ML-098

The Ras family of GTPases, including the Arf, Rho, Ras, and Rab GTPase subfamilies, regulates various cellular processes ranging from membrane trafficking to the control of cell proliferation. They regulate cell physiology by switching between active and inactive conformational states by binding either GTP or GDP. Alterations in GTPase function are a known hallmark of certain cancers and genetic diseases. ML-098 is an activator of the GTP-binding protein Rab7 (EC₅₀ = 77.6 nM) that demonstrates selectivity against the related GTPases cdc42, Ras, Rab-2A, and Rac1 (EC₅₀s = 588.8, 346.7, 158.5, and 794.3 nM, respectively).¹ It has been shown to function by increasing the affinity of the GTPase for guanine nucleotides.¹

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1. Surviladze, Z., Ursu, O., Miscisocia, F., et al. Three small molecule pan activator families of Ras-related GTPases. 1-42 (2009).