1. Epigenetics PI3K/Akt/mTOR Immunology/Inflammation Metabolic Enzyme/Protease
  2. AMPK Nuclear Factor of activated T Cells (NFAT) Interleukin Related Endogenous Metabolite
  3. 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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NFAT-133

NFAT-133 Chemical Structure

CAS No. : 165133-85-7

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Description

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)[1][2][3][4].

IC50 & Target[1][2]

AMPK

 

IL-2

 

In Vitro

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.

Western Blot Analysis[2]

Cell Line: Rat L6 myotubes
Concentration: 3 μM
Incubation Time: 16 h
Result: Stimulated AMPK activation but Akt.
Mediated AMPK activation did not affect CAMKKβ and LKB1.
Promoted AS160 phosphorylation and GLUT4 translocation.
Parmacokinetics[4]
Species Dose Route Indicator value
Mice 30 mg/kg i.p. Tmax 0.08 h
Mice 30 mg/kg p.o. Tmax 0.08 h
Mice 30 mg/kg i.p. Cmax 11.653 μg/mL
Mice 30 mg/kg p.o. Cmax 3.41 μg/mL
Mice 30 mg/kg i.p. Cmax 42.221 μM
Mice 30 mg/kg p.o. Cmax 12.34 μM
Mice 30 mg/kg i.p. AUClast 3.217
Mice 30 mg/kg p.o. AUClast 0.63
Mice 30 mg/kg i.p. AUC0-inf 3.553
Mice 30 mg/kg p.o. AUC0-inf 0.65
Mice 30 mg/kg i.p. T1/2 1.86 h
Mice 30 mg/kg p.o. T1/2 0.16 h
In Vivo

NFAT-133 (100 mg/kg, i.p., twice daily for 10 days) significantly reduces the blood sugar and insulin levels in diabetic mice[4].

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

Animal Model: Diabetes model established in l male db/db mice (7-9 weeks of age)[1]
Dosage: 100 mg/kg
Administration: Intraperitoneal injection (i.p.), twice daily for 10 days
Result: Significantly reduced blood sugar and insulin levels without increasing the weight of the liver or the body weight of the mice.
Molecular Weight

276.37

Formula

C17H24O3

CAS No.
SMILES

CC([C@@H](C)[C@H](O)[C@H](C1=C(C=C(C=C1)C)/C=C/CO)C)=O

Structure Classification
Initial Source

Dactylosporangium

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
NFAT-133
Cat. No.:
HY-N16431
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