3PO是一种新型小分子PFKFB3同工酶的抑制剂, 显着衰减几个人恶性造血细胞和腺癌细胞系的增殖 (IC50为1.4-24 μM) 。 Information 3PO 3PO (3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one) is a small-molecule inhibitor of PFKFB3 with an IC50 of 22.9 μM for recombinant human PFKFB3 protein and does not inhibit PFK-1 activity. It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH. Targets PFKFB3 22.9 μM In vitro 3PO is an inhibitor of the PFKFB3 isozyme primarily through competition with Fru-6-P and does not inhibit purified PFK-1 activity. 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μmol/L) and is selectively cytostatic to ras-transformed human bronchial epithelial cells relative to normal human bronchial epithelial cells. 3PO can cause G2-M phase arrest. In vivo i.p. administration of 3PO (0.07 mg/g) to tumor-bearing mice markedly reduces the intracellular concentration of Fru-2,6-BP, glucose uptake, and growth of established tumors in vivo. It suppresses tumorigenic growth of breast adenocarcinoma, leukemia, and lung adenocarcinoma cells in vivo. The PK properties of 3PO are examined in C57Bl/6 mice intravenously administered 3PO: clearance CL=2312 mL/min/kg, T 1/2 =0.3 hr, C max =113 ng/ml, AUC 0-inf =36 ng/hr/ml. 3PO is reported to have potent activity against a highly relevant mouse model of leukemia. Cell Research(from reference) Cell lines：Jurkat cells Concentrations：10 μmol/L Incubation Time：0, 4, 8, 16, 24, or 36 h
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
3PO
CAS number：18550-98-6 molecular formula：C13H10N2O
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | THALICARPINE [MI] | 2-Propen-1-one, 3-(3-pyridinyl)-1-(4-pyridinyl)- | BCP34641 | s7639 | SCHEMBL196639 | CHEBI:144367 | BDBM50445948 | AS-55969 | NCGC00386709-03 | (E)-3PO | (E)-3-(Pyridin-3-yl)-1-(pyridin-4-yl)prop-2-en-1-one | (E)-3-pyridin-3-yl-1-pyri | ||
| CAS number | 18550-98-6 | molecular formula | C13H10N2O |
| molecular weight | 210.23 g/mol | Exact mass | ≥99% |
| PSA | 42.900 Ų | logp | 1.600 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
