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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 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2.
Synonyms: PROTAC IRAK4 degrader-7; KYM-001
KT-474 (SAR444656) is a selective small-molecule PROTAC degrader of IRAK4, under development for the treatment of TLR/IL-1R–mediated autoimmune diseases. It effectively suppresses R848 (TLR7/8)- and LPS-induced IL-6 and IL-8 production in peripheral blood mononuclear cells (PBMCs), highlighting its potential as an anti-inflammatory therapeutic.
PROTAC IRAK3 Degrader-1 (Compound 23) is a potent and selective PROTAC molecule targeting IRAK3, with an IC₅₀ of 5 nM. It enables efficient degradation of IRAK3, providing a valuable tool for studying innate immune signaling and inflammatory pathways.
PROTAC IRAK4 Degrader-1 is a cereblon-based PROTAC targeting IRAK4, derived from US patent US20190192668A1 (Compound I-210). It induces IRAK4 degradation in OCI-LY-10 cells with 20–50% at 0.1 μM, and >50% at 1 μM.
KTX-582 is a potent heterobifunctional PROTAC degrader that targets interleukin-1 receptor–associated kinase 4 (IRAK4) and the transcription factor Ikaros, with DC₅₀ values of 4 nM and 5 nM, respectively. It induces apoptosis in MYD88^L265P-mutant diffuse large B-cell lymphoma (DLBCL) cells, a subtype characterized by constitutive IRAK4 signaling. In preclinical lymphoma models, KTX-582 effectively drives in vivo tumor regression, highlighting its therapeutic potential for MYD88-mutant hematologic malignancies.
SB1-G-187 is a multifunctional PROTAC designed as a multi-kinase degrader, capable of inducing the selective degradation of multiple kinase targets through the ubiquitin–proteasome system. In addition to its targeted degradation activity, SB1-G-187 features an alkyne functional group, enabling its use as a click chemistry reagent. It can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules, allowing for versatile applications in chemical biology, such as probe development, conjugation, and target identification.
JNJ-1013 is a selective degrader of IRAK1, demonstrating potent efficacy with IC50 values of 72 nM for IRAK1, 443 nM for IRAK4, and 1071 nM for VHL. This compound induces apoptosis and promotes the cleavage of PARP, signaling significant pro-apoptotic activity. Additionally, JNJ-1013 effectively reduces the expression of IRAK1, phosphorylated IKBα, and phosphorylated STAT3 (Tyr705), making it a valuable tool for research in inflammatory pathways and therapeutic interventions targeting IRAK1.
Synonyms: KT-413
Zomiradomide is an orally bioavailable PROTAC degrader targeting IRAK4, with a DC50 of 6 nM, which effectively inhibits the NF-κB signaling pathway. In addition to its suppression of IRAK4, Zomiradomide functions as a molecular glue, facilitating the degradation of Ikaros with a DC50 of 1 nM and consequently activating the type I IFN signaling pathway. This dual action positions Zomiradomide as a valuable tool in research focused on immune modulation and inflammatory responses.
KTX-951 is a selective IRAK4 degrader that employs a PROTAC mechanism to facilitate targeted degradation of IRAK4 and IMiD substrates, including Ikaros and Aiolos. With a Kd of 3.5 nM and DC50 values of 13 nM for IRAK4, Ikaros, and Aiolos, KTX-951 demonstrates potent biological activity. It also exhibits an IC50 of 35 nM against OCl-Ly10 CTG, indicating its potential use in antitumor research applications.
FIP22 is a potent and selective degrader of IRAK4 utilizing the PROTAC technology. It functions by inducing degradation through the formation of a ternary complex consisting of IRAK4, FIP22, and CRBN, with an EC50 of 12.63 nM. This mechanism effectively inhibits IRAK4-mediated signaling pathways, including NF-κB and MAPK pathways, making FIP22 valuable for research into conditions such as atopic dermatitis, where IRAK4 plays a critical role.
Synonyms: KYM-001 hydrochloride; PROTAC IRAK4 degrader-7 hydrochloride
KT-474 hydrochloride is a potent PROTAC degrader targeting IRAK4, exhibiting significant anti-tumor properties. This compound inhibits the cell cycle and induces apoptosis in affected cells, demonstrating tumor regression in xenograft models of MYD88-mutated ABC DLBCL. Additionally, KT-474 features an alkyne group facilitating click chemistry, allowing for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it a valuable tool for chemical biology research.
PROTAC IRAK4 degrader-13 is a selective IRAK4-directed PROTAC degrader that effectively targets IRAK4 with DC50 values of 0.86 nM and 1.1 nM in monocytes and lymphocytes, respectively. This compound significantly activates TIR signaling and reduces the expression of proinflammatory cytokines in an Imiquimod-induced psoriasis mouse model. PROTAC IRAK4 degrader-13 is applicable in research focused on TLR- and IL-1R-driven inflammatory diseases, including hidradenitis suppurativa and atopic dermatitis.
APH02174 is a highly selective IRAK4 PROTAC degrader that exhibits an impressive DC50 value of 4.01 nM in THP-1 cells. By effectively inhibiting the release of IL-6, APH02174 serves to block inflammatory signaling pathways. This compound is valuable for research into various inflammatory conditions, including psoriasis vulgaris and rheumatoid arthritis.
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PROTAC IRAK4 degrader-14 is an orally active degrader targeting IRAK4 with a DC50 of 2.4 nM. It functions by selectively degrading IRAK4, thereby inhibiting pro-inflammatory responses in various cell types, including T cells, monocytes, and keratinocytes. This compound has significant relevance in research focused on inflammatory diseases, particularly psoriasis.
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Synonyms: IRAK-1 (360-380)
IRAK-4 Peptide substrate (IRAK-1 residues 360-380) is a bioactive peptide specifically designed to serve as a substrate for Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4). This peptide facilitates the study of IRAK-4's role in signal transduction pathways associated with inflammatory responses. It is suitable for applications in cellular signaling research, particularly in the context of immune system studies and cytokine signaling.
PROTAC IRAK4 Degrader-3 is a PROTAC-based ligand designed to target and induce the degradation of interleukin-1 receptor-associated kinase 4 (IRAK4) via the von Hippel-Lindau (VHL) E3 ubiquitin ligase. This compound effectively modulates the inflammatory response by selectively degrading IRAK4, making it a valuable tool for exploring therapeutic strategies in inflammatory diseases and immune signaling pathways. Its application in research can provide insights into IRAK4's role in various pathologies, including cancer and autoimmune disorders.
PROTAC IRAK4 Degrader-8 is a targeted protein degradation compound designed to selectively degrade IRAK4, demonstrating an IC50 of 15.5 nM. This reagent effectively induces IRAK4 degradation in THP-1 cells with a DC50 of 1.8 nM. Additionally, PROTAC IRAK4 Degrader-8 inhibits L-6 production in human whole blood and LPS-induced human peripheral blood mononuclear cells, exhibiting IC50 values of 246 nM and 2.2 nM, respectively. This compound is a valuable tool for studying the role of IRAK4 in immune responses and offers potential applications in inflammatory and autoimmune research.
PROTAC IRAK4 Degrader-5 is a Cereblon-based targeted protein degrader specifically designed to induce the degradation of IRAK4. By modulating the ubiquitin-proteasome system, it enhances protein turnover, leading to a decrease in IRAK4 levels. This compound is valuable for research applications focused on inflammation and immune response regulation, enabling the investigation of IRAK4's role in various disease models.
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PROTAC IRAK4 degrader-12 is a PROTAC compound designed to selectively target and induce the degradation of IRAK4 via the Cereblon E3 ligase pathway. It demonstrates a significant degradation efficacy, achieving a maximum degradation rate of 108.46% in K562 cells with an IC50 of 4.87 nM. This reagent is particularly useful for research applications focused on inflammatory signaling pathways and therapeutic development targeting IRAK4-related diseases.
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IRAK4 modulator-1 is a selective modulator of IRAK4, demonstrating an IC50 of 4.647 μM. This compound is instrumental in the exploration of IRAK-mediated signaling pathways, making it a valuable tool for investigating diseases associated with dysregulated inflammation and immune responses. Researchers can utilize IRAK4 modulator-1 to further understand the role of IRAK4 in various pathological conditions.
PROTAC IRAK3 degrader-2 is a potent IRAK3 PROTAC degrader with a DC50 of less than or equal to 50 nM. This compound promotes the ubiquitination and subsequent degradation of the IRAK3 protein, making it a valuable tool for studying immune-related diseases. Its unique design incorporates ligands for E3 ligase and a linker configuration, facilitating targeted degradation and aiding research into therapeutic strategies for modulating immune responses.
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PROTAC IRAK4 Degrader-2 is a PROTAC-based compound designed to target and degrade IRAK4, displaying potent degradation efficacy with a DC50 value of 151 nM in peripheral blood mononuclear cells (PBMCs). It effectively reduces IRAK4 protein levels, achieving a DC50 of 36 nM in these cells. Additionally, PROTAC IRAK4 Degrader-2 inhibits the production of multiple cytokines, making it a valuable tool for research in inflammation and immune response modulation.
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KTX-612 is an orally bioavailable IRAK4 PROTAC degrader with a DC50 value of 7 nM. This compound is designed to selectively target and promote the degradation of IRAK4, a key protein involved in inflammatory and oncogenic signaling pathways. KTX-612 has potential applications in oncology research, facilitating studies focused on the modulation of IRAK4 and its implications in cancer progression and treatment.
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PROTAC IRAK3 degrader-1 is a potent and selective degrader targeting IRAK3, with an IC50 of 5 nM. This compound effectively facilitates the ubiquitination and subsequent degradation of IRAK3, thereby modulating inflammatory responses. Its primary research applications include studies on innate immunity and the development of targeted therapies for inflammatory diseases.
PROTAC IRAK4 degrader-4 is a Cereblon-based bifunctional molecule designed to degrade interleukin-1 receptor-associated kinase 4 (IRAK4). This compound facilitates targeted protein degradation, leading to effective modulation of IRAK4 levels in cells. Research applications include investigating inflammatory signaling pathways and therapeutic approaches for autoimmune diseases.
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