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 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.

Product information

CAS Number: 2059148-82-0

Molecular Weight: 453.53

Formula: C25H29F2N5O

Chemical Name: [(5-{3,4-difluoro-2-[2-(1,3,5-trimethyl-1H-pyrazol-4-yl)ethoxy]phenyl}-1-methyl-1H-indazol-3-yl)methyl]dimethylamine

Smiles: CN(C)CC1=NN(C)C2=CC=C(C=C21)C1=CC=C(F)C(F)=C1OCCC1C(C)=NN(C)C=1C

InChiKey: SOXNKJCQBRQUMS-UHFFFAOYSA-N

InChi: InChI=1S/C25H29F2N5O/c1-15-18(16(2)31(5)28-15)11-12-33-25-19(8-9-21(26)24(25)27)17-7-10-23-20(13-17)22(14-30(3)4)29-32(23)6/h7-10,13H,11-12,14H2,1-6H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (220.49 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. IMP-1088 (50 nM) significantly less enriches multiple N-myristoylated proteins in enriched samples. 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. 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. 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.

Products are for research use only. Not for human use.