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JH-X-119-01 is a highly potent and selective covalent inhibitor of IRAK1 with IC50 of 9 nM.
JH-X-119-01 (10 μM) decreases phosphorylation of NF-κB and mRNA levels of IL-6 and TNFα in LPS-treated macrophages in vitro. JH-X-119-01 exhibits off-target inhibition of only two additional kinases, YSK4 (IC50=57 nM) and MEK3.
JH-X-119-01 improves survival and decreases immunopathies of LPS-challenged mice. JH-X-119-01 increases survival of mice at the dose of 5 mg/kg body weight.
Molecular Weight | 452.46 |
Formula | C25H20N6O3 |
CAS Number | 2227368-54-7 |
Solubility (25°C) | DMSO > 100 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Related IRAK Products |
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HS-243
HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC50 values of 20 and 24 nM. |
BIO-7488
BIO-7488 is a potent, selective, oral active and CNS-penetrant IRAK4 inhibitor, with IC50 values of 0.6 nM and >30 μM for IRAK4 and hERG, respectively. |
IRAK4-IN-22
IRAK4-IN-22 is an orally potent and selective potent IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively.In addition, IRAK4-IN-21 potently inhibits the production of IL-23 (IC50=0.10 µM), which may be useful in studies related to autoimmune diseases such as plaque psoriasis and psoriasis vulgaris. arthritis). |
HS271
HS271 is an orally potent and selective IRAK4 inhibitor with an IC50 value of 7.2 μM. In addition, HS271 has superior in vitro enzymatic and cellular activities. |
PROTAC IRAK4 degrader-3
PROTAC IRAK4 degrader-3 is a von Hippel-Lindau based IRAK4 degrader PROTAC. |
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