A MAP4K4 inhibitor
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DMX-5084

Item No. 42334

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3,7-dihydro-5-[4-(2-methoxyethoxy)phenyl]-7-phenyl-4H-pyrrolo[2,3-d]pyrimidin-4-one
CAS Number
2306178-56-1
Molecular Formula
C21H19N3O3
Formula Weight
361.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C1N=CNC2=C1C(C3=CC=C(OCCOC)C=C3)=CN2C4=CC=CC=C4
InChi Code
InChI=1S/C21H19N3O3/c1-26-11-12-27-17-9-7-15(8-10-17)18-13-24(16-5-3-2-4-6-16)20-19(18)21(25)23-14-22-20/h2-10,13-14H,11-12H2,1H3,(H,22,23,25)
InChi Key
FUSHFOGORKZNNQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $83

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    10 mg

    $149

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    25 mg

    $290

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    50 mg

    $495

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    Product Description

    DMX-5084 is an inhibitor of MAP4K4 (IC50 = 3 nM).1 It is selective for MAP4K4 over a panel of 141 kinases at 1 µM but does inhibit MAP4K6 and TRAF2- and NCK-interacting kinase (TNIK; IC50s = 6.61 and 10.96 nM, respectively). DMX-5084 prevents hydrogen peroxide-induced decreases in viability in vCor.4U ventricular cardiomyocytes (EC50 = 3.16 nM). It inhibits decreases in the oxygen consumption rate (OCR) and extracellular acidification rate (ECAR) induced by menadione (vitamin K3; Item No. 15950) in vCor.4U cells when used at concentrations of 3 or 10 µM. DMX-5084 prevents menadione-induced decreases in the number of beats per minute and force of contraction in a 3D human-engineered heart tissue (hEHT) model using vCor.4U cells. In vivo, DMX-5084 (50 mg/kg) reduces infarct size in a mouse model of ischemia-reperfusion injury induced by left anterior descending (LAD) coronary artery occlusion.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fiedler, L.R., Chapman, K., Xie, M., et al. MAP4K4 inhibition promotes survival of human stem cell-derived cardiomyocytes and reduces infarct size in vivo. Cell Stem Cell 24(4), 579-591 (2019).