PFK-158 |
| Catalog No.GC19293 |
PFK-158은 IC50 값이 137nM인 강력하고 선택적인 PFKFB3 억제제입니다. PFK-158은 포도당 흡수, ATP 생성, 젖산 방출을 감소시키고 암세포에서 세포자멸사와 자가포식을 유도합니다. PFK-158은 광범위한 항종양 활성을 가지고 있습니다. PFK-158은 또한 박테리아에 대한 콜리스틴의 내성을 향상시킬 수 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1462249-75-7
Sample solution is provided at 25 µL, 10mM.
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PFK-158 is a potent and selective PFKFB3 inhibitor, which shows extensive anti-tumor activity by reducing the uptake of glucose in cancer cells, the production of ATP, the release of lactic acid and inducing apoptosis and autophagy[1].
PFK-158 suppressed cell viability in a dose- and time-dependent manner in EC cells. Co-treatment with PFK158 (5 μM) and CBPt led to a significant increase in the percentage of apoptotic cells in HEC-1B and ARK-2. Furthermore, Western blot analysis revealed that the active form of PARP was significantly increased upon co-treatment, compared to single treatment alone, further demonstrating that the combination treatment enhances cell apoptosis[2]
The efficacy of PFK158 alone and in combination with carboplatin (CBPt) was evaluated on primary tumor growth and metastasis in HeyA8MDR‐bearing nude mice i.p. A marked reduction of tumor growth was observed in the combination treatment.PFK-158 with CBPt significantly reduced ascites and reduced LDs in tumor tissue as seen by immunofluorescence and transmission electron microscopy compared to untreated mice[3]
References:
[1]. Gustafsson NMS, Färnegårdh K, et al. Targeting PFKFB3 radiosensitizes cancer cells and suppresses homologous recombination. Nat Commun. 2018 Sep 24;9(1):3872.
[2]. Xiao Y, Jin L, et al. Inhibition of PFKFB3 induces cell death and synergistically enhances chemosensitivity in endometrial cancer. Oncogene. 2021 Feb;40(8):1409-1424.
[3]. Mondal S, Roy D, et al. Therapeutic targeting of PFKFB3 with a novel glycolytic inhibitor PFK158 promotes lipophagy and chemosensitivity in gynecologic cancers. Int J Cancer. 2019 Jan 1;144(1):178-189.
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