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JH-X-119-01

Item No. 43041

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[[3-[(1-oxo-2-propen-1-yl)amino]benzoyl]amino]phenyl]-6-(1H-pyrazol-3-yl)-2-pyridinecarboxamide
CAS Number
2227368-54-7
Molecular Formula
C25H20N6O3
Formula Weight
452.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mLPBS (pH 7.2): Insouble
SMILES
O=C(NC1=CC=C(NC(C2=CC(NC(C=C)=O)=CC=C2)=O)C=C1)C3=NC(C4=NNC=C4)=CC=C3
InChi Code
InChI=1S/C25H20N6O3/c1-2-23(32)27-19-6-3-5-16(15-19)24(33)28-17-9-11-18(12-10-17)29-25(34)22-8-4-7-20(30-22)21-13-14-26-31-21/h2-15H,1H2,(H,26,31)(H,27,32)(H,28,33)(H,29,34)
InChi Key
WQVPGYMGERDXLH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    JH-X-119-01 is a covalent inhibitor of IL-1 receptor-associated kinase 1 (IRAK1; IC50 = 9 nM).1 It is selective for IRAK1 over IRAK4 (IC50 = >10,000 nM). JH-X-119-01 is cytotoxic against a panel of mutant MyD88-expressing Waldenstrom’s macroglobulinemia (WM), ABC subtype diffuse large B cell lymphoma (DLBCL), and lymphoma cells (EC50s = 0.59-9.72 µM). It has a synergistic cytotoxic effect in MyD88-mutant-expressing BCWM.1 WM and TMD8 ABC DLBCL cells when used in combination with ibrutinib (Item No. 16274). JH-X-119-01 (5 and 10 mg/kg) also reduces lung injury and increases survival in a mouse model of LPS-induced sepsis.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hatcher, J.M., Yang, G., Wang, L., et al. Discovery of a selective, covalent IRAK1 inhibitor with antiproliferative activity in MYD88 mutated B-cell lymphoma. ACS Med. Chem. Lett. 11(11), 2238-2243 (2020).

    2. Pan, B., Gao, J., Chen, W., et al. Selective inhibition of interleukin-1 receptor-associated kinase 1 ameliorates lipopolysaccharide-induced sepsis in mice. Int. Immunopharmacol. 85, 106597 (2020).