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Cat. No.: HY-154973

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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.

CAS No.: 2948304-00-3
Formula: C₂₅H₂₀N₄O₂
Molecular Weight:408.45

Storage:

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

Data Sheet (275 KB)

AMPK activator 11 Chemical Structure

CAS No.: 2948304-00-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All AMPK Isoforms :

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.

Chemical Information

CAS No. 2948304-00-3
Molecular Weight 408.45
Formula C₂₅H₂₀N₄O₂
SMILES

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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Xu YH,et.al. Design and Synthesis of Bouchardatine Derivatives as a Novel AMP-Activated Protein Kinase Activator for the Treatment of Colorectal Cancer. J Med Chem. 2023 Jun 8;66(11):7387-7404. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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