An ERK5 inhibitor
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XMD8-85

Item No. 29662

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5,11-dihydro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
CAS Number
1234479-76-5
Synonyms
  • ERK5-IN-1
Molecular Formula
C25H29N7O2
Formula Weight
459.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10mg/mLDMSO: 15mg/mLDMSO:PBS (pH 7.2) (1:1): 0.5mg/mLEthanol: 2mg/mL
λmax
291 nm
SMILES
CN1CCN(C2=CC(OC)=C(NC3=NC=C(N(C)C(C(C=CC=C4)=C4N5C)=O)C5=N3)C=C2)CC1
InChi Code
InChI=1S/C25H29N7O2/c1-29-11-13-32(14-12-29)17-9-10-19(22(15-17)34-4)27-25-26-16-21-23(28-25)30(2)20-8-6-5-7-18(20)24(33)31(21)3/h5-10,15-16H,11-14H2,1-4H3,(H,26,27,28)
InChi Key
DDTPGANIPBKTNU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    XMD8-85 is an ERK5 inhibitor (IC50 = 87 nM in an enzyme assay).1 It is selective for ERK5 over tyrosine non-receptor kinase 2 (TNK2; IC50 = 959 nM), but does inhibit the leucine-rich repeat kinase 2 (LRRK2) mutant LRRK2G2019S (IC50 = 26 nM), which has been found in patients with Parkinson’s disease.2,1 XMD8-85 inhibits EGF-induced ERK5 autophosphorylation in HeLa cells (EC50 = 0.19 μM).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Deng, X., Elkins, J.M., Zhang, J., et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur. J. Med. Chem. 70, 758-767 (2013).

    2. Groendyke, B.J., Powell, C.E., Feru, F., et al. Benzopyrimidodiazepinone inhibitors of TNK2. Bioorg. Med. Chem. Lett. 30(4), 126948 (2020).