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-148290
    KTX-951
    		Degrader 98.03%
    KTX-951 is an orally active IRAK4 and IMiD (Ikaros/Aiolos) substrates PROTAC degrader. KTX-951 has DC50 of 13 nM, 14 nM and 13 nM for IRAK4, Ikaros and Aiolos, respectively. TX-951 has antitumor activity.(Pink: IRAK4 ligand-12 (HY-48932); Black: Linker (HY-W382009); Blue: CRBN Ligand Pomalidomide (HY-10984))
    KTX-951
  • HY-13276
    IRAK inhibitor 2
    		Inhibitor 98.29%
    IRAK inhibitor 2 is IRAK4 (interleukin-1 receptor associated kinase 4) inhibitor .
    IRAK inhibitor 2
  • 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-123854
    PF-06426779
    		Inhibitor 99.89%
    PF-06426779 is a potent and selective inhibitor of interleukin‑1 receptor associated kinase 4 (IRAK4), with an IC50 of 0.3 nM.
    PF-06426779
  • 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
  • HY-151363
    IRAK4-IN-21
    		Inhibitor 99.54%
    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-153368
    Zomiradomide
    		Degrader
    KT-413 (example I-3) is an orally active PROTAC-class IRAK degrader. KT-413 consists of a target protein ligand (red part) PROTAC IRAK4 ligand-5 (HY-168311), an E3 ubiquitin ligase ligand (blue part) Thalidomide-4-Br (HY-W039116), and a PROTAC linker (black part) 2-(2-Azaspiro[3.3]heptan-6-yl)ethanamine (HY-168313). E3 ubiquitin ligase and linker can form Thalidomide-NH-C2-2-azaspiro[3.3]heptane (HY-168312). The active control for the target protein ligand is RSL3-4-Me (HY-169375).
    Zomiradomide
  • HY-153110A
    Larotinib mesylate hydrate
    		Inhibitor 98.66%
    Larotinib mesylate hydrate 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 mesylate hydrate
  • 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-153224
    GLPG2534
    		Inhibitor 98.73%
    GLPG2534 is an orally active and selective IRAK4 inhibitor, with IC50 values of 6.4 nM and 3.5 nM for human and mouse IRAK4. GLPG2534 can be used for the research of inflammatory skin diseases.
    GLPG2534
  • HY-148274
    KTX-582
    		Inhibitor 98.65%
    KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model.
    KTX-582
  • 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-13275
    IRAK inhibitor 1
    		Inhibitor 99.83%
    IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 3.801 μM, and >10 μM, respectively.
    IRAK inhibitor 1
  • HY-135382A
    PROTAC IRAK4 degrader-3
    		Inhibitor
    PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on von Hippel-Lindau.
    PROTAC IRAK4 degrader-3
  • 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-151365
    IRAK4-IN-22
    		Inhibitor 98.20%
    IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis.
    IRAK4-IN-22
  • HY-146112
    IRAK4-IN-14
    		Inhibitor 99.01%
    IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC50 of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib.
    IRAK4-IN-14
  • HY-13278A
    IRAK inhibitor 4 (trans)
    		Inhibitor 99.02%
    IRAK inhibitor 4 (trans) is the trans form of IRAK inhibitor 4. IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor.
    IRAK inhibitor 4 (trans)
  • HY-131903
    HS271
    		Inhibitor 99.92%
    HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties.
    HS271
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
IRAK Isoform Comparison

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