GSK621

製品コードS7898 バッチS789801

印刷

化学情報

Chemical Structure 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
* <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, GSK621 reduces the proliferation of all 20 lines with IC50 ranged from 13-30 μM, and increases apoptosis in 17 (85%) lines. In addition, GSK621 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
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 GSK621 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.

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：

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
Neuronal AMP-activated protein kinase hyper-activation induces synaptic loss by an autophagy-mediated process [ Cell Death Dis, 2019, 10(3):221] PubMed: 30833547
The Transcription Factors TFEB and TFE3 Link the FLCN-AMPK Signaling Axis to Innate Immune Response and Pathogen Resistance. [ Cell Rep, 2019, 26(13):3613-3628] PubMed: 30917316

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。

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