MTHFD2-IN-6

MTHFD2-IN-6 (Compound 41) potently and selectively inhibits recombinant human MTHFD2 over MTHFD1, with an MTHFD2 IC₅₀ of 1.46 μM and a 13-fold selectivity index^[1].
MTHFD2-IN-6 can directly bind to and stably purify recombinant human MTHFD2 protein and endogenous MTHFD2 protein in H1299 and H441 lung cancer cells; it also improves the thermostability of purified recombinant human MTHFD2 protein^[1].
MTHFD2-IN-6 (72 h) potently inhibits the proliferation of H1299 and H441 lung cancer cells (IC₅₀ < 20 μM) with low toxicity to BEAS-2B normal lung cells, and its antiproliferative activity is mediated at least in part by MTHFD2 inhibition^[1].
MTHFD2-IN-6 (10-30 μM; 2 weeks) dose-dependently inhibits colony formation in H1299 and H441 lung cancer cells, with no significant effect on BEAS-2B normal lung cells^[1].
MTHFD2-IN-6 (10-30 μM) dose-dependently induces G0/G1 phase arrest in H1299 and H441 lung cancer cells, with no effect on BEAS-2B normal lung cells^[1].
MTHFD2-IN-6 (10-30 μM; 48 h) dose-dependently induces apoptosis in H1299 and H441 lung cancer cells, with minimal apoptotic effect on BEAS-2B normal lung cells at equivalent concentrations^[1].
MTHFD2-IN-6 (10-30 μM; 24 h) dose-dependently increases intracellular ROS levels in H1299 and H441 lung cancer cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.