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PFK-015, also known as PFK15, is a potent inhibitor of the metabolic enzyme 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3). This enzyme is constitutively expressed by neoplastic cells and is essential for the high glycolytic rate (Warburg Effect) observed in these cells. PFK-015 effectively inhibits PFKFB3 (IC50 = 207 nM) without affecting 96 other kinases. It has demonstrated the ability to inhibit glucose and F26BP uptake, induce apoptosis, and reduce tumor growth both in vitro and in vivo. PFK-015 has shown promise in inhibiting tumor growth across various cancer models.

4382-63-2

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4382-63-2 Usage

Uses

Used in Anticancer Applications:
PFK-015 is used as an anticancer agent for targeting the high glycolytic rate in neoplastic cells. By inhibiting PFKFB3, it disrupts the Warburg Effect, which is a metabolic hallmark of cancer cells. This inhibition leads to reduced glucose and F26BP uptake, inducing apoptosis and subsequently reducing tumor growth in various cancer models.
Used in Drug Development:
PFK-015 is used as a lead compound in the development of novel cancer therapeutics. Its high specificity for PFKFB3 and minimal off-target effects on other kinases make it an attractive candidate for further research and potential clinical applications.
Used in Cancer Research:
PFK-015 is used as a research tool to study the role of PFKFB3 in cancer metabolism and the Warburg Effect. It can help researchers understand the underlying mechanisms of cancer cell metabolism and identify potential targets for therapeutic intervention.
Used in Drug Delivery Systems:
PFK-015 can be used in the development of drug delivery systems to improve its bioavailability, delivery, and therapeutic outcomes. By employing various organic and metallic nanoparticles as carriers, the efficacy of PFK-015 against cancer cells can be enhanced, potentially leading to more effective cancer treatments.

References

1) Clem?et al.?(2013),?Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer; Mol. Cancer Ther.?12?1461 2) Zhu?et al. (2016),?PFK15,a Small Molecule Inhibitor of PFKFB3, Induces Cell Cycle Arrest, Apoptosis and Inhibits Invasion in Gastric Cancer; PLoS One?11?e0163768 3) Li?et al. (2017),?Blockage of glycolysis by targeting PFKFB3 suppresses tumor growth and metastasis in head and neck squamous cell carcinoma; J. Exp. Clin. Cancer Res.?36?7

Check Digit Verification of cas no

The CAS Registry Mumber 4382-63-2 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 4,3,8 and 2 respectively; the second part has 2 digits, 6 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 4382-63:
(6*4)+(5*3)+(4*8)+(3*2)+(2*6)+(1*3)=92
92 % 10 = 2
So 4382-63-2 is a valid CAS Registry Number.

4382-63-2 Well-known Company Product Price

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  • Sigma

  • (SML1009)  PFK15  ≥98% (HPLC)

  • 4382-63-2

  • SML1009-5MG

  • 983.97CNY

  • Detail
  • Sigma

  • (SML1009)  PFK15  ≥98% (HPLC)

  • 4382-63-2

  • SML1009-25MG

  • 3,970.98CNY

  • Detail

4382-63-2SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 17, 2017

Revision Date: Aug 17, 2017

1.Identification

1.1 GHS Product identifier

Product name PFK15

1.2 Other means of identification

Product number -
Other names 1-(4-Pyridinyl)-3-(2-quinolinyl)-2-propen-1-one

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:4382-63-2 SDS

4382-63-2Downstream Products

4382-63-2Relevant academic research and scientific papers

Design, synthesis, and antibacterial evaluation of PFK-158 derivatives as potent agents against drug-resistant bacteria

Wang, Wei,Zhang, You-Wen,Hu, Shang-Jiu,Niu, Wei-Ping,Zhang, Guo-Ning,Zhu, Mei,Wang, Ming-Hua,Zhang, Fan,Li, Xue-Mei,Wang, Ju-Xian

supporting information, (2021/04/12)

Infections caused by antibiotic resistant bacteria are a major health concern throughout the world. It is well known that PFK-158 can enhance the antibacterial effect of polymyxin, but its own anti-bactericidal effect is rarely discussed. In order to inve

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