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

Hypothemycin demonstrates inhibitory activity against a range of mutated cells: it targets EOL1 eosinophilic cells with FIP1L1-PDGFRα mutations, MV-4-11 acute myeloid leukemia cells with FLT3-ITD mutations, and COLO829 melanoma cells with BRAF V600E mutations, displaying IC50 values of 0.4 nM, 6 nM, and 50 nM, respectively. Additionally, it inhibits HUVEC cells with VEGFR mutations, P815 mastocytoma cells with c-KIT D814Y mutations, A459 non-small cell lung cancer (NSCLC) cells with KRAS mutations, and SKOV-3 ovarian cells with HER2 mutations, with IC50 values of 70 nM, 370 nM, 6.0 μM, and 7.0 μM, respectively.

Hypothemycin (10 mg/kg) eradicates T. brucei in infected mice, fully curing one-third of them, though higher doses (>10 mg/kg) result in side effects.