A halogenated derivative of febrifugine that down-regulates Smad3

Halofuginone (hydrochloride) – 500 µg

Brand:
Cayman
CAS:
1217623-74-9
Storage:
-20
UN-No:
Non-Hazardous - /

Halofuginone is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.{26479} It has antimalarial and anticoccidial actions.{26479} In mammals, halofuginone at 10 ng/ml down-regulates Smad3, blocking TGF-β signaling and preventing both the differentiation of fibroblasts to myofibroblasts and the transitioning of epithelial cells to mesenchymal cells.{26479,26481} Through this action, halofuginone blocks fibrosis and tumor progression in a variety of different models.{26479,26482} This compound also competitively inhibits prolyl-tRNA synthetase (Ki = 18.3 nM), activating the amino acid starvation response.{26480,17217} This prevents the differentiation of TH17 cells, blunting an autoimmune response.{17217}  

 

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Description

A halogenated derivative of febrifugine that down-regulates Smad3, blocking TGF-β signaling relevant to fibrosis and tumor progression in a variety of different models; competitively inhibits prolyl-tRNA synthetase (Ki = 18.3 nM), preventing the differentiation of TH17 cells and blunting an autoimmune response

Formal name: 7-bromo-6-chloro-3-[3-[(2R,3S)-3-hydroxy-2-piperidinyl]-2-oxopropyl]-4(3H)-quinazolinone, monohydrochloride

Synonyms: 

Molecular weight: 451.1

CAS: 1217623-74-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Antibiotics||Product Type|Biochemicals|Antiparasitics|Antiprotozoals||Product Type|Biochemicals|Small Molecule Inhibitors|Amino Acid Turnover||Research Area|Cancer||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Autoimmunity||Research Area|Infectious Disease|Parasitic Diseases|Malaria

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