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-146072
    IRAK4-IN-11
    		Inhibitor
    IRAK4-IN-11 (compound 6) is a potent IRAK4 inhibitor with an IC50 of 0.008 µM. IRAK4-IN-11 shows cell pIRAK4 potencies with an IC50 of 0.19 µM.
    IRAK4-IN-11
  • HY-153673
    PROTAC IRAK4 degrader-8
    		Degrader
    PROTAC IRAK4 degrader-8 (Compound 2) is a PROTAC IRAK4 degrader (IC50: 15.5 nM). PROTAC IRAK4 degrader-8 degrades IRAK4 in THP-1 cells (DC50: 1.8 nM)。PROTAC IRAK4 degrader-8 also inhibits L-6 production in human whole blood and LPS-induced human PBMC cells, with IC50s of 246 nM and 2.2 nM respectively.
    PROTAC IRAK4 degrader-8
  • HY-153673
    PROTAC IRAK4 degrader-8
    		Inhibitor
    PROTAC IRAK4 degrader-8 (Compound 2) is a PROTAC IRAK4 degrader (IC50: 15.5 nM). PROTAC IRAK4 degrader-8 degrades IRAK4 in THP-1 cells (DC50: 1.8 nM)。PROTAC IRAK4 degrader-8 also inhibits L-6 production in human whole blood and LPS-induced human PBMC cells, with IC50s of 246 nM and 2.2 nM respectively.
    PROTAC IRAK4 degrader-8
  • HY-150733
    IRAK4-IN-19
    		Inhibitor
    IRAK4-IN-19 is a potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC50 value of 4.3 nM. IRAK4-IN-19 can inhibit LPS-induced IL23 production in THP and DC cells, and stop arthritis development in arthritis rats. IRAK4-IN-19 can be used for researching arthritis disease.
    IRAK4-IN-19
  • HY-123956
    HG-12-6
    		Inhibitor
    HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation.
    HG-12-6
  • HY-158760
    PROTAC IRAK4 degrader-11
    		Degrader
    PROTAC IRAK4 degrader-11 (compound 15) is PROTAC based on Cereblon ligand, and induces the degradation of IRAK4 with maximum degradation of 96.25% and the DC50 of 2.29 nM in HEK293 cells(Sturcture Note:(Blue: Cereblon ligand (HY-14658), Black: linker；Pink: IRAK4 inhibitor).
    PROTAC IRAK4 degrader-11
  • HY-162538
    LC-MI-3
    		Degrader
    LC-MI-3 is an orally active and potent interleukin-1 receptor-associated kinase 4 (IRAK4) PROTAC degrader, with a DC50 of 47.3 nM. LC-MI-3 effectively inhibits the activation of downstream NF-κB signaling. LC-MI-3 can be used for the research of acute and chronic inflammatory skin. (Blue: VHL ligand, Black: linker, Pink: CRBN ligand (HY-14658)).
    LC-MI-3
  • HY-155518
    IRAK4-IN-25
    		Inhibitor
    IRAK4-IN-25 (compound 38) is an orally acitve and potent IRAK4 inhibitor (IC50=7.3 nM), with low clearance (Cl=12 mL/min/kg). IRAK4-IN-25 inhibits production of pro-inflammatory cytokines, and shows in vitro safety and ADME profiles. IRAK4-IN-25 can be used for research in inflammatory and autoimmune disorders.
    IRAK4-IN-25
  • HY-148238
    GNE-2256
    		Inhibitor
    GNE-2256 (molecule 19) is an orally active IRAK4 (Interleukin 1 receptor associated kinase 4) inhibitor (IRAK4 Ki=1.4 nM; IL-6 IC50=190 nM).
    GNE-2256
  • HY-149345
    IRAK4-IN-24
    		Inhibitor
    IRAK4-IN-24 (compound 16) is a potent IRAK4 inhibitor, with high clearance (Cl) and poor oral bioavailability. IRAK4-IN-24 can be used for research in inflammatory and autoimmune disorders.
    IRAK4-IN-24
  • HY-155574
    IRAK4-IN-27
    		Inhibitor
    IRAK4-IN-27 (Compound 22) is a potent, selective inhibitor of IRAK4, with IC50 of 8.7 nM. IRAK4-IN-27 inhibits cell growth, and promotes apoptosis in MYD88 L265P diffuse large B-cell lymphoma (DLBCL) cell line. IRAK4-IN-27 can be used for DLBCL study.
    IRAK4-IN-27
  • HY-120561
    PC-046
    		Inhibitor
    PC-046 is a multi-target inhibitor for tyrosine receptor kinase B (TrkB), IRAK-4 and Pim-1, with IC50 of 13.4 μM, 15.4 μM and 19.1 μM, respectively. PC-046 exhibits cytotoxicity against pancreatic cancer cell BxPC3 with IC50 of 7.5-130 nM. PC-046 induces apoptosis and arrests cell cycle at G2/M phase in BxPC3. PC-046 exhibits antitumor efficacy and exhibits good pharmacokinetic characteristics in mice.
    PC-046
  • HY-155519
    IRAK4-IN-26
    		Inhibitor
    IRAK4-IN-26 (Compound 21) is a IRAK4 inhibitor (IC50: 6.2 nM). IRAK4-IN-26 displays an oral bioavailability of 21%. IRAK4-IN-26 can be used for research of inflammatory and autoimmune disorders.
    IRAK4-IN-26
  • HY-RS06900
    Irak4 Rat Pre-designed siRNA Set A
    		Inhibitor

    Irak4 Rat Pre-designed siRNA Set A contains three designed siRNAs for Irak4 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Irak4 Rat Pre-designed siRNA Set A
    Irak4 Rat Pre-designed siRNA Set A
  • HY-RS06898
    IRAK4 Human Pre-designed siRNA Set A
    		Inhibitor

    IRAK4 Human Pre-designed siRNA Set A contains three designed siRNAs for IRAK4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    IRAK4 Human Pre-designed siRNA Set A
    IRAK4 Human Pre-designed siRNA Set A
  • HY-W014223R
    2,4′-Dihydroxybenzophenone (Standard)
    		Inhibitor
    2,4′-Dihydroxybenzophenone (Standard) is the analytical standard of 2,4′-Dihydroxybenzophenone. This product is intended for research and analytical applications. 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 (Standard)
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
IRAK Isoform Comparison

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