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-19836
    Zimlovisertib
    		Inhibitor 99.94%
    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-N0039
    Ginsenoside Rb1
    		Inhibitor 98.75%
    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 .
    Ginsenoside Rb1
  • HY-135317
    Emavusertib
    		Inhibitor 99.94%
    Emavusertib (CA-4948) is a selective, potent and orally active IRAK4/FLT3 inhibitor. Emavusertib has an IC50 of 57 nM for IRAK4 in a FRET kinase assay. Emavusertib shows anti-tumor activity.
    Emavusertib
  • HY-145483
    KT-474
    		Inhibitor 99.27%
    KT-474 (KYM-001) is an orally active PROTAC IRAK4 degrader with antitumor activities. KT-474 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    KT-474
  • HY-13329
    IRAK-1-4 Inhibitor I
    		Inhibitor 99.88%
    IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor-associated kinase 1/4 (IRAK 1/4) with IC50s of 0.2 μM and 0.3 μM, respectively.
    IRAK-1-4 Inhibitor I
  • HY-W014223
    2,4′-Dihydroxybenzophenone
    		Inhibitor
    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-168586
    PROTAC IRAK4 degrader-12
    		Degrader
    PROTAC IRAK4 degrader-12 is a PROTAC based on Cereblon ligand, inducing a maximum degradation rate of IRAK4 of 108.46% in K562 cells with an IC50 value of 4.87 nM ( Structural Note: Pink, IRAK4 inhibitor (HY-168611); Blue, E3 (HY-W733885); Black, linker (HY-168613)).
    PROTAC IRAK4 degrader-12
  • 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-147141
    HS-276
    		Inhibitor 98.59%
    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 can be used for rheumatoid arthritis (RA) research.
    HS-276
  • HY-103017A
    JH-X-119-01
    		Inhibitor 99.03%
    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-139374
    Zabedosertib
    		Inhibitor 98.14%
    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-18992
    AS2444697
    		Inhibitor 99.12%
    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-103017
    JH-X-119-01 hydrochloride
    		Inhibitor 98.15%
    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.
    JH-X-119-01 hydrochloride
  • 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).
    AZ1495
  • HY-129966
    PROTAC IRAK4 degrader-1
    		Inhibitor 99.72%
    PROTAC IRAK4 degrader-1 is a Cereblon-based PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively.
    PROTAC IRAK4 degrader-1
  • HY-134911
    HS-243
    		Inhibitor 99.88%
    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-153188
    JNJ-1013
    		Degrader 99.80%
    JNJ-1013 is a potent and selective IRAK1 degrader with an IC50s of 72, 443, 1071 nM for IRAK1, IRAK4, VHL FP respectively. JNJ-1013 induces Apoptosis.html" class="link-product" target="_blank">Apoptosis and increases the expression of cleavaged PARP. JNJ-1013 decreases the expression IRAK1, p-IKBα, pSTAT3(Tyr705).
    JNJ-1013
  • HY-147264
    Edecesertib
    		Inhibitor 99.86%
    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-13276
    IRAK inhibitor 2
    		Inhibitor 98.29%
    IRAK inhibitor 2 is IRAK4 (interleukin-1 receptor associated kinase 4) inhibitor .
    IRAK inhibitor 2
  • HY-114181
    IRAK4-IN-4
    		Inhibitor 99.85%
    IRAK4-IN-4 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has 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
Cat. No. Product Name / Synonyms Application Reactivity
IRAK Isoform Comparison

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