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 |
|---|---|---|---|---|
|
V40494 | Emavusertib (CA-4948) | 1801344-14-8 | Emavusertib (CA-4948) is a first-in-class, orally bioactive and highly potent IRAK4/FLT3 inhibtor (IC50 of < 50 nM) with anticancer activity. |
|
V75059 | GLPG2534 | 2095615-97-5 | GLPG2534 is an orally bioactive and selective IRAK4 inhibitor (antagonist) with IC50s of 6.4 nM and 3.5 nM for human and mouse IRAK4. |
|
V75066 | GNE-2256 | 2102170-43-2 | GNE-2256 (molecule 19) is an orally bioactive IRAK4 (interleukin 1 receptor-associated kinase 4) inhibitor (IRAK4 Ki=1.4 nM; IL-6 IC50=190 nM). |
|
V75064 | HS271 | 2410393-15-4 | HS271 is a potent, orally bioactive, and selective IRAK4 inhibitor (antagonist) with IC50 of 7.2 μM. |
|
V75057 | IRAK degrader-1 | 2655656-99-6 | IRAK degrader-1 (example I-3) is a potent IRAK degrader. |
|
V34066 | IRAK inhibitor 1 | 1042224-63-4 | 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. |
|
V75063 | IRAK inhibitor 4 (trans) | 2070014-89-8 | IRAK inhibitor 4 (trans) is the trans form of IRAK inhibitor 4, which is a potent inhibitor of IRAK4. |
|
V22652 | IRAK-1/4 Inhibitor | 509093-47-4 | IRAK-1-4 Inhibitor I is an IRAK1/4 inhibitor (antagonist) with IC50 of 0.2 μM and 0.3 μM respectively. |
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V75062 | IRAK-4 protein kinase inhibitor 2 | 301675-24-1 | IRAK-4 protein kinase inhibitor 2 (compound 1) is a potent inhibitor of interleukin 1 (IL-1) receptor-associated kinase 4 (IRAK-4) with IC50 of 4 μM. |
|
V6791 | IRAK-IN-6 | 1042672-97-8 | IRAK-IN-6, formerly known as IRAK inhibitor 6, is an interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor. |
|
V32176 | IRAK4-IN-1 | 1820787-94-7 | IRAK4-IN-1 is an inhibitor (blocker/antagonist) of interleukin-1 receptor-associated kinase 4 (IRAK4) with IC50 of 7 nM. |
|
V79329 | IRAK4-IN-27 | IRAK4-IN-27 (Compound 22) is a potent and specific inhibitor of IRAK4 with IC50 of 8.7 nM. | |
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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. |
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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). |
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V75067 | KTX-497 | 2432993-46-7 | KTX-497 is an orally bioactive IRAK4 degrader with DC50 of 3 nM. |
|
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. |
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