M4K2234

M4K2234 is an inhibitor of activin receptor-like kinase 1 (ALK1) and ALK2 (IC₅₀s = 7 and 14 nM, respectively).¹ M4K2234 is selective for ALK1 and ALK2 over ALK3, -4, -5, and -6 (IC₅₀s = 168, 1,660, 1,950, and 88 nM, respectively), as well as 30 additional kinases at 1 µM, but does inhibit TRAF2- and NCK-interacting kinase (TNIK; IC₅₀ = 41 nM). M4K2234 also inhibits ALK2 containing the gain-of-function mutations ALK2^G328V, ALK2^R206H, and ALK^2R258G (IC₅₀s = 3, 6, and 6 nM, respectively).^1,2 It reduces BMP7-induced increases in the phosphorylation of SMAD1/5/8 in vitro when used at concentrations ranging from 100 to 10,000 nM and reduces the growth of SU-DIPG-XXI and HSJD-DIPG-007 cells derived from patients with diffuse intrinsic pontine gliomas (DIPGs) and containing the respective mutations ALK2^G328W and ALK2^R206H (GI₅₀s = 0.04 and 4.3 µM, respectively).¹ See the Structural Genomics Consortium (SGC) website for more information.

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1.  M4K2234 chemical probe for ALK1 and ALK2 protein kinases. https://www.thesgc.org/chemical-probes/m4k2234. (2003).

2. Ensan, D., Smil, D., Zepeda-Velázquez, C.A., et al. Targeting ALK2: An open science approach to developing therapeutics for the treatment of diffuse intrinsic pontine glioma. J. Med. Chem. 63(9), 4978-4996 (2020).