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IRAK inhibitors act on interleukin-1 receptor-associated kinases (IRAKs), kinases of innate immune receptor signaling. IRAK was cloned in 1996 as a serine/threonine kinase that associates with the interleukin-1 (IL-1) receptor after stimulation. Mice lacking IRAK4 showed severe defects in IL-1 and Toll-like receptor signaling, which established a central role for this family member. The adaptor myeloid differentiation primary response 88 (MyD88) recruits IRAK4, which then phosphorylates IRAK1 on the route to nuclear factor kappa B activation. Emavusertib, listed as CA-4948, and IRAK inhibitor 4 target IRAK4, while IRAK-1-4 Inhibitor I blocks both IRAK1 and IRAK4. The list also contains compounds with other targets, such as the c-Jun N-terminal kinase inhibitor JNK-IN-7.
IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 3.801 μM, and >10 μM, respectively.
IRAK inhibitor 2 is interleukin-1 receptor associated kinase inhibitor .
IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor.
Synonyms: IRAK-IN-6
IRAK-IN-6, also known as IRAK inhibitor 6, is an interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor. IRAK-4 is reported to be essential for the activation of the intracellular signalling cascades including NF-kB and MAPK pathways, which are critical for the production of inflammatory cytokines.
Synonyms: IRAK-1/4 Inhibitor I
IRAK-1-4 inhibitor is a benzimidazole that disrupts the activity of IRAK-1 and -4 with IC50 values of 300 and 200 nM, respectively.
CA-4948 is a potent, and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor. CA-4948 exhibited the greatest efficacy in four of the five ABC-DLBCL PDX models tested as compared to GBC-DLBCL and ABC/GCB DLBCL PDX models.
AS-2444697 is a potent and selective interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with IC50 value of 21 nM.
PF-06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4).
AZ1495 (compound 28) 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.
IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.
HS-243 is an inhibitor of transforming growth factor-beta kinase. HS-243 can be used in treatment of cancer, malaria, inflammatory and other TAK1-mediated diseases.
IRAK4-IN-4 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM.
Synonyms: CA-4948
Emavusertib, also known as CA-4948 is a potent IRAK4/FLT3 inhibitor with anti-tumor activity. CA-4948 demonstrated good cellular activity in ABC DLBCL and AML cell lines. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation.
HS-276 is an orally bioavailable, potent, and highly selective inhibitor of transforming growth factor-β–activated kinase 1 (TAK1), with a Kᵢ of 2.5 nM. It exhibits strong inhibition of TAK1 and moderate activity against a panel of other kinases, including CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with respective IC₅₀ values ranging from 8.25 to 5585 nM. HS-276 is a valuable tool for investigating TAK1-mediated signaling pathways and holds therapeutic potential for inflammatory conditions such as rheumatoid arthritis (RA).
IRAK4-IN-33 is a selective and potent inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4), exhibiting an IC50 of 0.36 nM. This compound effectively disrupts the pro-inflammatory signaling pathway associated with IRAK4, leading to decreased release of inflammatory cytokines such as TNFα and IFNα. IRAK4-IN-33 demonstrates minimal inhibition of the hERG channel, with an IC50 greater than 30 μM, making it a valuable tool for studying inflammation and immunological disorders, including rheumatoid arthritis.
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GLPG4471 is a selective inhibitor of IRAK4, demonstrating an IC50 of 1.7 nM. It exhibits potent inhibition of cytokine secretion, including TNFα and IFNα, in both cellular and whole blood assays. Notably, GLPG4471 shows significant therapeutic activity in a mouse model of collagen-induced arthritis, making it a valuable tool for researching inflammatory conditions such as arthritis.
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KME-2780 is an orally active inhibitor targeting IRAK1 and IRAK4, exhibiting IC50 values of 19 nM and 0.5 nM, respectively. It plays a crucial role in the modulation of innate immune signaling pathways, making it a valuable tool for investigating dysregulation associated with hematologic malignancies and related disorders. Researchers can utilize KME-2780 to explore the therapeutic potential of IRAK inhibition in various immunological contexts.
Synonyms: CA-4948 hydrochloride
Emavusertib hydrochloride is an orally active inhibitor targeting IRAK4, with an IC50 of 57 nM, and FLT3. This compound effectively inhibits NF-κB and MyD88 signaling pathways, resulting in decreased production of pro-inflammatory cytokines such as IL-6 and IL-10. Its anti-inflammatory and anti-proliferative properties make it a valuable tool for cancer research, as it promotes apoptosis in cancer cells and demonstrates antitumor efficacy in mouse model studies.
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IRAK4-IN-27 is a selective inhibitor of IRAK4, exhibiting an IC50 of 8.7 nM. This compound effectively inhibits cell growth and induces apoptosis in MYD88 L265P diffuse large B-cell lymphoma (DLBCL) cell lines. IRAK4-IN-27 is an important tool for studying the mechanisms underlying DLBCL and developing potential therapeutic strategies.
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PC-046 is a potent multitarget inhibitor of tyrosine receptor kinase B (TrkB), IRAK-4, and Pim-1, with IC50 values of 13.4 μM, 15.4 μM, and 19.1 μM, respectively. This compound demonstrates significant cytotoxicity against BxPC3 pancreatic cancer cells, with an IC50 range of 7.5-130 nM. PC-046 effectively induces apoptosis and disrupts the cell cycle at the G2/M phase in these cells. Additionally, it showcases promising antitumor efficacy and favorable pharmacokinetic properties in murine models, making it a valuable tool for cancer research.
Synonyms: CA-4948 phosphate
Emavusertib phosphate is a potent inhibitor of IRAK4, exhibiting an IC50 of 57 nM. This compound effectively disrupts NF-κB and MyD88 signaling pathways, leading to a significant reduction in pro-inflammatory cytokines such as IL-6 and IL-10. Emavusertib phosphate demonstrates both anti-inflammatory and anti-proliferative effects on cancer cells, promoting apoptosis and showcasing antitumor activity in preclinical mouse models. Its applications extend to investigating inflammatory diseases and cancer therapies.
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Synonyms: CA-4948 maleate
Emavusertib maleate is a potent inhibitor of IRAK4, demonstrating an IC50 of 57 nM, and FLT3. This orally bioavailable compound inhibits NF-κB and MyD88 signaling pathways, effectively reducing the production of pro-inflammatory cytokines such as IL-6 and IL-10. Its anti-inflammatory and anti-proliferative properties make it a valuable tool for cancer research, promoting apoptosis in cancer cells and demonstrating antitumor activity in preclinical mouse models.
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Synonyms: CA-4948 tosylate
Emavusertib tosylate is a potent inhibitor of IRAK4, displaying an IC50 of 57 nM. By targeting IRAK4 and FLT3, it effectively disrupts NF-κB and MyD88 signaling pathways, resulting in the reduction of pro-inflammatory cytokines such as IL-6 and IL-10. This compound demonstrates significant anti-inflammatory and anti-proliferative properties against cancer cells, promoting apoptotic mechanisms. Additionally, Emavusertib tosylate has shown noteworthy antitumor activity in preclinical mouse models, making it a valuable reagent for cancer research and inflammation studies.
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Synonyms: CA-4948 mesylate
Emavusertib mesylate is a potent inhibitor of IRAK4, demonstrating an IC50 of 57 nM. This orally active compound effectively disrupts the NF-κB and MyD88 signaling pathways, leading to a reduction in pro-inflammatory cytokines such as IL-6 and IL-10. Emavusertib mesylate displays anti-inflammatory and anti-proliferative properties against cancer cells, promoting apoptosis. Additionally, it has shown significant antitumor activity in mouse models, making it valuable for cancer research and therapeutic studies targeting inflammatory pathways.
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IRAK4 modulator-2 is a selective inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) and IRAK1, exhibiting IC50 values of 0.005 μM and 0.97 μM, respectively. This compound effectively disrupts IRAK-mediated signaling pathways, including JAK-STAT and NF-κB pathways, leading to a reduction in pro-inflammatory cytokine production, such as IL-1 and TNF. IRAK4 modulator-2 demonstrates potential for use in research focusing on autoimmune and inflammatory diseases, including rheumatoid arthritis, psoriasis, and inflammatory bowel disease.
