRBN-recruiting IRAK4 PROTAC degraders.
    JH-l-25-NH2
  • HY-160654
    IRAK4 modulator-1
    		Modulator 99.11%
    IRAK4 modulator-1 (example 161) is a modulator of IRAK4 with IC50=4.647 μM. IRAK4 modulator-1 can be used to study IRAK-mediated disorders.
    IRAK4 modulator-1
  • HY-169057
    BI1543673
    		Inhibitor
    BI1543673 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor. BI1543673 can reduce the inflammatory response stimulated by TLR4 and TLR7/8 in human lung tissue. BI1543673 can decrease inflammatory signaling in a mouse model of lung inflammation induced by LPS.
    BI1543673
  • 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).
    AP-24567
  • HY-145484
    PROTAC IRAK4 ligand-3
    PROTAC IRAK4 ligand-3 is a ligand for target protein for PROTAC, targeting IRAK4, can be used for synthesis of PROTAC KT-474 (HY-145483). PROTAC IRAK4 ligand-3 can be used in cancer research.
    PROTAC IRAK4 ligand-3
  • HY-181898
    PROTAC IRAK3 degrader-2
    		Degrader
    PROTAC IRAK3 degrader-2 (Compound 17) is a IRAK3 PROTAC degrader with a DC50 ≤ 50 nM. It promotes ubiquitination and degradation of IRAK3, and is applicable to the research of immune diseases.
    PROTAC IRAK3 degrader-2
  • HY-161620
    DW18134
    		Inhibitor
    DW18134 is an inhibitor for interleukin receptor-associated kinase 4 (IRAK 4) with an IC50 of 11.2 nM. DW18134 inhibits phosphorylation of IRAK4 and IKK, downregulates the secretion of TNF-α and IL-6. DW18134 attenuates the Lipopolysaccharides (HY-D1056)-induced peritonitis and DSS-induced colitis in mouse models, and protects the intestinal barrier function .
    DW18134
  • HY-135382
    PROTAC IRAK4 degrader-2
    		Inhibitor
    PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC50 in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC50 of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs.
    PROTAC IRAK4 degrader-2
  • HY-148277
    KTX-612
    KTX-612 is an orally active IRAK4 PROTAC degrader with a DC50 value of 7 nM. KTX-612 can be used for the research of oncology.
    KTX-612
  • HY-162641
    AF-45
    		Inhibitor
    AF-45 inhibits IRAK4 and IRAK1, with IC50s of 128 nM and 1765 nM. AF-45 inhibits the release of IL-6 and TNF-α in macrophages, with IC50s of 0.53-1.54 μM and 0.6-2.75 μM. AF-45 is also an inhibitor for NF-κB/MAPK signaling pathway. AF-45 exhibits anti-inflammatory activities against DSS-induced ulcerative colitis and Lipopolysaccharide (HY-D1056)-induced acute lung injury in mouse model. AF-45 exhibits good pharmacokinetic characteristics in rat models.
    AF-45
  • HY-48932
    IRAK4 ligand-12
    		Ligand
    IRAK4 ligand-12 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). IRAK4 ligand-12 can be used for the synthesis of KTX-951 (HY-148290).
    IRAK4 ligand-12
  • HY-172591
    IRAK4 ligand-13
    		Ligand
    IRAK4 ligand-13 is a IRAK4 ligand. IRAK4 ligand-13 is a ligand for Target Protein for PROTAC. IRAK4 ligand-13 can be used for synthesis of PROTACs, such as LZ-07 (HY-172591).
    IRAK4 ligand-13
  • HY-158374
    BIO-8169
    		Inhibitor
    BIO-8169 is a selective inhibitor for interleukin receptor-associated kinase 4 (IRAK 4), with an IC50 of 0.23 nM. BIO-8169 exhibits good pharmacokinetic character, reduces the production of pro-inflammatory cytokines, and attenuates the autoimmune encephalomyelitis in EAE mice model. BIO-8169 exhibits good blood brain penetrant with a rat Kpu,u of 0.7.
    BIO-8169
  • HY-183799
    GSI526
    		Degrader
    GSI526 is a IRAK4 PROTAC degrader (DC50=40.17 nM, Dmax=97%; THP-1) based on the VHL ubiquitin-proteasome system. GSI526 inhibits IRAK4-mediated NF-κB and MAPK inflammatory signaling pathways, and induces IRAK4 degradation in myeloid cells. GSI526 is applicable to inflammation-related research.
    GSI526
  • HY-142662
    PROTAC IRAK3 degrader-1
    		Degrader
    PROTAC IRAK3 degrader-1 is a potent and selective IRAK3 degrader with a DC50 of 0.002 μM. PROTAC IRAK3 degrader-1 induces proteasome-dependent degradation of IRAK3 via ternary complex formation with IRAK3 and CRBN. PROTAC IRAK3 degrader-1 can be used for cancer research.
    PROTAC IRAK3 degrader-1
  • HY-139315
    PROTAC IRAK4 degrader-4
    		Degrader
    PROTAC IRAK4 degrader-4 is a Cereblon-based PROTAC as interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-127.
    PROTAC IRAK4 degrader-4
  • HY-158434
    IRAK1-IN-1
    		Inhibitor
    IRAK1-IN-1 (compound B8) is an orally active IRAK1 inhibitor. IRAK1-IN-1 inhibits the release of IL-6 with the IC50 values of 4.57 μM and 6.51 μM on mouse cells J774A. 1 and human cells THP-1, respectively. IRAK1-IN-1 alleviats LPS (HY-D1056)-induced acute lung injury (ALI) and DSS(HY-116282C)-induced colitis in mice.
    IRAK1-IN-1
Cat. No. Nombre del producto / Synonyms Application Reactivity
IRAK Isoform Comparison

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