GSK621

製品コードS7898 バッチS789801

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₆H₂₀ClN₃O₅

分子量

489.91

CAS No.

1346607-05-3

Solubility (25°C)*

体外

DMSO

97 mg/mL (197.99 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	GSK621 is a specific and potent AMPK activator.
in vitro	In AML cell lines and primary AML samples, GSK621 markedly increases phosphorylation at AMPKα T172, a marker of AMPK activation. In a set of 20 cell lines, this compound reduces the proliferation of all 20 lines with IC50 ranged from 13-30 μM, and increases apoptosis in 17 (85%) lines. In addition, it also triggers autophagy, which partially contributes to AML cell death. ^[1]
in vivo	In nude mice bearing MOLM-14 xenografts, GSK621 (30 mg/kg, i.p.) reduces leukemia growth and significantly extends survival by enhancing AMPK activity and the induction of apoptosis. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	AMPK enzymatic assay
キナーゼアッセイ	HEPG2 cells are treated with increasing doses of A-769662 or GSK621, and ACC S79 phosphorylation is assessed as a surrogate marker for AMPK activation using a commercially available ELISA kit.
細胞アッセイ	細胞株	MV4-11, OCI-AML3, OCI-AML2, HL-60, Kasumi, HEL, UT7, NB4, TF-1, KG1A, Nomo p28, SKM-1, U937, YHP1, MOLM-14, Mo7e, K562, MOLM-13, EOL-1, SET-2 cell lines
	濃度	~30 μM
	反応時間	~4 d
	実験の流れ	Twenty AML cell lines are treated with log10 dilutions of GSK621 and relative viability is determined by CellTiter-Glo?assay. IC50 of this compound among these 20 cell lines is calculated using the Prism software and are presented as log[C] with [C] in mol/l (M). Results are presented for 5 different cell lines per panel.
動物実験	動物モデル	NUDE Mice bearing MOLM-14 Xenografts
	投薬量	30 mg/kg, twice daily
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/26004183/

カスタマーフィードバック

: Data from [Data independently produced by , , Haematologica, 2018, doi:10.3324/haematol.2018.191403]

: Data from [Data independently produced by , , J Cell Mol Med, 2018, doi:10.1111/jcmm.13975]

: Data from [Data independently produced by , , PLoS One, 2016, 11(8):e0161017.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

(Pro)renin receptor aggravates myocardial pyroptosis in diabetic cardiomyopathy through AMPK-NLRP3 pathway [ Front Pharmacol, 2024, 15:1453647]	PubMed: 39545058
AMPK stimulation inhibits YAP/TAZ signaling to ameliorate hepatic fibrosis [ Sci Rep, 2024, 14(1):5205]	PubMed: 38433278
Redefining the role of AMPK in autophagy and the energy stress response [ Nat Commun, 2023, 14(1):2994]	PubMed: 37225695
AMPK Stimulation Inhibits YAP/TAZ Signaling to Ameliorate Hepatic Fibrosis [ Research Square, 2023, 10.21203/rs.3.rs-3727864/v1]	PubMed: none
AMPK-PERK axis represses oxidative metabolism and enhances apoptotic priming of mitochondria in acute myeloid leukemia [ Cell Rep, 2022, 38(1):110197]	PubMed: 34986346
GPR120 induces regulatory dendritic cells by inhibiting HK2-dependent glycolysis to alleviate fulminant hepatic failure [ Cell Death Dis, 2021, 13(1):1]	PubMed: 34911928
Effects of (Pro)renin Receptor on Diabetic Cardiomyopathy Pathological Processes in Rats via the PRR-AMPK-YAP Pathway [ Front Physiol, 2021, 12:657378]	PubMed: 34122131
GPA peptide inhibits NLRP3 inflammasome activation to ameliorate colitis through AMPK pathway [ Aging (Albany NY), 2020, 12(18):18522-18544]	PubMed: 32950971
Metformin induces lipogenic differentiation in myofibroblasts to reverse lung fibrosis [ Nat Commun, 2019, 10(1-:2987]	PubMed: 31278260
Ubiquinol-cytochrome C reductase core protein II promotes tumorigenesis by facilitating p53 degradation. [ EBioMedicine, 2019, 40:92-105]	PubMed: 30674441

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。