IMP-1088 是一种有效的人 N-肉豆蔻酰转移酶 NMT1 和 NMT2 双重抑制剂，对 HsNMT1 和 HsNMT2 的 IC50<1 nM。
| Cas No. | 2059148-82-0 |
| 化学名 | 5-[3,4-difluoro-2-[2-(1,3,5-trimethyl-1H-pyrazol-4-yl)ethoxy]phenyl]-N,N,1-trimethyl-1H-indazole-3-methanamine |
| Canonical SMILES | FC1=C(F)C=CC(C2=CC=C(N(C)N=C3CN(C)C)C3=C2)=C1OCCC4=C(C)N(C)N=C4C |
| 分子式 | C25H29F2N5O |
| 分子量 | 453.5 |
| 溶解度 | A solution in methyl acetate |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | IMP-1088 is an inhibitor of N-myristoyltransferase 1 (NMT1) and NMT2 (IC50 = <1 nM for both human enzymes).[1] It inhibits replication of rhinovirus (RV), the virus most commonly responsible for the common cold, by inhibiting myristoylation of the RV capsid protein VP0 from strain RV-A16 in HeLa cells. IMP-1088 (500 nM) reduces RV-A16, RV-A1, RV-B14, and RV-A28 viral titers in HeLa cells without affecting cell growth (IC50 = >1,000 nM). It also blocks production of infectious RV-16 virus in primary human bronchial epithelial cells (hBECs) when added 3 hours post infection via inhibition of viral capsid assembly.
Reference:
1. Mousnier, A., Bell, A.S., Swieboda, D.P., et al. Fragment-derived inhibitors of human N-myristoyltransferase block capsid assembly and replication of the common cold virus. Nat. Chem. 10(6), 599-606 (2018). |
