Identification of a potent and selective covalent Pin1 inhibitor was written by Pinch, Benika J.;Doctor, Zainab M.;Nabet, Behnam;Browne, Christopher M.;Seo, Hyuk-Soo;Mohardt, Mikaela L.;Kozono, Shingo;Lian, Xiaolan;Manz, Theresa D.;Chun, Yujin;Kibe, Shin;Zaidman, Daniel;Daitchman, Dina;Yeoh, Zoe C.;Vangos, Nicholas E.;Geffken, Ezekiel A.;Tan, Li;Ficarro, Scott B.;London, Nir;Marto, Jarrod A.;Buratowski, Stephen;Dhe-Paganon, Sirano;Zhou, Xiao Zhen;Lu, Kun Ping;Gray, Nathanael S.. And the article was included in Nature Chemical Biology.HPLC of Formula: 86069-86-5 The following contents are mentioned in the article:
Peptidyl-prolyl cis/trans isomerase NIMA-interacting 1 (Pin1) is commonly over-expressed in human cancers, including pancreatic ductal adenocarcinoma (PDAC). While Pin1 is dispensable for viability in mice, it is required for activated Ras to induce tumorigenesis, suggesting a role for Pin1 inhibitors in Ras-driven tumors, such as PDAC. We report the development of rationally designed peptide inhibitors that covalently target Cys113, a highly conserved cysteine located in the Pin1 active site. The inhibitors were iteratively optimized for potency, selectivity and cell permeability to give BJP-06-005-3, a versatile tool compound with which to probe Pin1 biol. and interrogate its role in cancer. In parallel to inhibitor development, we employed genetic and chem.-genetic strategies to assess the consequences of Pin1 loss in human PDAC cell lines. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5HPLC of Formula: 86069-86-5).
(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.HPLC of Formula: 86069-86-5
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem