IMP-1088 |
Catalog No.GC40101
One-Click Copy Product Info
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IMP-1088은 인체 N-myristoyltransferases NMT1(IC50 값 0.24nM)와 NMT2(IC50 값 < 1nM)의 피코몰 이중 억제제이다.
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Cas No.: 2059148-82-0
Sample solution is provided at 25 µL, 10mM.
IMP-1088은 인체 N-myristoyltransferases NMT1(IC50 값 0.24nM)와 NMT2(IC50 값 < 1nM)의 피코몰 이중 억제제이다. IMP-1088은 유선류 아레나바이러스, 호흡기 비루스, 말라리아 기생충을 표적으로 하는 광범위한 항바이러스 잠재력이 있다 [2][3].
체외 실험에서 유방암 MDA-MB-231 세포와 자궁경부암 HeLa 세포에 대해 24, 48 또는 72시간 동안 1mM에서 0.1pM까지의 IMP-1088 노출은 48시간과 72시간 후에만 MDA-MB-231과 HeLa 세포의 증식에 영향을 미치고 농도 의존적으로 달라진다. 1μM의 IMP-1088에 18시간 동안 노출되면 식별된 대부분의 NMT 기질 단백질의 N-미리스토일화가 현저하게 억제되었지만 단백질 합성은 줄어들지 않았고 세포 주기는 변화하지 않았다 [4]. 1μM의 IMP-1088로 처리된 HEK293T 세포는 24시간 동안 림프구성 뇌막염 바이러스 폴리머라제 단백질과 핵 단백질을 발현하는 플라스미드로 전염되었고 Z 단백질의 미리스토일화를 표적으로 하여 바이러스의 조립과 발아를 방해하지만 Z 매개의 바이러스 리보핵 단백질(vRNP) 활성의 억제에는 영향을 미치지 않는다 [5]. 0.001-100μM의 IMP-1088로 처리된 HeLa 세포는 24시간 동안 Vaccinia 바이러스(VACV)에 감염되었고 약 100nM에서 바이러스 수율과 바이러스 전파가 50% 이상 감소되었고 최대 10μM의 IMP-1088 존재하에서 세포 독성은 관찰되지 않았다 [6].
References:
[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. 2018 Jun;10(6):599-606.
[2] Agoni C, Salifu E Y, Enslin G, Kwofie S K, Soliman M E. Dual-Inhibition of Human N-Myristoyltransferase Subtypes Halts Common Cold Pathogenesis: Atomistic Perspectives from the Case of IMP-1088. Chem Biodivers. 2022 Feb;19(2):e2021007.
[3] Mendez A, Bolling C, Taylor S, et al. Structure of Plasmodium vivax N-myristoyltransferase with inhibitor IMP-1088: exploring an NMT inhibitor for antimalarial therapy. Acta Crystallogr F Struct Biol Commun. 2025 Jan 1;81(Pt 1):1-10.
[4] Kallemeijn W W, Lueg G A, Faronato M, et al. Validation and Invalidation of Chemical Probes for the Human N-myristoyltransferases. Cell Chem Biol. 2019 Jun 20;26(6):892-900.e4.
[5] Witwit H, de la Torre J C. Mammarenavirus Z Protein Myristoylation and Oligomerization Are Not Required for Its Dose-Dependent Inhibitory Effect on vRNP Activity. Biochem (Basel). 2025 Jun;5(2):10.
[6] Priyamvada L, Kallemeijn W W, Faronato M, et al. Inhibition of vaccinia virus L1 N-myristoylation by the host N-myristoyltransferase inhibitor IMP-1088 generates non-infectious virions defective in cell entry. PLoS Pathog. 2022 Oct 10;18(10):e1010662.
| 세포 실험 [1]: | |
세포 라인 | 유방암 MDA-MB-231세포와 자궁경부암 HeLa 세포 |
제조 방법 | MDA-MB-231 세포와 자궁경부암 HeLa 세포는 1μM의 IMP-1088에 18시간 동안 노출되었습니다. |
반응 조건 | 1μM; 18시간 동안 |
응용 분야 | 1μM의 IMP-1088에 18시간 동안 노출되면 식별된 대부분의 NMT 기질 단백질의 N-myristoylation가 현저하게 억제되었지만 단백질 합성은 줄어들지 않았고 세포 주기는 변화하지 않았습니다. |
References: | |
| Cas No. | 2059148-82-0 | SDF | |
| Chemical Name | 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 | ||
| Formula | C25H29F2N5O | M.Wt | 453.5 |
| Solubility | A solution in methyl acetate | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2051 mL | 11.0254 mL | 22.0507 mL |
| 5 mM | 441 μL | 2.2051 mL | 4.4101 mL |
| 10 mM | 220.5 μL | 1.1025 mL | 2.2051 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >95.00% Appearance: A solution in methyl acetate
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)