JH-X-119-01 | Selective IRAK1 inhibitor

CAS:
 2227368-54-7
Catalog Number:
 10-4691
JH-X-119-01 chemical structure Focus Biomolecules

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JH-X-119-01 (2227368-54-7) is a highly selective (only significantly inhibited YSK4 and MEK3 in a panel of over 300 kinases) and potent (IC50 = 9 nM) covalent inhibitor of interleukin 1 receptor-associated kinase 1 (IRAK1). It displayed cytotoxic activity against several lymphoma cell lines and exhibited synergism with the BTK inhibitor Ibrutinib in the same systems. JH-X-119-01 protected mice from LPS-induced sepsis2 and ameliorated acute graft-versus-host disease in mice undergoing allogenic hematopoietic cell transplantation without effecting the anti-lymphoma effect3.

References/Citations:

  1. Hatcher et al. (2020), Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma; ACS Chem. Lett. 11 2238
  2. Pan et al. (2020), Selective inhibition of interleukin-1 receptor-associated kinase 1 ameliorates lipopolysaccharide-induced sepsis in mice; Int. Immunopharmacol. 85 106597
  3. Gao et al. (2022), Inhibition of IL1 Receptor-Associated Kinase 1 Decreases Murine Acute Graft-versus-Host Disease While Preserving the Graft-versus-Lymphoma Effect; Transplant Cell Ther. 28 134.e1
CAS:
2227368-54-7
Catalog Number:
10-4691
Activity:
Selective IRAK1 inhibitor
Chemical Names:
N-(4-(3-Acrylamidobenzamido)phenyl)-6-(1H-pyrazol-5-yl)picolinamide; N-[4-[[3-(Prop-2-enoylamino)benzoyl]amino]phenyl]-6-(1H-pyrazol-5-yl)pyridine-2-carboxamide
Molecular Weight:
452.47
Molecular Formula:

C25H20N6O3

Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Yellow solid
Purity:

>98% by HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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