2. Others PI3K/Akt/mTOR Epigenetics
  3. Drug Derivative mTOR AMPK
  4. AMPK/mTOR modulator-1

AMPK/mTOR modulator-1, Ginsenoside derivative, is an orally active mTOR inhibitor and AMPK activator. AMPK/mTOR modulator-1 activates AMPK signaling with a Kd of 4.759 μM. AMPK/mTOR modulator-1 promotes M1-like tumor-associated macrophage polarization while suppressing M2-like polarization. AMPK/mTOR modulator-1 can enhance glycolysis. AMPK/mTOR modulator-1 significantly inhibits tumor progression and shows anti-inflammation activity. AMPK/mTOR modulator-1 can be used for the research of colorectal cancer.

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AMPK/mTOR modulator-1

AMPK/mTOR modulator-1 Chemical Structure

CAS No. : 1190602-80-2

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AMPK/mTOR modulator-1 Related Antibodies

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mTOR mTORC1 mTORC2

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

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Description

AMPK/mTOR modulator-1, Ginsenoside derivative, is an orally active mTOR inhibitor and AMPK activator. AMPK/mTOR modulator-1 activates AMPK signaling with a Kd of 4.759 μM. AMPK/mTOR modulator-1 promotes M1-like tumor-associated macrophage polarization while suppressing M2-like polarization. AMPK/mTOR modulator-1 can enhance glycolysis. AMPK/mTOR modulator-1 significantly inhibits tumor progression and shows anti-inflammation activity. AMPK/mTOR modulator-1 can be used for the research of colorectal cancer[1].

IC50 & Target

AMPK

4.759 μM (Kd)

In Vitro

AMPK/mTOR modulator-1 (Compound AD-1) directly binds to recombinant AMPK protein with a Kd of 4.759 × 10−6 M[1].
AMPK/mTOR modulator-1 (2.5-10 μM; 24 h) promotes M1-like polarization and suppresses M2-like polarization in RAW264.7-derived TAMs in a dose-dependent manner[1].
AMPK/mTOR modulator-1 (2.5-10 μM; 24 h) activates AMPK and inhibits mTOR signaling in RAW264.7-derived TAMs in a dose-dependent manner[1].
AMPK/mTOR modulator-1 (2.5-10 μM; 24 h) enhances glycolytic activity in RAW264.7-derived TAMs in a dose-dependent manner[1].

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

AMPK/mTOR modulator-1 Related Antibodies

RT-PCR[1]

Cell Line: RAW264.7-derived TAMs in TCS of mouse colon cancer cells (CT26)
Concentration: 2.5, 5, and 10 μM
Incubation Time: 24 h
Result: Downregulated M2 -associated markers (Arg-1, IL-10, and TGF-β)
and upregulated M1-associated markers (iNOS, TNF-α, and IL-1β).

Western Blot Analysis[1]

Cell Line: RAW264.7-derived TAMs in TCS of mouse colon cancer cells (CT26)
Concentration: 2.5, 5, and 10 μM
Incubation Time: 24 h
Result: Increased protein levels of iNOS and reduced Arg-1 levels.
Increased P-AMPK AMPK ratio and reduced p-mTOR/mTOR ratio.
Upregulated the expression of key glycolytic en-zymes, including GLUT1, LDHA, PKM2, and HK2.

ELISA Assay[1]

Cell Line: RAW264.7-derived TAMs in TCS of mouse colon cancer cells (CT26)
Concentration: 2.5, 5, and 10 μM
Incubation Time: 24 h
Result: Reduced TGF-β, IL-10 levles and increased IL-1β, TNF-α levels.
In Vivo

AMPK/mTOR modulator-1 (Compound AD-1) (10 mg/kg; i.g.; daily; 64 days) inhibits the development and progression of colitis-associated tumors by promoting M1-like polarization and suppressing M2-like polarization in AOM (HY-111375)/DSS (HY-116282C)-induced CAC mice[1].
AMPK/mTOR modulator-1 (10 mg/kg; oral gavage; daily; 15 days) suppresses tumor growth and reprograms TAM polarization in HT-29 cells xenograft mice[1].

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

Animal Model: CAC mice induced by AOM/DSS (male, BALB/c， 6–8 weeks old, 20–22 g)[1]
Dosage: 10 mg/kg
Administration: oral gavage; daily; 64 days
Result: Restored colon length and reduced tumor number.
Alleviated crypt destruction, epithelial damage, and inflammatory infiltration.
Decreased Ki-67-positive proliferating cells and reduced proportion of F4/80+CD206+ (M2-like) TAMs.
Increased levels of TNF-α and IL-1β and decreased IL-10 levels.
Increased iNOS protein levels and decreased Arg-1 protein levels.
Increased infiltration of F4/80+CD86+ (M1-like) TAMs and decreased F4/80+CD206+ TAMs in colonic tissues.
Animal Model: CRC mice with HT-29 cells xenograft (female, BALB/c nude, 6–8 weeks old, 20–22 g)[1]
Dosage: 10 mg/kg
Administration: oral gavage; daily; 15 days
Result: Reduced tumor volume and weight, inflammatory cell infiltration and improved tissue architecture in tumor sections.
Decreased tumor cell proliferation (lower Ki-67 expression).
Elevated iNOS expression and decreased Arg-1 expression.
Increased abundance of F4/80+CD86+ (M1-like) TAMs; reduced number of F4/80+CD206+ (M2-like) TAMs in tumor tissue.
Molecular Weight

492.77

Formula

C31H56O4
CAS No.
SMILES

CC1(C)[C@@H](O)CC[C@@]2(C)C1CC[C@]3(C)C2C[C@@H](O)C4[C@@]3(C)CCC4[C@](C)(OC)CCCC(C)(C)O
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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AMPK/mTOR modulator-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

AMPK/mTOR modulator-11190602-80-2Drug DerivativemTORAMPKDrug derivativeMammalian target of RapamycinAMP-activated protein kinasetumor immune microenvironmentM1-like polarizationRAW264.7M2-like polarizationglycolysistumor-associated macrophageCRCcolorectal cancerHT-29Inhibitorinhibitorinhibit

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