Girolline
Girolline (RP 49532) is a protein synthesis inhibitor and a functional modulator of eIF5A. Girolline induces ribosome stalling by interfering with the binding of eIF5A to ribosomes. Girolline also inhibits the production of IL-6 and IL-8, and induces cell cycle arrest in tumor cells. Girolline is applicable to research related to inflammatory diseases, solid tumors, leukemia and malaria.
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- CAS No.: 110883-46-0
- Formule: C6H11ClN4O
- Masse moléculaire:190.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
IL-6 |
IL-8 |
In Vitro
Girolline (0.08-40000 ng/mL; 4.5 h) inhibits flagellin-induced TLR5 NF-κB luciferase reporter gene activity in CHO-K1-TLR5 cells[1].
Girolline (2 μg/mL; 7 h) potently inhibits flagellin-induced IL-8 secretion and NF-κB/AP-1 activity in THP1-derived macrophages[1].
Girolline (2 μg/mL; 7 h) blocks flagellin-induced secretion of IL-6 and IL-8 in human peripheral blood mononuclear cells (PBMCs)[1].
Girolline (8-5000 ng/mL; 7 h) dose-dependently inhibits NF-κB/AP-1 activity induced by various TLRs, IL-1β and TNF-α in HEK293 reporter cells, with significant inhibition observed at concentrations ≥200 ng/mL[1].
Girolline (50 μM; 24 h) induces G2/M cell cycle arrest in FL, HeLa and A549 tumor cell lines, with the most pronounced effect observed in FL cells[2].
Girolline (5-50 μM; 24 h) induces concentration-dependent accumulation of polyubiquitinated p53 in FL cells[2].
Girolline (0.1-1.0 μM; 1-4 days) induces dose- and time-dependent G2 phase arrest in human 293 cells, with the most prominent accumulation of G2/M phase cells observed at 1.0 μM for 48 h, while prolonged treatment leads to increased apoptotic cell death[3].
Girolline (10-300 μM; 1 h) dose-dependently inhibits the interaction between hypusinated eIF5A and ribosomes in HEK293T cells[4].
Girolline (1-5 μM; 16 h) selectively inhibits the translation of sequences containing AAA-encoded Lys (but not AAG-encoded Lys) in HEK293T cells, with longer AAA sequences correlating with stronger inhibitory effects[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:FL, HeLa, A549
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Concentration:50 μM
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Incubation Time:24 h
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Result:Induced G2/M cell cycle arrest in FL cells.
Induced G2/M cell cycle arrest to a lesser extent in HeLa and A549 cells.
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Cell Line:human 293 cells
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Concentration:0.1 μM, 0.5 μM, 1.0 μM; 1 μM
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Incubation Time:1 day, 2 days, 3 days, 4 days
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Result:Increased the percentage of cells in G2/M phase from 7.8% to 32.1% and decreased G0/G1 phase cells from 49.5% to 24.5% at 1.0 μM for 48 h, with S phase percentage unchanged.
Resulted in 27.1% of cells in G2/M phase at 1 μM for 2 days; this percentage decreased to 18.1% and 13.1% after 3 and 4 days, respectively.
Increased the pre-G0/G1 apoptotic cell population from 1.9% at day 1 to 18.1% at day 4 with 1 μM treatment.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 110883-46-0
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Masse moléculaire 190.63
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Formule C6H11ClN4O
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SMILES
NC[C@H](Cl)[C@H](C1=CN=C(N)N1)O
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Synonyms
RP 49532
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Structure Classification
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Initial Source
Cymbastela cantharella (Pseudaxinyssa cantharella)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Fung SY, et al. Unbiased screening of marine sponge extracts for anti-inflammatory agents combined with chemical genomics identifies girolline as an inhibitor of protein synthesis. ACS Chem Biol. 2014;9(1):247-257. [Content Brief]
[2]. Tsukamoto S, et al. Girolline, an antitumor compound isolated from a sponge, induces G2/M cell cycle arrest and accumulation of polyubiquitinated p53. Biol Pharm Bull. 2004;27(5):699-701. [Content Brief]
[3]. Diop D, et al. Girolline interferes with cell-cycle progression, but not with translation. C R Biol. 2007;330(12):855-860. [Content Brief]
[4]. Schneider-Poetsch T, et al. Girolline is a sequence context-selective modulator of eIF5A activity. Nat Commun. 2025;16(1):223. Published 2025 Jan 10. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Girolline Related Classifications
HY-106801 Related Classifications
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