GLI1 Inhibitors Identified by Target Protein Oriented Natural Products Isolation (TPO-NAPI) with Hedgehog Inhibition was written by Arai, Midori A.;Ochi, Fumie;Makita, Yoshinori;Chiba, Tetsuhiro;Higashi, Kyohei;Suganami, Akiko;Tamura, Yutaka;Toida, Toshihiko;Iwama, Atsushi;Sadhu, Samir K.;Ahmed, Firoj;Ishibashi, Masami. And the article was included in ACS Chemical Biology in 2018.Computed Properties of C14H25NO The following contents are mentioned in the article:
This report describes the development of a target-protein-oriented natural-products-isolation (TPO-NAPI) method for Hedgehog inhibitors and the direct GLI1 inhibitor, 5′-O-methyl-3-hydroxyflemingin A , which inhibited hedgehog (Hh) signal transduction and diminished characteristics of cancer stem cells. Eight natural products (including three newly described products) that directly bind to GLI1 were rapidly obtained via the TPO-NAPI method developed using GLI1 protein-immobilized beads. 5′-O-Methyl-3-hydroxyflemingin A inhibited Hh signaling (IC50 7.3 μM), leading to decreasing production of the Hh target proteins BCL2, PTCH1, and BMI1. 5′-O-Methyl-3-hydroxyflemingin A was cytotoxic to Hh-related cancer cells. CD experiments revealed that 5′-O-methyl-3-hydroxyflemingin A directly bound GLI1 (Kd = 7.7 μM). Moreover, 5′-O-methyl-3-hydroxyflemingin A diminished cancer stem cell characters of Huh7 such as sphere formation and production of the cancer stem cell marker EpCAM. These results suggest that Hh inhibitors can efficiently suppress the activity of cancer stem cells. This study involved multiple reactions and reactants, such as (2E,4E)-N-Isobutyldeca-2,4-dienamide (cas: 18836-52-7Computed Properties of C14H25NO).
(2E,4E)-N-Isobutyldeca-2,4-dienamide (cas: 18836-52-7) belongs to amides. Amides can be viewed as a derivative of a carboxylic acid RC(=O)OH with the hydroxyl group –OH replaced by an amine group −NR′R″; or, equivalently, an acyl (alkanoyl) group RC(=O)− joined to an amine group. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Computed Properties of C14H25NO
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics