FR900359
Based on 4 publication(s) in Google Scholar
FR900359 is a depsipeptide selective inhibitor of Gαq/11/14 in mammalia, can inhibits ERK pathway. FR900359 suppresses the proliferation of melanoma cells and decreases of blood pressure. FR900359 also protected against airway hyperreactivity in murine models of allergen sensitization in Ovalbumin, low endotoxin (HY-W250978A)-induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research.
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- 純度: 99.90%
- CAS 番号: 107530-18-7
- 分子式: C49H75N7O15
- 分子量:1002.16
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 FR900359
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生物活性
FR900359 (1.0 μM, 1 hours) inhibits Gαq, Gα11 and Gα /14, but not Gα16 or any other mammalian Gα isoform in HEK293 cells[1].
FR900359 (0-10 μM, 24 hours) effectively reduces growth of B16 cells and suppressed cell proliferation and inhibits migration in a concentration-dependent manner[1].
FR900359 (10 nM, 72 hours) induces G1 cell cycle arrest in melanoma cells with Gq tone and forces melanoma cells (B16 cells) into differentiation [1].
FR900359 (1.0 μM, 5 min) interdicts the activation of extracellular signal-regulated kinases 1 and 2 (ERK1/2) that be largely Gq-mediated28[1].
FR900359 (1 μM, 24 hours) significantly induces more 92.1 cells undergoing apoptosis compared to untreated [3].
FR900359 (30 nM, 60 min) induces dose-dependent relaxation of murine, porcine, and human airways ex vivo[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:B16 cells
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Concentration:0-10 μM
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Incubation Time:24 hours
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Result:Effectively reduced growth of B16 cells in a concentration-dependent manner and suppressed cell proliferation and migration.
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Cell Line:B16 cells
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Concentration:10 nM
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Incubation Time:72 hours
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Result:Induced G1 cell cycle arrest in melanoma cells with Gq tone.
Treated cells appeared flattened, rather dark, and packed with melanin vesicles, attributes consistent with the adoption of a more differentiated state.
Made melanocyte differentiation marker gp100 was upregulated considerably on FR treatment.
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Cell Line:HEK293 cells
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Concentration:1.0 μM
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Incubation Time:5 min
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Result:FR interdicts Gq-dependent ERK1/2 activation
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Cell Line:92.1 cells
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Concentration:1.0 μM
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Incubation Time:24 hours
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Result:Significantly induced more 92.1 cells undergoing apoptosis compared to untreated cells
FR900359 (0.1 mg/ml, 2.5 mg/mouse, intratracheally) abolishes airway hyperreactivity after Ovalbumin (HY-W250978)-induced sensitization in mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Isometric force measurements in mouse tail artery [1]
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Dosage:1.0 μM
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Administration:Washed
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Result:Strongly reduced vascular tone
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Animal Model:Ovalbumins–induced sensitization model of asthma. [4]
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Dosage:0.1 mg/ml, 2.5 mg per mouse
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Administration:Intratracheally
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Result:Abolished airway hyperreactivity after ovalbumin-induced sensitization in mice
化学情報
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CAS 番号 107530-18-7
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性状 Solid
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分子量 1002.16
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分子式 C49H75N7O15
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Color White to yellow
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SMILES
CC(C)[C@@H](O)[C@H](NC(CC)=O)C(O[C@@H]([C@H](NC([C@H](C)N(C)C([C@H](C)NC(C(N(C)C([C@@H](CC1=CC=CC=C1)O2)=O)=C)=O)=O)=O)C(N(C)[C@@H]([C@H](OC)C)C(O[C@H](C(C)C)[C@H](NC(C)=O)C2=O)=O)=O)C(C)C)=O
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Structure Classification
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Initial Source
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Cancer Discov
Myofibroblasts Induce Neuroplasticity to Promote Pancreatic Inflammation and Cancer Progression. [Abstract]2026 Feb 9. PMID: 41661076
FR900359 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2026 Feb 9. [Abstract]
Western blot of phospho-ERK in GqC-PSCs treated with the α1-agonist PE or 1 µM of DCZ in the presence or absence of the selective Gαq inhibitor FR900359 (1 μM).
FR900359 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2026 Feb 9. [Abstract]
FR900359 (1 μM) led to a complete abrogation of the NE-induced [Ca2+]i signal, confirming that this calcium response is Gαq-dependent.
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Cell Host Microbe
Immunometabolic reprogramming of macrophages by gut microbiota-derived cadaverine controls colon inflammation. [Abstract]2025 Sep 30:S1931-3128(25)00375-0. PMID: 41033313 -
Neuron
2025 Nov 26:S0896-6273(25)00842-6. PMID: 41308645
FR900359 purchased from MedChemExpress. Usage Cited in: Neuron. 2025 Nov 26:S0896-6273(25)00842-6. [Abstract]
WT mice were injected with AAV2/9-E-SARE-ERT2-CreERT2-PEST and AAV2/9-CAG-FLEX-H3R-EGFP in the PVT. PVTHFD neurons were labeled with tamoxifen injection-paired HFD supply and EGFP-positive neurons were patched during electrophysiological assays. Representative firing curves of PVTHFD neurons after 100-pA depolarizing current injection (left), and the firing frequency with 0–100-pA depolarizing current injection (right) before and at 20 min FR900359 (10 μM, n = 10 cells) perfusion. The phosphorylation levels of the downstream proteins were determined by western blotting and shown in the lower right corner.
FR900359 purchased from MedChemExpress. Usage Cited in: Neuron. 2025 Nov 26:S0896-6273(25)00842-6. [Abstract]
HDC-CreERT2 mice were injected with AAV2/9-CAG-FLEX-mCherry (AAV-FLEX-mCherry) or AAV2/9-CAG-FLEX-oChIEF-mCherry (AAV-FLEX-oChIEFmCherry) in the TMN. An optical fiber and a cannula were implanted in the PVT. Mice were exposed to blue (λ = 473 nm) or yellow (λ = 598 nm) light as indicated. Mice underwent HFD normal feeding test. Rhosin (10 μM), FR900359 (10 μM), or Barbadin (30 μM) diluted in saline was injected via the cannula before the test. n = 6 male mice in oChIEF + yellow light + saline group; 5 male mice in mCherry + blue light + saline group; 9 male mice in oChIEF + blue light+ saline group; 8 male mice in oChIEF + blue light + Rhosin group; 7 male mice in oChIEF + blue light + FR900359 group; 6 male mice in oChIEF + blue light + Barbadin group. blue light + FR900359 (1 μM).
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Biochem Pharmacol
Bosentan confers cardioprotection against cisplatin toxicity: Involvement of β-arrestin-linked ETA receptor signaling. [Abstract]2026 Aug;250(Pt 2):118027. PMID: 42069228
純度とドキュメンテーション
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データシート (286 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Schrage R, et.al. The experimental power of FR900359 to study Gq-regulated biological processes. Nat Commun. 2015 Dec 14;6:10156. [Content Brief]
[3]. Lapadula D, et.al. Effects of Oncogenic Gαq and Gα11 Inhibition by FR900359 in Uveal Melanoma. Mol Cancer Res. 2019 Apr;17(4):963-973. [Content Brief]
[4]. Matthey M, et.al. Targeted inhibition of Gq signaling induces airway relaxation in mouse models of asthma. Sci Transl Med. 2017 Sep 13;9(407):eaag2288. [Content Brief]
Calculators
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FR900359 関連分類
HY-117037 関連分類
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