Zelenirstat

Zelenirstat is an orally acitve, small-molecule, dual N-myristoyltransferase (NMT) inhibitor, with IC₅₀s of 5 nM (NMT1) and 8 nM (NMT2), respectively. Zelenirstat can induce cell apoptosis, has anti-cancer activity, inhibits early B cell receptor (BCR) signaling, and can be used to study malignant lymphoma^[1][2]. In Vitro: Zelenirstat does not inhibit any kinase at 10 µM (5380 ng/mL) and shows moderate inhibition of three kinases (MRCKA, PIP5K2B and SRPK1) at 100 µM (53800 ng/mL)^[1].
Zelenirstat (0-10 μM, 4 days) inhibits the proliferation of tumor cells such as BL2 and DOHH2, but has no effect on normal cells IM9^[2].
Zelenirstat (0-1 μM, 1 h) reduces total protein myristoylation in IM9 and BL2 and induces apoptosis of lymphoma cells^[2]. In Vivo: Zelenirstat (5-1000 mg/kg, oral, once daily, 14-21 days) has an MTD of 50 mg/kg in a 21-day study in mice, >75 mg/kg in a 14-day study in rats, and between 5 and 25 mg/kg in a 14-day study in dogs^[1].
Zelenirstat (0-50 mg/kg, subcutaneous injection, once daily; 0-15 days) induces tumor regression in BL2 xenograft mice^[2].