NFAT-133
NFAT-133 is an aromatic polyketide with immunosuppressive and antidiabetic activity. NFAT-133 activates the AMPK pathway, promoting glucose uptake in L6 muscle fibers, thereby resisting diabetes. NFAT-133 inhibits the transcriptional activity of activated T-cell nuclear factor (NFAT), thereby suppressing the expression of IL-2 and the proliferation of T cells, demonstrating an immunosuppressive effect. NFAT-133 does not exhibit antibacterial activity or cytotoxicity, but it can weaken the production of NO in RAW264.7 cells induced by Lipopolysaccharide (LPS) (HY-D1056).
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- CAS No.: 165133-85-7
- Formule: C17H24O3
- Masse moléculaire:276.37
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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AMPK |
IL-2 |
NFAT-133 (0.01-100 μM, 0.5-24 h) stimulates glucose uptake in a dose- and time-dependent manner, with an EC₅₀ value of 1.5 μM in rat L6 myotubes and has low cytotoxicity[2].
NFAT-133 (3 μM, 16 h) activates the AMPK-ACC signaling axis and ultimately promotes the translocation of GLUT4 to the cell membrane by phosphorylating AS160 in rat L6 myotubes (its mechanism of action is independent of the insulin signaling pathway (PI3K/Akt))[2].
NFAT-133 (0-50 μM) is inactive against Staphylococcus aureus ATCC 12600, Bacillus subtilis ATCC 6051, Escherichia coli ATCC 11775, and Pseudomonas aeruginosa ATCC 9721 and does not show any cytotoxicity towards RAW264.7, HeLa, NCI-H460 and MCF-7 cells[3].
NFAT-133 (25 h) weakly reduced the production of LPS-induced nitric oxide (NO) in RAW264.7 cells in a dose-dependent manner[3].
NFAT-133 (100 μM) fails to activate PPARγin rat L6 myotubes, thereby avoiding side effects such as weight gain, liver toxicity and cardiovascular risks[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Rat L6 myotubes
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Concentration:3 μM
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Incubation Time:16 h
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Result:Stimulated AMPK activation but Akt.
Mediated AMPK activation did not affect CAMKKβ and LKB1.
Promoted AS160 phosphorylation and GLUT4 translocation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Diabetes model established in l male db/db mice (7-9 weeks of age)[1]
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Dosage:100 mg/kg
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Administration:Intraperitoneal injection (i.p.), twice daily for 10 days
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Result:Significantly reduced blood sugar and insulin levels without increasing the weight of the liver or the body weight of the mice.
Chemical Information
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CAS No. 165133-85-7
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Masse moléculaire 276.37
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Formule C17H24O3
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SMILES
CC([C@@H](C)[C@H](O)[C@H](C1=C(C=C(C=C1)C)/C=C/CO)C)=O
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Structure Classification
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Initial Source
Dactylosporangium
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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]. Yang Y, et al. Absolute configuration of NFAT-133, an aromatic polyketide with immunosuppressive and antidiabetic activity from actinomycetes. J Antibiot (Tokyo). 2016 Jan;69(1):69-71. [Content Brief]
[2]. Thakkar CS, et al. NFAT-133 increases glucose uptake in L6 myotubes by activating AMPK pathway. Eur J Pharmacol. 2015 Dec 15;769:117-26. [Content Brief]
[3]. Zhou W, et al. Identification and Biological Activity of NFAT-133 Congeners from Streptomyces pactum. J Nat Prod. 2021 Sep 24;84(9):2411-2419. [Content Brief]
[4]. Kulkarni-Almeida AA, et al. Fermentation, Isolation, Structure, and antidiabetic activity of NFAT-133 produced by Streptomyces strain PM0324667. AMB Express. 2011 Nov 21;1(1):42. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NFAT-133 Related Classifications
HY-N16431 Related Classifications
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