IRAK

Isoform-selective Products

IRAK Products

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  • IRAK Inhibitors (16)
  • New IRAK Products
Catalog No. Product Name Information Product Use Citations Product Validations
S8663 Takinib Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib induces apoptosis.
Nat Commun, 2023, 14(1):143
Front Immunol, 2023, 14:1266315
Cells, 2023, 12(23)2696
S8531 Zimlovisertib (PF-06650833) Zimlovisertib (PF-06650833) is a potent, selective inhibitor of IRAK4 with an IC50 of 0.2 nM.
Nat Commun, 2022, 13(1):4229
Nat Commun, 2022, 13(1):4229
J Innate Immun, 2022, 1-11
S3924 Ginsenoside Rb1 Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
J Biol Chem, 2021, S0021-9258(21)00790-0
Mol Immunol, 2021, 139:140-152
S0008 IRAK4-IN-1 IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with IC50 of 7 nM.
Syst Biol Reprod Med, 2022, 1-15
Histochem Cell Biol, 2021, 156(3):227-237
S8562 IRAK4-IN-2 IRAK4-IN-2 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades.
Cancer Lett, 2021, 503:75-90
Cancer Lett, 2021, 503:75-90
S6598 IRAK-1-4 Inhibitor I IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor associated kinase (IRAK) with IC50 values of 0.3 μM and 0.2 μM for IRAK-1 and IRAK-4, respectively. It displays IC50 values >10 µM in a panel of 27 other kinases tested.
Nat Commun, 2022, 13(1):6226
Nat Commun, 2022, 13(1):6226
S9779 Emavusertib (CA-4948) Emavusertib (CA-4948) is a potent and orally bioavailable inhibitor of interleukin-1 receptor-associated kinase 4/FMS-like Tyrosine Kinase 3 (IRAK4/FLT3) with anti-tumor activity.
Arthritis Rheumatol, 2021, 10.1002/art.42043
S3607 Sarsasapogenin Sarsasapogenin (SAR, Parigenin) is a steroidal sapogenin. It can provoke the generation of reactive oxygen species and activate unfolded protein response (UPR) signaling pathways. SAR potently inhibits NF-κB and MAPK activation, as well as IRAK1, TAK1, and IκBα phosphorylation in LPS-stimulated macrophages.
J Exp Clin Cancer Res, 2022, 41(1):174
E1655New KT 474 KT-474 (SAR444656) is a selective small-molecule degrader of IRAK4 in development for the treatment of TLR/IL-1R–driven autoimmune diseases. KT-474 potently downregulates R848 (TLR7/8) and lipopolysaccharide (LPS)-induced IL-6 and IL-8 production in peripheral blood mononuclear cells (PBMCs).
E2837 Zabedosertib Zabedosertib (BAY 1834845) is a IRAK4 inhibitor with immunomodulatory potential, which is a protein kinase involved in signaling innate immune responses from Toll-like receptors.
S0775 IRAK4-IN-4 IRAK4-IN-4 (compound 15) is an inhibitor of interleukin-1 receptor–associated kinase 4 (IRAK4) and cyclic GMP-AMP synthase (cGAS) with IC50 of 2.8 nM and 2.1 nM, respectively.
S9780 JH-X-119-01 JH-X-119-01 is a highly potent and selective covalent inhibitor of IRAK1 with IC50 of 9 nM.
S9701 HS-243 HS-243 is a highly potent interleukin-1 receptor-associated kinase (IRAK) inhibitor with IC50 of 24 nM, 20 nM and 0.5 μM for IRAK-1, IRAK-4 and TAK1, respectively.
S2039 IRAK inhibitor 6 IRAK inhibitor 6 is a selective Interleukin-1 receptor-associated kinase 4(IRAK4) inhibitor with IC50 of 0.16 μM.
E0533 IRAK-4 protein kinase inhibitor 2 IRAK-4 protein kinase inhibitor 2 is a potent inhibitor of interleukin-1 (IL-1) receptor-associated kinase-4 (IRAK-4), with an IC50 of 4 μM.
E2647 AZ1495 AZ1495 is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively.
S8663 Takinib Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib induces apoptosis.
Nat Commun, 2023, 14(1):143
Front Immunol, 2023, 14:1266315
Cells, 2023, 12(23)2696
S8531 Zimlovisertib (PF-06650833) Zimlovisertib (PF-06650833) is a potent, selective inhibitor of IRAK4 with an IC50 of 0.2 nM.
Nat Commun, 2022, 13(1):4229
Nat Commun, 2022, 13(1):4229
J Innate Immun, 2022, 1-11
S3924 Ginsenoside Rb1 Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
J Biol Chem, 2021, S0021-9258(21)00790-0
Mol Immunol, 2021, 139:140-152
S0008 IRAK4-IN-1 IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with IC50 of 7 nM.
Syst Biol Reprod Med, 2022, 1-15
Histochem Cell Biol, 2021, 156(3):227-237
S8562 IRAK4-IN-2 IRAK4-IN-2 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades.
Cancer Lett, 2021, 503:75-90
Cancer Lett, 2021, 503:75-90
S6598 IRAK-1-4 Inhibitor I IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1 receptor associated kinase (IRAK) with IC50 values of 0.3 μM and 0.2 μM for IRAK-1 and IRAK-4, respectively. It displays IC50 values >10 µM in a panel of 27 other kinases tested.
Nat Commun, 2022, 13(1):6226
Nat Commun, 2022, 13(1):6226
S9779 Emavusertib (CA-4948) Emavusertib (CA-4948) is a potent and orally bioavailable inhibitor of interleukin-1 receptor-associated kinase 4/FMS-like Tyrosine Kinase 3 (IRAK4/FLT3) with anti-tumor activity.
Arthritis Rheumatol, 2021, 10.1002/art.42043
S3607 Sarsasapogenin Sarsasapogenin (SAR, Parigenin) is a steroidal sapogenin. It can provoke the generation of reactive oxygen species and activate unfolded protein response (UPR) signaling pathways. SAR potently inhibits NF-κB and MAPK activation, as well as IRAK1, TAK1, and IκBα phosphorylation in LPS-stimulated macrophages.
J Exp Clin Cancer Res, 2022, 41(1):174
E1655New KT 474 KT-474 (SAR444656) is a selective small-molecule degrader of IRAK4 in development for the treatment of TLR/IL-1R–driven autoimmune diseases. KT-474 potently downregulates R848 (TLR7/8) and lipopolysaccharide (LPS)-induced IL-6 and IL-8 production in peripheral blood mononuclear cells (PBMCs).
E2837 Zabedosertib Zabedosertib (BAY 1834845) is a IRAK4 inhibitor with immunomodulatory potential, which is a protein kinase involved in signaling innate immune responses from Toll-like receptors.
S0775 IRAK4-IN-4 IRAK4-IN-4 (compound 15) is an inhibitor of interleukin-1 receptor–associated kinase 4 (IRAK4) and cyclic GMP-AMP synthase (cGAS) with IC50 of 2.8 nM and 2.1 nM, respectively.
S9780 JH-X-119-01 JH-X-119-01 is a highly potent and selective covalent inhibitor of IRAK1 with IC50 of 9 nM.
S9701 HS-243 HS-243 is a highly potent interleukin-1 receptor-associated kinase (IRAK) inhibitor with IC50 of 24 nM, 20 nM and 0.5 μM for IRAK-1, IRAK-4 and TAK1, respectively.
S2039 IRAK inhibitor 6 IRAK inhibitor 6 is a selective Interleukin-1 receptor-associated kinase 4(IRAK4) inhibitor with IC50 of 0.16 μM.
E0533 IRAK-4 protein kinase inhibitor 2 IRAK-4 protein kinase inhibitor 2 is a potent inhibitor of interleukin-1 (IL-1) receptor-associated kinase-4 (IRAK-4), with an IC50 of 4 μM.
E2647 AZ1495 AZ1495 is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively.
E1655New KT 474 KT-474 (SAR444656) is a selective small-molecule degrader of IRAK4 in development for the treatment of TLR/IL-1R–driven autoimmune diseases. KT-474 potently downregulates R848 (TLR7/8) and lipopolysaccharide (LPS)-induced IL-6 and IL-8 production in peripheral blood mononuclear cells (PBMCs).

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