Hypothemycin is a fungal polyketide and is a multikinase inhibitor (Kis: 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively).

ERK1:8.4 μM （ki）, MEK1:17 nM (ki), PDGFRβ:900 nM （ki）, MEK2:38 nM (ki), ERK2:2.4 μM （ki）, PDGFRα:1.5 μM （ki）, FLT3:90 nM （ki）, VEGFR2:10 nM (ki), VEGFR1:70 nM (ki)

Hypothemycin inhibits eosinophilic EOL1 cell carrying mutations in FIP1L1-PDGFRα, acute myeloid leukemia MV-4-11 cell carrying mutations in FLT3-ITD, and melanoma COLO829 cell carrying mutations in BRAF V600E. It has an IC50s of 0.4 nM, 6 nM, and 50 nM, respectively. Hypothemycin also inhibits HUVEC cell carrying mutations in VEGFR, mastocytoma P815 cell carrying mutations in c-KIT D814Y, NSCLC A459 cell carrying mutations in KRAS, and ovarian SKOV-3 cell carrying mutations in HER2 (IC50s: 70 nM, 370 nM, 6.0 μM, and 7.0 μM, respectively)[2].

Hypothemycin (10 mg/kg) kills T. brucei in infected mice. However, it completely curing the infection in one third of animals, although high doses of Hypothemycin (>10 mg/kg) leads to side effects.