1. Metabolic Enzyme/Protease PI3K/Akt/mTOR Epigenetics
  2. Oxidative Phosphorylation Mitochondrial Metabolism AMPK
  3. AMPK activator 11

AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research.

For research use only. We do not sell to patients.

AMPK activator 11

AMPK activator 11 Chemical Structure

CAS No. : 2948304-00-3

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Description

AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research[1].

Cellular Effect
Cell Line Type Value Description References
DLD-1 IC50
<1 μM
Compound: 18a
Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 24 hrs
Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 24 hrs
[PMID: 37253101]
HCT-116 IC50
<1 μM
Compound: 18a
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs
[PMID: 37253101]
L02 IC50
>15 μM
Compound: 18a
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs
[PMID: 37253101]
LX-2 IC50
>15 μM
Compound: 18a
Cytotoxicity against human LX2 cells assessed as reduction in cell viability incubated for 24 hrs
Cytotoxicity against human LX2 cells assessed as reduction in cell viability incubated for 24 hrs
[PMID: 37253101]
NCM460 IC50
>15 μM
Compound: 18a
Cytotoxicity against human NCM460 cells assessed as reduction in cell viability incubated for 24 hrs
Cytotoxicity against human NCM460 cells assessed as reduction in cell viability incubated for 24 hrs
[PMID: 37253101]
RKO IC50
>1 μM
Compound: 18a
Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 24 hrs in presence of FCCP by propidium iodide staining based high-content screening method
Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 24 hrs in presence of FCCP by propidium iodide staining based high-content screening method
[PMID: 37253101]
RKO IC50
>1 μM
Compound: 18a
Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 24 hrs in presence of oligomycin by propidium iodide staining based high-content screening method
Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 24 hrs in presence of oligomycin by propidium iodide staining based high-content screening method
[PMID: 37253101]
RKO IC50
0.07 μM
Compound: 18a
Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 24 hrs by propidium iodide staining based high-content screening method
Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 24 hrs by propidium iodide staining based high-content screening method
[PMID: 37253101]
RKO IC50
0.1 μM
Compound: 18a
Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 24 hrs
Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 24 hrs
[PMID: 37253101]
SW480 IC50
<1 μM
Compound: 18a
Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 24 hrs
Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 24 hrs
[PMID: 37253101]
In Vitro

AMPK activator 11 (Compound 18a) (0-30 μΜ;0-7 days) inhibits the growth and migration of CRC cells with IC50 values below 1 μM[1].
AMPK activator 11 (0-0.1 μΜ;24 hours) dramatically enhances of global oxygen consumption rate (OCR) in RKO cells while the slightly changed extracellular acidification rate (ECAR). AMPK activator 11 upregulates the expression of p-AMPK and mitochondrial complex III and V and has the ability to selectively activate OXPHOS in CRCs[1].

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

Cell Viability Assay[1]

Cell Line: CRC cells
Concentration: 0-30 μM
Incubation Time: 0-7 days
Result: Selectively inhibited the growth and migration of CRC cells.
Inhibited the proliferation of different CRCs with IC50 values below 1 μM.

Western Blot Analysis[1]

Cell Line: RKO cells
Concentration: 0.1 μM
Incubation Time: 24 hours
Result: Upregulated the expression of p-AMPK and mitochondrial complex III and V and has the ability to selectively activate OXPHOS.
In Vivo

AMPK activator 11 (Compound 18a) (2.5 or 10 mg/kg for i.p. for 25 days) selectively suppresses tumor growth without causing toxicity in RKO cells related axenograft mice model[1].

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

Animal Model: RKO cells related axenograft model on male BALB/nude mice[1]
Dosage: 2.5 or 10 mg/kg
Administration: Intraperitoneal injection (i.p.) for 25 days
Result: Resulted in 58.2% tumor growth inhibition, with no significant weight loss observed.
Resulted in 77.1% inhibition of tumor growth but also caused a 36% weight loss.
Immunohistochemistry results also showed activation of AMPK in tumor tissue.
Molecular Weight

408.45

Formula

C25H20N4O2

CAS No.
SMILES

OC1=CC=C(CCNC2=NC(C3=C(C4=CC=CC=C4N3)C=O)=NC5=C2C=CC=C5)C=C1

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Storage

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

Purity & Documentation
References
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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.

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AMPK activator 11
Cat. No.:
HY-154973
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