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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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CAS 番号: 2948304-00-3
分子式: C₂₅H₂₀N₄O₂
分子量:408.45

保管条件:

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

Data Sheet (275 KB)

AMPK activator 11 構造式

CAS 番号: 2948304-00-3

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生物活性
- 製品説明
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

AMPK アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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.

体内実験

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.

化学情報

CAS 番号 2948304-00-3
分子量 408.45
分子式 C₂₅H₂₀N₄O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (275 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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.

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100 mg

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生物活性
- 製品説明
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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AMPK activator 11

AMPK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

AMPK activator 11 関連分類

HY-154973 関連分類