IMP-1088

IMP-1088 is a potent human N-myristoyltransferases NMT1 and NMT2 dual inhibitor with IC₅₀s of <1 nM for HsNMT1 and HsNMT2. IMP-1088 has a K_d of <210 pM for HsNMT1. IMP-1088 efficiently blocks rhinovirus replication by blocking rhinovirus virus-encoded protein (VP0) N-myristoylation. IMP-1088 protects host cells from the cytotoxic effects of viral infection^[1]. IC50 & Target: IC50: <1 nM (HsNMT1) and <1 nM (HsNMT2)^[1]
Kd: <210 pM (HsNMT1)^[1] In Vitro: IMP-1088 (1-1000 nM) prevents virus-induced cytopathic effect (CPE) in a dose-dependent manner with an IC₅₀ of 17 nM. IMP-1088 (125 nM) complete suppresses of new infectious virus with an IC₅₀ of 5.8 nM. IMP-1088 (1-1000 nM) blocks production of infectious virus and inhibits single cycle replication in primary human bronchial epithelial cells (hBEC) infected with rhinovirus RV-A1 (MOI 5) for 7 h. IMP-1088 significantly inhibits production of infectious virus even when added up to 3 hours post-infection^[1].
IMP-1088 (50 nM) significantly less enriches multiple N-myristoylated proteins in enriched samples^[1].
IMP-1088 (500 nM) inhibits production of infectious rhinovirus particles by blocking virus assembly in HeLa cells infected with rhinovirus RV-A16 (MOI 20) for 6 h^[1].
IMP-1088 (0.24 nM-1 µM; for 24 hours +24 hours washout) has no long-term effect on cell viability and NMT activity fully recovers by 24 h^[1].
IMP-1088 potently blocks a key step in viral capsid assembly by inhibition of co-translational myristoylation of a specific virus-encoded protein (VP0). IMP-1088 blocks neither production of viral RNA, nor translation of rhinovirus polyprotein^[1].