STAT3-IN-52

• Description:

  STAT3-IN-52 (Compound 9) is a selective and orally active signal transducer and activator of transcription 3 (STAT3) inhibitor. STAT3-IN-52 binds to the pY705 site of STAT3 (Ki = 440 nM), blocking the phosphorylation and dimerization of STAT3. STAT3-IN-52 shows strong cytotoxicity against various cancer cells, such as breast cancer MDA-MB-231 (IC50 = 0.7 μM), medulloblastoma UW426, pancreatic cancer BKPC3 cells. STAT3-IN-52 can induce cell apoptosis, inhibit the STAT3 nuclear transport and DNA binding activity and downregulate the expression of the STAT3 target gene MMP9. STAT3-IN-52 can be used for research related to STAT3 abnormal activation in cancer[1].

• UNSPSC:

  12352005

• Target:

  Apoptosis; MMP; STAT

• Related Pathways:

  Apoptosis; JAK/STAT Signaling; Metabolic Enzyme/Protease; Stem Cell/Wnt

• Field of Research:

  Cancer

• Smiles:

  O=S(C(C=CC=C1C(C(NC2=CC=CC=C2N3CCNCC3)=C4)=O)=C1C4=O)(N)=O

• Molecular Formula:

  C20H20N4O4S

• Molecular Weight:

  412.46

• References & Citations:

  [1]Yu W, et al. Discovery of an Orally Selective Inhibitor of Signal Transducer and Activator of Transcription 3 Using Advanced Multiple Ligand Simultaneous Docking. J Med Chem. 2017 Apr 13;60 (7) :2718-2731.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  MMP-9; STAT3

• CAS Number:

  [1556861-34-7]