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-150594
    IRAK4-IN-17
    		Inhibitor
    IRAK4-IN-17 (Compound 5) is a potent IRAK4 inhibitor with the IC50 of 1.3 nM. IRAK4-IN-17 can be used in large B-cell lymphoma (DLBCL) research.
    IRAK4-IN-17
  • HY-RS06893
    IRAK1 Human Pre-designed siRNA Set A
    		Inhibitor

    IRAK1 Human Pre-designed siRNA Set A contains three designed siRNAs for IRAK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    IRAK1 Human Pre-designed siRNA Set A
    IRAK1 Human Pre-designed siRNA Set A
  • HY-120041
    ND-2158
    		Inhibitor
    ND-2158 is a competitive IRAK4 inhibitor, with the Ki of 1.3 nM. ND-2158 suppresses LPS-induced TNF production in human white blood cells, alleviated collagen-induced arthritis, and blocked gout formation in mouse models. ND-2158 has antitumor activity in vivo.
    ND-2158
  • HY-158758
    PROTAC IRAK4 degrader-10
    		Degrader
    PROTAC IRAK4 degrader-10 (compound 10) is an oral active PROTAC based on Cereblon ligand, and induces the degradation of IRAK4 with maximum degradation of 95.94% and the DC50 of 7.68 nM in HEK293 cells (Sturcture Note:(Blue: Cereblon ligand, Black: linker；Pink: IRAK4 ligand).
    PROTAC IRAK4 degrader-10
  • HY-139317
    PROTAC IRAK4 degrader-6
    		Inhibitor
    PROTAC IRAK4 degrader-6 is a Cereblon-based PROTAC as interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-172.
    PROTAC IRAK4 degrader-6
  • HY-176735
    FLT3/IRAK4-IN-1
    		Inhibitor
    FLT3/IRAK4-IN-1 is a selective FLT3/IRAK4 inhibitor with the remarkable activity towards FLT3-WT (IC50 = 1.95 nM), FLT3-D835Y (IC50 = 3.22 nM) and IRAK4 (IC50 = 53.72 nM). LT3/IRAK4-IN-1 has relatively low toxicity to normal bone marrow cells, can effectively promote cell apoptosis, and has the potential to overcome drug resistance. FLT3/IRAK4-IN-1 can be used for research on acute myeloid leukemia (AML).
    FLT3/IRAK4-IN-1
  • HY-RS06894
    Irak1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Irak1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Irak1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Irak1 Mouse Pre-designed siRNA Set A
    Irak1 Mouse Pre-designed siRNA Set A
  • 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-172590
    LZ-07
    		Degrader
    LZ-07 is a IRAK4 PROTAC degrader (DC50 = 1.14 nM). LZ-07 leads to marked suppression of cytokines including IL-6, IL-1β, TNF-α, and IL-10 upon degradation of IRAK4. LZ-07 can be studied in research for autoimmune diseases (Pink: IRAK4 ligand (HY-172591); Blue: CRBN ligand (HY-34590); Black: linker (HY-B0149); CRBN ligand + linker: HY-172593).
    LZ-07
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
IRAK Isoform Comparison

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