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  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 Chemical Structure

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].

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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    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
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HY-154973
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