WR-S-462
WR-S-462 is a STAT3 inhibitor. WR-S-462 effectively suppresses STAT3 phosphorylation and biological functions in vitro. WR-S-462 inhibits MDA-MB-231 cells with an IC50 of 0.03 μM. WR-S-462 displays a strong binding affinity towards the STAT3 protein with a Kd of 58 nM. WR-S-462 inhibits the nuclear translocation of p-STAT3, selectively inhibits the expression of p-STAT3Tyr705 and downstream target genes regulated by STAT3 in MDA-MB-231 cells such as Cyclin D1, Bcl-2, and Bcl-xl. WR-S-462 inhibits TNBC (triple-negative breast cancer) growth and metastasis[1].
Product Specifications
UNSPSC
12352005
Target
Bcl-2 Family; STAT
Related Pathways
Apoptosis; JAK/STAT Signaling; Stem Cell/Wnt
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Smiles
COC1=C(NC(N2CC(SC(NC(C3=CC=CC(OC)=C3)=O)=C4C#N)=C4CC2)=O)C=CC=C1
Molecular Formula
C24H22N4O4S
Molecular Weight
462.52
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Bcl-2; Bcl-xL; STAT3
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