IRAK Inhibitor

Emavusertib phosphate (CA-4948 phosphate) is the phosphate salt form of Emavusertib (HY-135317). Emavusertib phosphate is an orally active inhibitor for IRAK4 (IC₅₀=57 nM) and FLT3. Emavusertib phosphate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib phosphate exhibits antitumor activity in mouse model.

AZ1495 (Standard) is the analytical standard of AZ1495 (HY-111101). This product is intended for research and analytical applications. AZ1495, a weak base, is a potent orally active interleuK_in-1 receptor associated K_inase 4 (IRAK4) inhibitor. AZ1495 has a favorable physicochemical and K_inase 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).

(S)-JNJ-1013 is an isomer of IRAK1 PROTAC degrader JNJ-1013 (HY-153188). (S)-JNJ-1013 loses VHL binding affinity (IC₅₀ >10 μM) and shows no significant IRAK1 degradation activity (DC₅₀ > 10 μM). (S)-JNJ-1013 selectively inhibits IRAK1 with an IC₅₀ of 79 nM. (S)-JNJ-1013 can be used to study cancers dependent on the scaffolding function of IRAK1.

IRAK4-IN-1 (Standard) is the analytical standard of IRAK4-IN-1 (HY-101922). This product is intended for research and analytical applications. IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC₅₀ of 7 nM.

IRAK4-IN-34 (compound 19) is a potent, selective, and orally active Interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC₅₀ of 0.73 nM. IRAK4-IN-34 exhibits good selectivity vs both hERG and other kinases. IRAK4-IN-34 shows favorable in vivo PK properties. IRAK4-IN-34 can be used for inflammatory diseases research.

Emavusertib maleate (CA-4948 maleate) is the maleate salt form of Emavusertib (HY-135317). Emavusertib maleate is an orally active inhibitor for IRAK4 (IC₅₀=57 nM) and FLT3. Emavusertib maleate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib maleate exhibits antitumor activity in mouse model.

ND-2110 is a selective IRAK4 inhibitor (K_i: 7.5 nM). ND-2110 binds to the ATP pocket of IRAK4. ND-2110 targets the subset of activated B cell-like (ABC) subtype of diffuse large B cell lymphoma (DLBCL) cell lines with MYD88 L265P mutations,. ND-2110 inhibits LPS-induced TNF production, alleviates collagen-induced arthritis, and blocks gout formation in mouse models.

JH-I-25 is an orally active IRAK1 and IRAK4 inhibitor. JH-I-25 inhibits LPS-induced IRAK4 phosphorylation, IRAK1 degradation, MAPK activation, and the expression of proinflammatory cytokines TNF-α and IL-6 in lung tissues. JH-I-25 improves the survival rate of LPS-induced septic mice and serves as an IRAK4 recruiter in the design of proteolysis-targeting chimeric molecules. JH-I-25 can be used in research related to diffuse large B-cell lymphoma, Waldenström's macroglobulinemia, septic shock, rheumatoid arthritis, atherosclerosis, Alzheimer's disease, acute lung injury, sepsis, and psoriasis.

Emavusertib tosylate (CA-4948 tosylate) is the tosylate salt form of Emavusertib (HY-135317). Emavusertib tosylate is an orally active inhibitor for IRAK4 (IC₅₀=57 nM) and FLT3. Emavusertib tosylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib tosylate exhibits antitumor activity in mouse model.

JH-X-119-01 (Standard) is the analytical standard of JH-X-119-01 (HY-103017A). This product is intended for research and analytical applications. 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.

IRAK4-IN-7 (Standard) is the analytical standard of IRAK4-IN-7 (HY-109585). This product is intended for research and analytical applications. IRAK4-IN-7 is a selective, potent and orally active interleuK_in-1 receptor-associated K_inase 4 (IRAK4) inhibitor, extracted from patent WO2015104688 (example 1). IRAK4-IN-7 has the potential for cancer and inflammatory diseases treatment.

Trimebutine (Standard) is the analytical standard of Trimebutine (HY-B0380). This product is intended for research and analytical applications. 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).

IRAK4-IN-32 (Compound 10) is a potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an enzymatic IC₅₀ value of 18.86 nM and a cellular IC₅₀ value of 6.19 nM. IRAK4-IN-32 is promising for research of inflammatory and autoimmune diseases.

Emavusertib mesylate (CA-4948 mesylate) is the mesylate salt form of Emavusertib (HY-135317). Emavusertib mesylate is an orally active inhibitor for IRAK4 (IC₅₀=57 nM) and FLT3. Emavusertib mesylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib mesylate exhibits antitumor activity in mouse model.