Girolline  (Synonyms: RP 49532)

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^[1][2][3][4].

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.

Girolline exhibits low toxicity in dogs and mice in preclinical toxicological studies^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

190.63

C₆H₁₁ClN₄O

110883-46-0

NC[C@H](Cl)[C@H](C1=CN=C(N)N1)O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]