| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
HsNMT1 ( IC50 < 1 nM ); HsNMT2 ( IC50 < 1 nM ); HsNMT1 ( Kd < 210 pM )
IMP-1088 targets human N-myristoyltransferases NMT1 and NMT2, enzymes that catalyze the attachment of myristic acid to the N-terminus of proteins. This N-myristoylation is essential for the function of many viral proteins, including the rhinovirus capsid protein VP0. By potently inhibiting NMT1 and NMT2 with IC50 <1 nM and Kd <210 pM for HsNMT1, IMP-1088 blocks a key step in viral capsid assembly, preventing the production of infectious virus particles. |
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| 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].
In vitro, IMP-1088 demonstrates potent inhibition of NMT1 and NMT2 with IC50 <1 nM for both enzymes and Kd <210 pM for HsNMT1. At 1-1000 nM, it blocks the production of infectious virus in primary human bronchial epithelial cells infected with rhinovirus RV-A1 and inhibits single-cycle replication within 7 hours. It shows low nanomolar antiviral activity against multiple rhinovirus strains, poliovirus, and foot-and-mouth disease virus. IMP-1088 (500 nM) reduces RV-A16 replication in HeLa cells. |
| ln Vivo |
In vivo data for IMP-1088 is limited in publicly available sources. As a potent NMT inhibitor with broad-spectrum antiviral activity against rhinoviruses and other picornaviruses, the compound has potential applications in animal models of viral respiratory infections. By blocking a key step in viral capsid assembly, IMP-1088 could provide a novel therapeutic approach for treating the common cold and other viral infections. However, specific published in vivo efficacy studies are not widely reported.
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| Enzyme Assay |
The in vitro NMT inhibition assay for IMP-1088 uses recombinant human NMT1 and NMT2 enzymes and a peptide substrate. Enzyme activity is measured using radioactive or fluorescence-based detection methods, and IC50 values and Kd values are calculated from dose-response curves. Antiviral assays are performed in rhinovirus-infected cells, with viral replication measured by quantifying viral RNA, plaque formation, or cytopathic effect.
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| Cell Assay |
Cellular assays for IMP-1088 are conducted in primary human bronchial epithelial cells and HeLa cells infected with rhinovirus. Cells are treated with IMP-1088 at concentrations of 1-1000 nM. Viral replication is measured by quantifying viral RNA, plaque formation, or cytopathic effect. Cell viability is assessed to confirm that antiviral activity is not due to cytotoxicity. The compound's effects on N-myristoylation of viral proteins are confirmed by Western blotting.
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| Animal Protocol |
In vivo studies for IMP-1088 would typically involve animal models of rhinovirus or other picornavirus infections. The compound would be administered via oral or intranasal routes at doses determined by pharmacokinetic studies. Efficacy would be assessed by measuring viral loads in respiratory tissues, clinical signs of infection, and inflammatory responses. However, specific published in vivo protocols for IMP-1088 are not available in the current literature. The compound is currently used as a research tool.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for IMP-1088 is not extensively reported in publicly available sources. The compound has a molecular weight of 453.53 g/mol and a molecular formula of C25H29F2N5O. It is soluble in DMSO at 91 mg/mL and in ethanol at 30 mg/mL, but insoluble in water. As a small molecule NMT inhibitor, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life are not available in the current literature.
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| Toxicity/Toxicokinetics |
Toxicity data for IMP-1088 is limited in publicly available sources. As with all research compounds, IMP-1088 is intended for research use only and not for human therapeutic applications. The compound's potent inhibition of host NMTs suggests potential toxicity concerns that would need to be addressed. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References | |
| Additional Infomation |
IMP-1088 is a potent dual inhibitor of human NMT1 and NMT2 with IC50 <1 nM for both enzymes and Kd <210 pM for HsNMT1. It effectively inhibits the production of infectious rhinovirus virions by blocking N-myristoylation of the VP0 protein. IMP-1088 shows low nanomolar antiviral activity against multiple rhinovirus strains, poliovirus, and foot-and-mouth disease virus. It has a molecular formula of C25H29F2N5O and a molecular weight of 453.53 g/mol. IMP-1088 is a valuable research tool for studying N-myristoylation and developing antiviral therapies.
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| Molecular Formula |
C25H29F2N5O
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|---|---|
| Molecular Weight |
453.53
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| Exact Mass |
453.234
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| Elemental Analysis |
C, 66.21; H, 6.45; F, 8.38; N, 15.44; O, 3.53
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| CAS # |
2059148-82-0
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| PubChem CID |
132274735
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| Appearance |
Colorless to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
566.9±50.0 °C at 760 mmHg
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| Flash Point |
296.6±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.595
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| LogP |
3.73
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
642
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SOXNKJCQBRQUMS-UHFFFAOYSA-N
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| 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
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| Chemical Name |
1-[5-[3,4-difluoro-2-[2-(1,3,5-trimethylpyrazol-4-yl)ethoxy]phenyl]-1-methylindazol-3-yl]-N,N-dimethylmethanamine
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| Synonyms |
IMP1088; IMP 1088; IMP-1088
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~220.5 mM)
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| 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. View More
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. |
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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