A cell-permeable inhibitor of STAT3; induces apoptosis in U87-MG (IC50 = 5.6 µM) and U373-MG (IC50 = 3.7 µM) cells; orally bioavailable

WP1066 – 1 mg

Brand:
Cayman
CAS:
857064-38-1
Storage:
-20
UN-No:
Non-Hazardous - /

WP1066 is a cell-permeable inhibitor of STAT3 that directs dephosphorylation and nuclear export of constitutively phosphorylated STAT3 in U87-MG and U373-MG malignant glioma cells when given at a concentration of 10 µM.{24389} It also induces apoptosis in U87-MG (IC50 = 5.6 µM) and U373-MG (IC50 = 3.7 µM) cells.{24389} WP1066 is orally bioavailable, crosses the blood-brain barrier, and demonstrates in vivo activity, including immune activation as indicated by the up-regulation of CD80 and CD86 and the induction of proliferation of effector T cells.{24390,24391} In addition to inducing apoptosis in cancer cells, WP1066 suppresses vascular smooth muscle cell proliferation after vascular injury in mice and prevents seizures following brain injury in rats.{24388,24392}  

 

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Description

A cell-permeable inhibitor of STAT3; induces apoptosis in U87-MG (IC50 = 5.6 µM) and U373-MG (IC50 = 3.7 µM) cells; orally bioavailable, crosses the blood-brain barrier, and demonstrates in vivo activity

Formal name: 3-(6-bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2E-propenamide

Synonyms:  STAT Inhibitor III

Molecular weight: 356.2

CAS: 857064-38-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|JAK/STAT Signaling||Research Area|Cancer|Transcription Factors|STATs||Research Area|Cardiovascular System|Vasculature|Angiogenesis||Research Area|Cardiovascular System|Vasculature|Smooth Muscle Cells||Research Area|Immunology & Inflammation|Adaptive Immunity

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