1126367-99-4

Usage

Uses

Used in Pharmaceutical Industry:
A⁽⁰⁸⁰⁾Z₁₂₂₈₂ is used as a hedgehog antagonist for inhibiting the SMO receptor, which is involved in embryonic growth and development. Its application in this industry is primarily focused on the development of treatments for various conditions related to the abnormal functioning of the hedgehog signaling pathway.
Used in Research and Development:
In the research and development sector, A⁽⁰⁸⁰⁾Z₁₂₂₈₂ is utilized as a valuable tool for studying the hedgehog signaling pathway and its role in embryonic development. A⁽⁰⁸⁰⁾Z₁₂₂₈₂ aids scientists in understanding the molecular mechanisms underlying various developmental processes and diseases, ultimately contributing to the advancement of medical knowledge and the development of novel therapeutic strategies.
Used in Drug Discovery:
A⁽⁰⁸⁰⁾Z₁₂₂₈₂ is employed as a lead compound in drug discovery efforts, particularly for the development of new therapeutic agents targeting the hedgehog signaling pathway. Its potent inhibitory activity against the SMO receptor makes it a promising candidate for the treatment of conditions associated with the dysregulation of this pathway, such as certain types of cancer and developmental disorders.

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Relevant academic research and scientific papers

Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO

Cell-based subset screening of compounds using a Gli transcription factor reporter cell assay and shh stimulated cell differentiation assay identified a series of bisamide compounds as hedgehog pathway inhibitors with good potency. Using a ligand-based optimization strategy, heteroaryl groups were utilized as conformationally restricted amide isosteres replacing one of the amides which significantly increased their potency against SMO and the hedgehog pathway while decreasing activity against p38α kinase. We report herein the identification of advanced lead compounds such as imidazole 11c and 11f encompassing good p38α selectivity, low nanomolar potency in both cell assays, excellent physiochemical properties and in vivo pharmacokinetics.

HETEROCYCLIC AMIDES USEFUL FOR THE TREATMENT OF CANCER AND PSORIASIS

The present disclosure relates to heterocyclic amide compounds, which are useful for inhibiting the Hedgehog pathway, and their use in treating a disease or medical condition mediated alone or in part by Hedgehog pathway inhibition. Also disclosed are methods for manufacture of these compounds, pharmaceutical compositions including these compounds, and use of these compounds in the manufacture of medicaments for treating such diseases and medical conditions in a subject. Formula (IA) with the provisio that either R2or R3 is (Z).