IMP-1088

• CAT Number: I015380
• CAS Number: 2059148-82-0
• Molecular Formula: C₂₅H₂₉F₂N₅O
• Molecular Weight: 453.53
• Purity: ≥95%
• Target: DNA/RNA Synthesis

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 Kd 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].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].

Reference

[1]. Aurélie Mousnier, et al. Fragment-derived Inhibitors of Human N-myristoyltransferase Block Capsid Assembly and Replication of the Common Cold Virus. Nat Chem. 2018 Jun;10(6):599-606.