| Identification | Back Directory | [Name]
2-Pyridinecarboxamide, N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)- | [CAS]
2227368-54-7 | [Synonyms]
JH-X-119-01
N-(4-(3-Acrylamidobenzamido)phenyl)-6-(1H-pyrazol-3-yl)picolinamide
2-Pyridinecarboxamide, N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)-
inhibit,MYD88,IRAK,IL-1R associated kinase,Waldenstr?m,Inhibitor,IRAK1,Interleukin-1 receptor associated kinase,JHX11901,Diffused Large B-cell Lymphoma,JH X 119 01,macroglobulinemia | [Molecular Formula]
C25H20N6O3 | [MDL Number]
MFCD34593626 | [MOL File]
2227368-54-7.mol | [Molecular Weight]
452.46 |
| Chemical Properties | Back Directory | [Boiling point ]
654.0±55.0 °C(Predicted) | [density ]
1.405±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 250 mg/mL (552.54 mM; Need ultrasonic) | [form ]
Solid | [pka]
10.98±0.70(Predicted) | [color ]
Light yellow to brown |
| Hazard Information | Back Directory | [Uses]
JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice[1]. JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM[2]. | [in vivo]
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. Survival is further improved when the dose is increased to 10 mg/kg[1]. | Animal Model: | C57BL/6 (20-22 g, male) mice[1] | | Dosage: | 5 mg/kg and 10 mg/kg | | Administration: | Intraperitoneally injected; 5 days | | Result: | Protected mice from LPS (20 mg/kg)-induced sepsis. Survival at day 5 was 13.3% in control group where septic mice were treated by vehicle, while the values were 37.5% and 56.3% for 5 mg/kg and 10 mg/kg. |
| [IC 50]
IRAK-1: 9 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Bin Pan, et al. Selective inhibition of interleukin-1 receptor-associated kinase 1 ameliorates lipopolysaccharide-induced sepsis in mice. Int Immunopharmacol. 2020 Aug;85:106597. DOI:10.1016/j.intimp.2020.106597
[2] John M Hatcher, et al. Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma. ACS Med Chem Lett. 2020 Oct 9;11(11):2238-2243. DOI:10.1021/acsmedchemlett.0c00378 |
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| Company Name: |
DC Chemicals
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