4382-63-2
4382-63-2
Chemical Structure
PFK-015
- CAS No.: 4382-63-2
- Formula:C17H12N2O
- Molecular Weight:260.29
IUPAC Name: (E)-1-(pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one
InChIKey: UJJUKZPBUMCSJZ-BQYQJAHWSA-N
SMILES: O=C(C1=CC=NC=C1)/C=C/C2=NC3=CC=CC=C3C=C2
Biological Activity: PFK-015, a derivative of 3PO, is a specific PFKFB3 inhibitor. PFK-015 inhibits recombinant PFKFB3 with an IC50 value of 110 nM and inhibits PFKFB3 activity in cancer cells with an IC50 value of 20 nM. PFK-015 can be used for the research of multiple cancers such as lung cancer, stomach cancer, colon cancer and esophageal squamous cell carcinoma (ESCC)[1][2].
| Cat. No. | 상품명 | Purity | 제품 설명 | Pricing | |||||||||||||||||||
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PFK-015 | 99.48% | PFK-015, a derivative of 3PO, is a specific PFKFB3 inhibitor. PFK-015 inhibits recombinant PFKFB3 with an IC50 value of 110 nM and inhibits PFKFB3 activity in cancer cells with an IC50 value of 20 nM. PFK-015 can be used for the research of multiple cancers such as lung cancer, stomach cancer, colon cancer and esophageal squamous cell carcinoma (ESCC). | ||||||||||||||||||||
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DMU2105 | 99.31% | DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively. | ||||||||||||||||||||
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(E/Z)-DMU2105 | (E/Z)-DMU2105 (Compound 7k) is a potent and highly selective CYP1B1 inhibitor. (E/Z)-DMU2105 inhibits human CYP1B1 enzyme bound to yeast-derived microsomes with an IC50 value of 10 nM. (E/Z)-DMU2105 also potently inhibits CYP1B1 expressed within ‘live’ recombinant yeast and human HEK293 kidney cells with an IC50 value of 63.65 nM. (E/Z)-DMU2105 can be used for the research of cancer, glaucoma, ischemia and obesity. | |||||||||||||||||||||
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(E/Z)-3PO | 99.86% | (E/Z)-3PO is a potent PFKFB3 inhibitor. (E/Z)-3PO can inhibit the glycolysis process, reduce the extracellular acidification rate, and inhibit the capillary tube formation, migration of endothelial cells, and the formation of aortic sprouts, thereby suppressing angiogenesis. (E/Z)-3PO is promising for research of diseases such as cancer, acute lung injury, pulmonary fibrosis, and atherosclerosis. | ||||||||||||||||||||
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Quininib | 98.1% | Quininib is a cysteinyl leukotriene 1 and 2 receptor antagonist with IC50s of 1.2 and 52 μM for CysLT1R and CysLT2R, respectively. Quininib is a potent inhibitor of developmental angiogenesis in the zebrafish eye. Quininib can be used for the research of ocular neovascular pathologies and may complement current anti-VEGF biological agents. | ||||||||||||||||||||
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PFK-158 | 98.95% | PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria. | ||||||||||||||||||||
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Q8 | Q8, an effective antiangiogenic drug, is a CysLt1 antagonist (IC50 of 4.9 μM). Q8 is sufficient to reduce cellular levels of NF-κB and calpain-2 and secreted levels of the proangiogenic proteins intercellular adhesion molecule-1, vascular cell adhesion protein-1, and VEGF. | |||||||||||||||||||||
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hCYP3A4-IN-1 | hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC50 values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM). | |||||||||||||||||||||
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CYP1B1-IN-7 | 99.88% | CYP1B1-IN-7 (compound 2a) is a selective inhibitor of CYP1B1 (IC50: 75 nM). CYP1B1-IN-7 also reverses resistance (IC50: 29 μM) and exhibits cytotoxicity in the CYP1B1-overexpressing MCF-7 cell line that is resistant to Docetaxel (HY-B0011). | ||||||||||||||||||||
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3PO | 99.85% | 3PO is an inhibitor of PFKFB3. 3PO attenuates the proliferation of several cancer cell lines with IC50s of 1.4-24 μmol/L. 3PO suppresses glucose uptake and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+ and NADH. 3PO can be used for the research of cancer. | ||||||||||||||||||||
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Tubulin polymerization-IN-75 | 98.0% | Tubulin polymerization-IN-75 (Compound 6) is an inhibitor for tubulin polymerization with an IC50 of 30 μM. Tubulin polymerization-IN-75 inhibits the proliferation of cancer cell Huh7 and 293T with IC50 of 14.3 μM and 13.8 μM. | ||||||||||||||||||||
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References
- [1]. Jia Bo Zheng, et al. Glucose metabolism inhibitor PFK-015 combined with immune checkpoint inhibitor is an effective treatment regimen in cancer. Oncoimmunology. 2022 May 25;11(1):2079182. [Content Brief]
- [2]. Brian Clem, et al. Characterization of a novel small molecule antagonist of 6-phosphofructo-2-kinase that suppresses glucose metabolism and tumor growth. ORAL PRESENTATIONS - PROFFERED ABSTRACTS| APRIL 15 2011.
