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. |
-
Gut Microbes, 2024, 16(1):2402543
-
Nat Commun, 2023, 14(1):143
-
Front Immunol, 2023, 14:1266315
|
|
S8531 |
Zimlovisertib (PF-06650833)
|
Zimlovisertib (PF-06650833) is a potent, selective inhibitor of IRAK4 with an IC50 of 0.2 nM. |
-
J Gen Virol, 2023, 104(5)001858
-
Nat Commun, 2022, 13(1):4229
-
Nat Commun, 2022, 13(1):4229
|
|
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 Biol Chem, 2024, 300(8):107542
-
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
-
J Biol Chem, 2021, S0021-9258(21)00790-0
|
|
S0008 |
IRAK4-IN-1
|
IRAK4-IN-1 (Compound 23) is a highly selective inhibitor of IRAK4 with an 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. |
-
J Gen Virol, 2023, 104(5)001858
|
|
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. |
- Gut Microbes, 2024, 16(1):2402543
- Nat Commun, 2023, 14(1):143
- Front Immunol, 2023, 14:1266315
|
|
S8531 |
Zimlovisertib (PF-06650833)
|
Zimlovisertib (PF-06650833) is a potent, selective inhibitor of IRAK4 with an IC50 of 0.2 nM. |
- J Gen Virol, 2023, 104(5)001858
- Nat Commun, 2022, 13(1):4229
- Nat Commun, 2022, 13(1):4229
|
|
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 Biol Chem, 2024, 300(8):107542
- J Ethnopharmacol, 2021, S0378-8741(21)00169-0
- J Biol Chem, 2021, S0021-9258(21)00790-0
|
|
S0008 |
IRAK4-IN-1
|
IRAK4-IN-1 (Compound 23) is a highly selective inhibitor of IRAK4 with an 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. |
- J Gen Virol, 2023, 104(5)001858
|
|
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. |
|
|