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XMD8-85

Chemical Structure : XMD8-85

CAS No.: 1234479-76-5

XMD8-85 (ERK5 inhibitor XMD8-85)

Catalog No.: PC-72142Not For Human Use, Lab Use Only.

XMD8-85 is a selective ERK5 inhibitor with IC50 of 87 nM in enzyme assay.

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Biological Activity

XMD8-85 is a selective ERK5 inhibitor with IC50 of 87 nM in enzyme assay.
XMD8-85 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).
XMD8-85 inhibits EGF-induced ERK5 autophosphorylation in HeLa cells (EC50= 0.19 μM).
XMD8-85 also inhibits Brd4/BET family bromodomains, transcriptional regulators required for Nanog expression.

Physicochemical Properties

M.Wt 459.5
Formula C25H29N7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-((2-Methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-5,11-dimethyl-5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one

References

1. Deng, X, et al. Eur. J. Med. Chem. 70, 758-767 (2013).

3. Di Micco R., et al. Cell Rep. 2014;9:234–247.

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