IMP1088|IMP-1088|NMT1/NMT2 dual inhibitor

Cas No.:	2059148-82-0
Synonyms:	IMP-1088,IMP1088,IMP 1088
SMILES:	CN1N=C(CN(C)C)C2=C1C=CC(C3=CC=C(F)C(F)=C3OCCC4=C(C)N(C)N=C4C)=C2
Formula:	C₂₅H₂₉F₂N₅O
M.Wt:	453.53
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

IMP-1088, a picomolar dual inhibitor of the human N-myristoyltransferases NMT1 and NMT2, and use it to demonstrate that pharmacological inhibition of host-cell N-myristoylation rapidly and completely prevents rhinoviral replication without inducing cytotoxicity. The identification of cooperative binding between weak-binding fragments led to rapid inhibitor optimization through fragment reconstruction, structure-guided fragment linking and conformational control over linker geometry. The inhibition of the co-translational myristoylation of a specific virus-encoded protein (VP0) by IMP-1088 potently blocks a key step in viral capsid assembly, to deliver a low nanomolar antiviral activity against multiple RV strains, poliovirus and foot and-mouth disease virus, and protection of cells against virus-induced killing, highlighting the potential of host myristoylation as a drug target in picornaviral infections.

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