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IRAK

IRAK

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.

IRAK related products

Structure Cat No. Product Name CAS No. Product Description
4抑制剂 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.
BIO-7488 V86890 BIO-7488 2573211-25-1 BIO-7488 is a potent, selective, orally active and blood-brain barrier permeable IRAK4 inhibitor with IC50 values of 0.6 nM and > 30 μM for IRAK4 and hERG, respectively.
BIO-8169 V86889 BIO-8169 2792153-06-9 BIO-8169 is a selective inhibitor of interleukin receptor-associated kinase 4 (IRAK 4) with an IC50 of 0.23 nM.
DW18134 V86885 DW18134 2626988-87-0 DW18134 is an inhibitor of interleukin receptor-associated kinase 4 (IRAK 4) with IC50 of 11.2 nM.
Emavusertib (CA-4948) 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.
GLPG2534 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.
GNE-2256 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).
HS271 V75064 HS271 2410393-15-4 HS271 is a potent, orally bioactive, and selective IRAK4 inhibitor (antagonist) with IC50 of 7.2 μM.
IRAK degrader-1 V75057 IRAK degrader-1 2655656-99-6 IRAK degrader-1 (example I-3) is a potent IRAK degrader.
IRAK inhibitor 1 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.
IRAK inhibitor 4 (trans) 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.
IRAK 抑制剂 6 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.
IRAK-4 protein kinase inhibitor 2 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.
IRAK1-IN-1 V86892 IRAK1-IN-1 IRAK1-IN-1 (compound B8) is an orally active IRAK1 inhibitor.
IRAK4 modulator-1 V86891 IRAK4 modulator-1 1356014-97-5 IRAK4 modulator-1 (example 161) is a regulator of IRAK4 with IC50=4.647 μM.
IRAK4-IN-1 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.
IRAK4-IN-27 V79329 IRAK4-IN-27 IRAK4-IN-27 (Compound 22) is a potent and specific inhibitor of IRAK4 with IC50 of 8.7 nM.
IRAK4-IN-28 V75054 IRAK4-IN-28 2952532-92-0 IRAK4-IN-28 (compound 42) is an orally bioactive IRAK4 inhibitor (ICIC50=8.9 nM).
IRAK4-IN-6 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.
IRAK4-IN-7(CA4948模拟) 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.
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