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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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