IRAK1 Inhibitor

Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na⁺, K⁺-ATPase activity with an IC₅₀ of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .

HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a K_i of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC₅₀ values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 reduces the expression of TNF, IL-6, and IL-1β. HS-276 can be used for rheumatoid arthritis (RA) research.

JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice. JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC₅₀ of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM.

KME-2780 is the orally active inhibitor for IRAK1 and IRAK4 with IC₅₀s of 19 nM and 0.5 nM. KME-2780 can be used for research of dysregulation of innate immune signaling and hematologic malignancies.

IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride is an orally active, potent and selective IRAK/pan-FLT3 kinase inhibitor with IC₅₀s of 5 nM, 0.6 nM and <0.5 nM against IRAK1, IRAK4 and FLT3, respectively. IRAK1/4/pan-FLT3 Kinase-IN-1 hydrochloride can be used for research on AML.

HS-276 hydrochloride is an orally active, potent and highly selective TAK1 inhibitor, with a K_i of 2.5 nM. HS-276 hydrochloride shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC₅₀ values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 hydrochloride reduces the expression of TNF, IL-6, and IL-1β. HS-276 hydrochloride can be used for rheumatoid arthritis (RA) research.

AP-24567 is a Ligands for Target Protein for PROTAC, which can be used for the synthesis of SB1-G-187 (HY-137342).

AZ1495, a weak base, is a potent orally active interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor. AZ1495 has a favorable physicochemical and kinase selectivity for IRAK4 and IRAK1 with IC₅₀ values of 0.005 μM and 0.023 μM, respectively. AZ1495 has IRAK4 inhibition with a K_d value of 0.0007 μM. AZ1495 can be used for the research of diffuse large B-cell lymphoma (DLBCL).

JH-X-119-01 hydrochloride is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 hydrochloride ameliorates LPS-induced sepsis in mice.

Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC₅₀ values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC₅₀ of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity.

IRAK1/4/pan-FLT3 Kinase-IN-1 is an orally active, potent and selective IRAK/pan-FLT3 kinase inhibitor with IC₅₀s of 5 nM, 0.6 nM and <0.5 nM against IRAK1, IRAK4 and FLT3, respectively. IRAK1/4/pan-FLT3 Kinase-IN-1 can be used for research on AML.

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.

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.

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.

UR241-2 is an IRAK4 inhibitor. UR241-2 suppresses IL-1–induced IRAK1/4 signaling, NF-κβ activation, and phosphorylation of p65 and p38. UR241-2 selectively inhibits leukemia stem cell clonogenicity. UR241-2 can serve as a ligand for target proteins for PROTAC, facilitating the development and design of PROTAC degraders for IRAK4. UR241-2 can be used in the research of acute myeloid leukemia.

Ginsenoside Rb1 (Standard) is the analytical standard of Ginsenoside Rb1. This product is intended for research and analytical applications. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na⁺, K⁺-ATPase activity with an IC₅₀ of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .

IRAK4 modulator-2 (Compound 5) is a selective dual Interleukin-1 Receptor Associated Kinase 4 (IRAK4) and IRAK1 inhibitor with IC₅₀ values of 0.005 μM and 0.97 μM, erespectively. IRAK4 modulator-2 blocks IRAK-mediated signaling pathways (e.g., JAK-STAT, NF-κB pathways), reduces the production of pro-inflammatory cytokines (e.g., IL-1, TNF), and exerts anti-inflammatory activity. IRAK4 modulator-2 is promising for research of autoimmune diseases and inflammatory diseases, such as rheumatoid arthritis, psoriasis, inflammatory bowel disease.

AF-45 inhibits IRAK4 and IRAK1, with IC₅₀s of 128 nM and 1765 nM. AF-45 inhibits the release of IL-6 and TNF-α in macrophages, with IC₅₀s of 0.53-1.54 μM and 0.6-2.75 μM. AF-45 is also an inhibitor for NF-κB/MAPK signaling pathway. AF-45 exhibits anti-inflammatory activities against DSS-induced ulcerative colitis and Lipopolysaccharide (HY-D1056)-induced acute lung injury in mouse model. AF-45 exhibits good pharmacokinetic characteristics in rat models.