Through their function in Toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) mediated signaling pathways, interleukin-1 receptor-associated kinases (IRAKs), which are serine/threonine kinases, play critical roles in initiating innate immune responses against foreign pathogens and other types of dangers. Two active kinases, IRAK-1 and IRAK-4, and two inactive kinases, IRAK-2 and IRAK-M, are among the four distinct IRAK-like molecules that have been discovered. Nuclear factor-kappaB (NF-B) and mitogen-activated protein kinase (MAPK) pathways are both activated by all IRAKs.
The adaptor molecule MyD88 and the IRAK-1, 2, M, and 4 members of the IL-1R-associated kinase family are used by toll-like receptors to transmit their signals. The Myddosomes formed by MyD88-IRAK-4, IRAK-1, and IRAK-2 are known to mediate TLR7-induced, TAK1-dependent NF-B activation. It is known that IRAK-M acts as a negative regulator, preventing the dissociation of IRAKs from MyD88 and obstructing subsequent signaling.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V79329 | IRAK4-IN-27 | IRAK4-IN-27 (Compound 22) is a potent and specific inhibitor of IRAK4 with IC50 of 8.7 nM. | |
|
V75054 | IRAK4-IN-28 | 2952532-92-0 | IRAK4-IN-28 (compound 42) is an orally bioactive IRAK4 inhibitor (ICIC50=8.9 nM). |
|
V75055 | IRAK4-IN-6 | 2454244-02-9 | IRAK4-IN-6 is an oral, potent and specific IRAK inhibitor (antagonist) with IC50 of 4 nM, targeting MyD88 L265P mutant diffuse large B-cell lymphoma. |
|
V3947 | IRAK4-IN-7 (CA4948 analog) | 1801343-74-7 | IRAK4-IN-7 (CA-4948 analog; AU-4948) is a novel, potent, selective, and orally bioactive small molecule inhibitor of IRAK4 (interleukin-1 receptor-associated kinase 4) which has the potential to be used as a therapeutic agent for hematological cancers with dysregulated TLR/MYD88/IRAK4 signaling. |
|
V2464 | JH-X-119-01 | 2227368-54-7 | JH-X-119-01 (JH-X119-01) is a novel, potent, selective and covalent inhibitor of IRAK1 (interleukin-1 receptor-associated kinases 1) (IC50 = 9 nM) with anticancer activity. |
|
V75058 | JH-X-119-01 hydrochloride | 2591344-30-6 | JH-X-119-01 HCl is a potent and specific inhibitor of interleukin 1 receptor-associated kinase 1 (IRAK1). |
|
V83498 | KME-2780 | 2968466-26-2 | |
|
V75067 | KTX-497 | 2432993-46-7 | KTX-497 is an orally bioactive IRAK4 degrader with DC50 of 3 nM. |
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V75070 | KTX-612 | 2573298-14-1 | KTX-612 is an orally bioactive IRAK4 degrader with DC50 of 7 nM. |
|
V75065 | KTX-955 | 2573302-50-6 | KTX-955 is a potent IRAK4 degrader with DC50s of 5 nM and 130 nM for IRAK4 and Ikaros, respectively. |
|
V86886 | LC-MI-3 | LC-MI-3 is an orally active, potent interleukin-1 receptor-associated kinase 4 (IRAK4) PROTAC degrader with a DC50 value of 47.3 nM. | |
|
V75060 | PF-06426779 | 1817628-40-2 | PF-06426779 is a potent and specific inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) with IC50 of 0.3 nM. |
|
V75056 | PROTAC IRAK4 degrader-8 | 2911615-06-8 | PROTAC IRAK4 degrader-8 (compound 2) is a PROTAC targeting IRAK4 (IC50=15.5 nM). |
|
V4593 | Takinib | 1111556-37-6 | Takinib is a novel, potent and selectiveTAK1inhibitor with anIC50of 9.5 nM. |
|
V75052 | Zabedosertib (BAY 1834845) | 1931994-81-8 | Zabedosertib (BAY 1834845) is an IRAK4 inhibitor (antagonist) with immunomodulatory potential. |
|
V4562 | Zimlovisertib (PF06650833) | 1817626-54-2 | PF06650833 is a novel, potent and selective inhibitor ofInterleukin-1 receptor associated kinase 4 (IRAK4) which is used to treat autoimmune diseases such as rheumatoid arthritis, lupus, and lymphomas. |
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