An ERK5 inhibitor
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AX-15836

Item No. 28774

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[2-ethoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dihydro-5-methyl-11-(methylsulfonyl)-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
CAS Number
2035509-96-5
Molecular Formula
C32H40N8O5S
Formula Weight
648.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
CN1CCN(C2CCN(C(C3=CC(OCC)=C(NC4=NC=C(N(C)C(C(C=CC=C5)=C5N6S(C)(=O)=O)=O)C6=N4)C=C3)=O)CC2)CC1
InChi Code
InChI=1S/C32H40N8O5S/c1-5-45-28-20-22(30(41)39-14-12-23(13-15-39)38-18-16-36(2)17-19-38)10-11-25(28)34-32-33-21-27-29(35-32)40(46(4,43)44)26-9-7-6-8-24(26)31(42)37(27)3/h6-11,20-21,23H,5,12-19H2,1-4H3,(H,33,34,35)
InChi Key
HTFNVAVTYILUCF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    AX-15836 is an inhibitor of ERK5 (IC50 = 8 nM).1 It is selective for ERK5 over a panel of 100 other kinases at 1 µM. AX-15836 (1 µM) inhibits ERK5 autophosphorylation in HeLa cervical cancer cells. It induces apoptosis in combination with ivermectin (Item No. 35518) in A375 melanoma spheroids when used at a concentration of 1 µM.2 AX-15836 (15 mg/kg per day) also decreases skin thickness and scaling in a mouse model of allergic skin inflammation induced by imiquimod (Item No. 14956).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lin, E.C.K., Amantea, C.M., Nomanbhoy, T.K., et al. ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc. Natl. Acad. Sci. USA 113(42), 11865-11870 (2016).

    2. Lombardi, Z., Gardini, L., Kashchuk, A.V., et al. Importin subunit beta-1 mediates ERK5 nuclear translocation, and its inhibition synergizes with ERK5 kinase inhibitors in reducing cancer cell proliferation. Mol. Oncol. 19(1), 99-113 (2025).

    3. Ding, Y., Ouyang, Z., Zhang, C., et al. Tyrosine phosphatase SHP2 exacerbates psoriasis-like skin inflammation in mice via ERK5-dependent NETosis. MedComm (2020) 3(1), e120 (2022).