IMP-1088 is a novel dual inhibitor of human N-myristoyltransferase NMT1 and NMT2 with IC50 of <1 nM for HsNMT1 and HsNMT2. IMP-1088 has a Kd of less than 210 pM for HsNMT1. The rhinovirus's N-myristoylated protein (VP0) is blocked by IMP-1088, which effectively prevents rhinovirus replication. Due to its cytotoxic properties, IMP-1088 shields host cells against virus infection.

Physicochemical Properties

Molecular Formula	C25H29F2N5O
Molecular Weight	453.53
Exact Mass	453.234
Elemental Analysis	C, 66.21; H, 6.45; F, 8.38; N, 15.44; O, 3.53
CAS #	2059148-82-0
PubChem CID	132274735
Appearance	Colorless to light yellow solid powder
Density	1.2±0.1 g/cm3
Boiling Point	566.9±50.0 °C at 760 mmHg
Flash Point	296.6±30.1 °C
Vapour Pressure	0.0±1.6 mmHg at 25°C
Index of Refraction	1.595
LogP	3.73
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	7
Heavy Atom Count	33
Complexity	642
Defined Atom Stereocenter Count	0
InChi Key	SOXNKJCQBRQUMS-UHFFFAOYSA-N
InChi Code	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
Chemical Name	1-[5-[3,4-difluoro-2-[2-(1,3,5-trimethylpyrazol-4-yl)ethoxy]phenyl]-1-methylindazol-3-yl]-N,N-dimethylmethanamine
Synonyms	IMP1088; IMP 1088; IMP-1088
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	HsNMT1 ( IC50 < 1 nM ); HsNMT2 ( IC50 < 1 nM ); HsNMT1 ( Kd < 210 pM )
ln Vitro	IMP-1088 (1-1000 nM) has an IC50 of 17 nM and inhibits the virus-induced cytopathic effect (CPE) in a dose-dependent manner. With an IC50 of 5.8 nM, IMP-1088 (125 nM) completely inhibits novel infectious viruses. In primary human bronchial epithelial cells (hBEC) infected with rhinovirus RV-A1 (MOI 5), IMP-1088 (1-1000 nM) suppresses single cycle replication and stops the formation of infectious virus for a duration of 7 hours. Even when added up to three hours after infection, IMP-1088 dramatically reduces the generation of infectious viruses[1]. In enriched samples, IMP-1088 (50 nM) considerably reduces the enrichment of several N-myristoylated proteins[1]. By preventing virus assembly in HeLa cells infected with rhinovirus RV-A16 (MOI 20) for six hours, IMP-1088 (500 nM) reduces the generation of infectious rhinovirus particles[1]. NMT activity fully recovers in 24 hours and IMP-1088 (0.24 nM-1 µM; for 24 hours + 24 hours washout) has no long-term effect on cell viability[1]. IMP-1088 effectively inhibits co-translational myristoylation of a virus-specific encoded protein (VP0), hence blocking a crucial stage in viral capsid construction. IMP-1088 does not impede the translation of rhinovirus polyprotein or the synthesis of viral RNA[1].
References	[1]. 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.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~220.5 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.2049 mL	11.0246 mL	22.0493 mL
	5 mM	0.4410 mL	2.2049 mL	4.4099 mL
	10 mM	0.2205 mL	1.1025 mL	2.2049 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.