FR900359 (Synonyms: UBO-QIC) |
| Catalog No.GC49089 |
FR900359 is an inhibitor of G proteins Gαq, Gα11, and Gα14 with IC50 values of 13.18, 10.47, and 10nM, respectively and is isolated from the leaves of the ornamental plant Ardisia crenata
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 107530-18-7
Sample solution is provided at 25 µL, 10mM.
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FR900359 is an inhibitor of G proteins Gαq, Gα11, and Gα14 with IC50 values of 13.18, 10.47, and 10nM, respectively and is isolated from the leaves of the ornamental plant Ardisia crenata[1][2]. FR900359 has shown significant therapeutic potential in various disease models, including cancer, cardiovascular diseases, asthma and pulmonary arterial hypertension[3][4][5].
In vitro, FR900359 (0.01, 0.1, 1.0 and 10µM) incubated melanoma cell B16 for 72h reduced cell growth in a concentration-dependent manner without causing direct cytotoxicity but by arresting cell cycle in the G1 phase[2]. FR900359 (100nM, 300nM, 1μM) treated uveal melanoma cells for 1-4 days inhibited cancer cell growth by inhibiting Gαq and downregulating proteins involved in cell cycle and cell proliferation[3]. FR900359 (50nM) treated human patelets for 5min abolished platelet aggregation and secretion induced by lower concentration of the agonists as well. FR900359 treatment with higher concentrations (100nM) for 5min is required to cause a complete inhibition when used with murine platelets[4].
In vivo, FR900359 applied intratracheally (0.1mg/ml, 50μl) before each application of house dust mite allergen on mouse model of asthma prevented increase in collagen deposition and airway hyperresponsiveness[5]. FR900359 (2.5µg/mouse) or DMSO was applied to the lung via the intra-tracheal (i.t.) route 1h before hemodynamic measurements in mice with chronic hypoxia(Hx)-induced pulmonary hypertension (PH). FR900359 application reduced elevated basal right ventricular systolic pressure and slightly attenuated basal heart rate in Hx-induced PH mouse model[6].
References:
[1]Fujioka, M, Koda S, Morimoto Y. Structure of FR900359, a cyclic depsipeptide from Ardisia crenata sims J. Org. Chem. 1988, 53 (12), 2820−2825.
[2] Schrage R, Schmitz L A, Gaffal E et.al. The experimental power of FR900359 to study Gq-regulated biological processes. Nat Commun. 2015 Dec 14;6:10156
[3] Lapadula D, Farias E, Randolph E C, et al. Effects of Oncogenic Gαq and Gα11 Inhibition by FR900359 in Uveal Melanoma. Mol Cancer Res. 2019 Apr;17(4):963-973.
[4] Inamdar V, Patel A, Bhanu Kanth Manne B K, et al. Characterization of UBO-QIC as a Gαq inhibitor in platelets.Platelets. 2015;26(8):771-8
[5] Matthey M, Roberts R, Seidinger A, et al.Targeted inhibition of Gq signaling induces airway relaxation in mouse models of asthma. Sci Transl Med. 2017 Sep 13;9(407):eaag2288.
[6] Seidinger A, Roberts R, Bai Y, et al. Pharmacological Gq inhibition induces strong pulmonary vasorelaxation and reverses pulmonary hypertension. EMBO Mol Med. 2024 Aug;16(8):1930-1956.
| Cell experiment [1]: | |
Cell lines | Uveal melanoma cells |
Preparation Method | Uveal melanoma cells were plated on poly-L-lysine coated 96-well white bottom plates at 5 × 103 cells per well and allowed to sit overnight at 37°C and 5% CO2 in a humidified incubator. Cells were then treated with DMSO or 100nM, 300nM or 1μM FR900359 for 1–4 days and harvested by removing the media and lysing the cells with 100μl of cell-grade water for 1h at 37°C. |
Reaction Conditions | 100nM, 300nM or 1μM; 1–4days |
Applications | FR900359 treatment of uveal melanoma cells induced cell growth arrest by inhibiting Gαq and decreasing levels of proteins involved in cell cycle and cell proliferation. FR900359 also induced cancer cell apoptosis. |
| Animal experiment [2]: | |
Animal models | Female Balb/c mice |
Preparation Method | Female Balb/c mice at 10 weeks of age sensitized with intratracheal application of 1µg of house dust mite (HDM) (in 50µl of PBS) per mouse was performed on day 0. Then, mice were challenged by intratracheal application of 10µg of HDM (in 50µl of PBS) on days 7 to 11. Control mice received 50µl of PBS intratracheally on the respective days. Mice that received HDM were treated with either control solution or FR900359 (0.1mg/ml, 50µl) 4h before each HDM application on day 0 and days 7 to 11. Analysis was done on days 13 and 14. |
Dosage form | 0.1mg/ml, 50µl; i.t.; day 0 and day 7 to 11 |
Applications | FR900359 applied prevented increase in collagen deposition and airway hyperresponsiveness. |
References: | |
| Cas No. | 107530-18-7 | SDF | |
| Synonyms | UBO-QIC | ||
| Canonical SMILES | CCC(N[C@@H]([C@H](O)C(C)C)C(O[C@@H]([C@@]1([H])C(N([C@@](C(O[C@@H]([C@@H](C(O[C@@H](C(N(C(C(N[C@H](C(N([C@H](C(N1)=O)C)C)=O)C)=O)=C)C)=O)CC2=CC=CC=C2)=O)NC(C)=O)C(C)C)=O)([H])[C@@H](C)OC)C)=O)C(C)C)=O)=O | ||
| Formula | C49H75N7O15 | M.Wt | 1002.2 |
| Solubility | Chloroform: soluble | Storage | -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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.9978 mL | 4.989 mL | 9.978 mL |
| 5 mM | 0.1996 mL | 0.9978 mL | 1.9956 mL |
| 10 mM | 0.0998 mL | 0.4989 mL | 0.9978 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >95.00%
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Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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