Formula: C7H6O2. DeSouza, SR; Olson, MC; Tinucci, SL; Sinner, EK; Flynn, RS; Marshall, QF; Jakubowski, HV; McIntee, EJ in [DeSouza, Shirin R.; Olson, Maxwell C.; Tinucci, Samantha L.; Sinner, Erica K.; Flynn, Rebecca S.; Marshall, Quinlen F.; Jakubowski, Henry, V; McIntee, Edward J.] St Johns Univ, Coll St Benedict, Dept Chem, St Joseph, MN 56374 USA published SAR of non-hydrolysable analogs of pyridoxal 5 ‘-phosphate against low molecular weight protein tyrosine phosphatase isoforms in 2020.0, Cited 15.0. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4.
Kinases and phosphatases are key enzymes in cell signal transduction pathways. Imbalances in these enzymes have been linked to numerous disease states ranging from cancer to diabetes to autoimmune disorders. The two isoforms (IFA and IFB) of Low Molecular Weight Protein Tyrosine Phosphatase (LMW-PTP) appear to play a role in these diseases. Pyridoxal 5’-phosphate (PLP) has been shown to act as a potent but, impractical micromolar inhibitor for both isoforms. In this study, a series of non-hydrolysable phosphonate analogs of PLP were designed, synthesized and tested against the two isoforms of LMW-PTP. Assay results demonstrated that the best inhibitor for both isoforms was compound 5 with a K-is of 1.84 mu M (IFA) and 15.6 mu M (IFB). The most selective inhibitor was compound 16, with a selectivity of roughly 370-fold for IFA over IFB.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles