IRAK

Cat. No.

A26156

CAS No.

3091132-73-6

FIP22

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.

Cat. No.

A30038

CAS No.

525625-52-9

Agatolimod

Synonyms: ODN 2006; PF-3512676; CpG 7909; ODN 7909

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.

Cat. No.

A30246

CAS No.

2968466-26-2

KME-2780

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.

Cat. No.

A31483

CAS No.

845508-29-4

KTX-582 intermediate-1

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.

Cat. No.

A31508

CAS No.

2376399-42-5

Emavusertib hydrochloride

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.

Cat. No.

A32016

CAS No.

2751703-31-6

KT-474 hydrochloride

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.

Cat. No.

A32736

CAS No.

2626988-86-9

IRAK4-IN-27

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.

Cat. No.

A32744

CAS No.

1202401-59-9

PC-046

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.

Cat. No.

A32963

CAS No.

2376399-38-9

Emavusertib phosphate

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.

Cat. No.

A32996

CAS No.

2376399-39-0

Emavusertib maleate

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.

Cat. No.

A33002

CAS No.

1000373-79-4

KTX-582 intermediate-4

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.

Cat. No.

A33029

CAS No.

2573304-30-8

KTX-582 intermediate-3

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.

Cat. No.

A33031

CAS No.

2376399-41-4

Emavusertib tosylate

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.

Cat. No.

A33134

CAS No.

2434850-07-2

KTX-582 intermediate-2

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.

Cat. No.

A33148

CAS No.

2376399-40-3

Emavusertib mesylate

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.

Cat. No.

A33312

CAS No.

1356013-27-8

IRAK4 modulator-2

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.

Cat. No.

A33668

CAS No.

2760328-82-1

IRAK1/4/pan-FLT3 Kinase-IN-1

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.

Cat. No.

A33689

CAS No.

2923221-56-9

Lomonitinib

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.

Cat. No.

A33728

CAS No.

2193085-94-6

NCGC1481

NCGC1481 is a potent inhibitor of FLT3, IRAK1, and IRAK4, displaying IC50 values of

Cat. No.

A34333

CAS No.

1103508-80-0

Tepotinib hydrochloride

Synonyms: EMD-1214063 hydrochloride

Tepotinib hydrochloride is a highly selective, reversible, ATP-competitive inhibitor of c-Met, exhibiting an IC50 of 3 nM and over 200-fold selectivity for c-Met compared to other kinases such as IRAK4, TrkA, Axl, IRAK1, and Mer. This compound effectively inhibits c-Met phosphorylation and promotes autophagy. Tepotinib hydrochloride demonstrates significant antitumor activity and is applicable in cancer research targeting c-Met-driven pathways.

Cat. No.

A35300

CAS No.

131-56-6

2,4′-Dihydroxybenzophenone

Synonyms: Ultraviolet absorber UV-0

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.

Cat. No.

A35335

CAS No.

2432992-21-5

PROTAC IRAK4 degrader-13

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.

Cat. No.

A35442

CAS No.

1610017-20-3

BMS-986126

BMS-986126 is a potent and selective inhibitor of IRAK4, with an IC50 value of 5.3 nM. It effectively disrupts MyD88-dependent signaling pathways, thereby attenuating inflammatory responses associated with autoimmune conditions. In preclinical studies, BMS-986126 has demonstrated significant efficacy in murine models of lupus, including MRL/lpr and NZB/NZW strains. This compound is valuable for research applications related to systemic lupus erythematosus (SLE) and other autoimmune diseases.

Cat. No.

A35937

CAS No.

3065494-66-5

APH02174

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.

Cat. No.

A36111

CAS No.

3113890-51-7

PROTAC IRAK4 degrader-14

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.