Catalog No.
Product Name
Application
Product Information
Citations
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IRAK-4 inhibitor
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. -
interleukin-1 receptor associated kinase inhibitor
IRAK inhibitor 2 is interleukin-1 receptor associated kinase inhibitor . -
IRAK modulator
IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2. -
IRAK4 inhibitor
IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor. -
IRAK inhibitor
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. - 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.
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Thalidomide-based Cereblon ligand
Thalidomide fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.
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IRAK4 inhibitor
AS-2444697 is a potent and selective interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with IC50 value of 21 nM. -
IRAK4 inhibitor
PF-06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4). -
IRAK4 inhibitor
IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM. -
IRAK4 inhibitor
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. -
IRAK4/FLT3 inhibitor
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. -
multi-kinase PROTAC degrader
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. -
IRAK4 degrader
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. -
TAK1 inhibitor
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). -
PROTAC IRAK4 degrader
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% at 0.01 μM, >20–50% at 0.1 μM, and >50% at 1 μM. - 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.
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PROTAC IRAK4 degrader
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. -
IRAK1 Degrader
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. -
PROTAC IRAK Degrader
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. -
IRAK4 Degrader
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. -
IRAK4 Inhibitor
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. -
IRAK4 Inhibitor
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. -
IRAK4 PROTAC Degrader
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. -
Intermediate
KTX-582 intermediate-1 is a crucial intermediate in the synthesis of KTX-582, serving as a key component for antibody-drug conjugate (ADC) preparation. KTX-582 functions as an IRAK4 degrader, effectively inducing apoptosis with DC50 values of 4 nM for IRAK4 and 5 nM for Ikaros. This compound is instrumental for research applications focused on targeting IRAK4-related pathways and exploring therapeutic strategies in various cancers. -
IRAK4 Inhibitor
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. -
TLR9 Agonist
Agatolimod is a Toll-like receptor 9 (TLR9) agonist and immunomodulator with an EC50 of 180 nM. It activates TLR9 and upregulates TLR6 expression, initiating downstream signaling through IRAK4, IRF5, and IRF7. Agatolimod enhances Th1-type immune responses and promotes the activation of various immune cells, leading to increased antigen presentation, antibody regulation, cytokine secretion, apoptosis, and enhanced cytotoxicity. This compound is relevant for research into COVID-19, breast cancer, lung adenocarcinoma, HPV-related tumors, melanoma, and salmonellosis. -
Ligand for E3 Ligase
Thalidomide 5-fluoride is a thalidomide-derived ligand for the E3 ubiquitin ligase Cereblon, enabling targeted protein degradation via the PROTAC approach. This compound can be conjugated with specific target protein ligands, such as IRAK4, to create PROTAC molecules for enhanced therapeutic applications. Notably, PROTAC IRAK4 degrader-1 demonstrated significant IRAK4 protein degradation in OCI-LY-10 cells at concentrations of 0.01, 0.1, and 1 μM, achieving degradation levels of <20%, >20-50%, and >50%, respectively. This underlines its potential utility in cellular studies of protein regulation and targeted therapeutics. -
IRAK Inhibitor
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. -
IRAK4/IRAK1 Inhibitor
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. -
IRAK1 Kinase Inhibitor
IRAK1/4/pan-FLT3 Kinase-IN-1 is a selective inhibitor targeting 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. This compound exhibits strong pharmacokinetic properties, indicating its potential for therapeutic application in acute myeloid leukemia research. Its efficacy in promoting survival suggests it may serve as a valuable tool for exploring novel treatment strategies in hematological malignancies. -
FLT3/IRAK4 Inhibitor
Lomonitinib is a potent and selective pan-FLT3/IRAK4 inhibitor that demonstrates significant antitumor activity. It is particularly relevant for research involving myeloid leukemia, where it may offer insights into therapeutic strategies targeting these pathways. Its unique mechanism of action makes it a valuable tool for investigating the roles of FLT3 and IRAK4 in cancer biology. -
FLT3/IRAK1/4 Inhibitor
NCGC1481 is a potent inhibitor of FLT3, IRAK1, and IRAK4, displaying IC50 values of <0.5 nM, 22.6 nM, and 0.8 nM, respectively. This compound effectively mitigates the adaptive resistance of leukemia cells to FLT3 inhibitors, demonstrating significant antileukemic activity. NCGC1481 is suitable for research focused on leukemia treatment and the modulation of key signaling pathways involved in cancer cell survival and proliferation. -
IRAK4 Inhibitor
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. -
TrkB Inhibitor
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. -
IRAK4 Inhibitor
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. -
IRAK4 Inhibitor
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. -
Intermediate
KTX-582 intermediate-4 is a key synthetic intermediate in the development of IRAK4 degrading agents. This compound demonstrates significant apoptotic activity, making it a valuable tool for research focused on cell death pathways. Its application extends to studies investigating inflammation and related signaling pathways, contributing to a deeper understanding of disease mechanisms. -
Intermediate
KTX-582 intermediate-3 is a crucial intermediate in the synthesis of KTX-582, which functions as an IRAK4 degrader and apoptosis inducer. This compound exhibits potent biological activity, with DC50 values of 4 nM for IRAK4 and 5 nM for Ikaros. KTX-582 intermediate-3 is valuable for applications in antibody-drug conjugate (ADC) preparation and other research endeavors aimed at studying IRAK4-related pathways and apoptosis mechanisms. -
IRAK4 Inhibitor
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. -
Intermediate
KTX-582 intermediate-2 is a crucial intermediate in the synthesis of KTX-582, which functions as an IRAK4 degrader and apoptosis inducer. This compound exhibits potent biological activity with DC50 values of 4 nM for IRAK4 and 5 nM for Ikaros. KTX-582 intermediate-2 is suitable for applications in antibody-drug conjugate (ADC) development and facilitates research into targeted therapies involving IRAK4 inhibition. -
IRAK4 Inhibitor
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. -
PROTAC IRAK4 Degrader
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. -
Anti-Inflammatory Agent
2,4′-Dihydroxybenzophenone acts as an anti-inflammatory agent by targeting the hydrophobic pocket of MD2, effectively inhibiting the dimerization of TLR4. This compound demonstrates significant biological activity by suppressing LPS-induced mitochondrial reactive oxygen species (mtROS) production and attenuating the inflammatory response through downregulation of pro-inflammatory mediators, including MyD88, p-IRAK4, and NF-κB. Additionally, 2,4′-Dihydroxybenzophenone serves as an effective UV absorber, enhancing its utility in research on oxidative stress and inflammation. -
IRAK4 PROTAC Degrader
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.
