irak1

IRAK1 4 pan-FLT3 Kinase-IN-1 (Compound 31) is a potent inhibitor of IRAK1, IRAK4, and FLT3 kinases, demonstrating IC50 values of 5 nM for IRAK1, 0.6 nM for IRAK4, and less than 0.5 nM for FLT3. It exhibits favorable pharmacokinetic properties and holds promise for research in acute myeloid leukemia, with survival extension effects comparable to Gilteritinib.

HS-243 is an inhibitor of IRAK-4 and IRAK-1 with IC50s of 20 and 24 nM. HS-243 shows anti-inflammatory and anticancer activity.

GLPG2534 is an orally active, selective and potent IRAK4 inhibitor with anti-inflammatory activity. GLPG2534 inhibits human and mouse IRAK4 and could be used to study psoriasis and atopic dermatitis.

Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM).

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. Which Shows activity in treatment of mutant MYD88L265P diffuse large B-cell lymphoma (DLBCL).

TAK-756 is a TAK1 inhibitor that selectively targets IRAK1 4 and exhibits excellent intra-articular pharmacokinetic properties. TAK1 is a potential molecular target for osteoarthritis (OA) due to its complementary anti-catabolic and anti-inflammatory effects.

HS-276 is a highly selective, orally active inhibitor of TAK1 (Ki: 2.5 nM). HS-276 significantly inhibits TAK1 (IC50: 8.25 nM), CLK2 (IC50: 29 nM), GCK (IC50: 22 nM), ULK2 (IC50: 63 nM), MAP4K5 (IC50. HS-276 can be used to study rheumatoid arthritis (RA).

NCGC1481 is a potent inhibitor of FLT3 and IRAK1/4 with improved stability, solubility, and permeability properties.

JH-X-119-01 is a highly potent and selective covalent inhibitor of IRAK-1 (Interleukin-1 Receptor-Associated Kinase 1).

Larotinib is an orally active, potent, and broad-spectrum tyrosine kinase inhibitor (TKI) with an IC50 of 0.6 nM for EGFR.

Larotinib mesylate hydrate is a potent, broad-spectrum, and orally active tyrosine kinase inhibitor (TKI), primarily targeting EGFR with an IC50 value of 0.6 nM.

IRAK-1-4 Inhibitor I is a dual inhibitor targeting IRAK1 and IRAK4.

IRAK-4 protein kinase inhibitor 2 is a potent inhibitor of interleukin-1 receptor-associated kinase-4 (IC50 = 4 μM).

KME-2780 is a potent, selective dual inhibitor of IRAK1 and IRAK4, suitable for research on dysregulation in innate immune signaling and hematologic malignancies [1].

JNJ-1013 is a potent and selective IRAK1 degrader, with IC50 values of 72 nM for IRAK1, 443 nM for IRAK4, and 1071 nM for VHL FP. It induces apoptosis, increases cleaved PARP expression, and decreases the expression of IRAK1, p-IKBα, and pSTAT3(Tyr705) [1].

JH-I-25 is an IRAK1 kinase inhibitor.

Euscaphic acid has anti-diabetic, and anti-inflammatory activities, it inhibits LPS-induced inflammatory responses by interference with the clustering of TRAF6 with IRAK1 and TAK1, resulting in blocking the activation of IKK and MAPKs signal transduction

JH-X-119-01 hydrochloride is a potent, selective inhibitor of interleukin-1 receptor-associated kinase 1 (IRAK1) that effectively alleviates lipopolysaccharide (LPS)-induced sepsis in mice.