SI-109

SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM) . SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36[1].

Product Specifications

CAS Number

[2429877-30-3]

UNSPSC

12352005

Target

Ligands for Target Protein for PROTAC; STAT

Type

Reference compound

Related Pathways

JAK/STAT Signaling; PROTAC; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/si-109.html

Purity

99.91

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C([C@@H](NC([C@@H]1CC[C@H](CCN(C(C)=O)C[C@@H]2NC(C3=CC(C=C(C(F)(P(O)(O)=O)F)C=C4)=C4N3)=O)N1C2=O)=O)CCC(N)=O)NC(C5=CC=CC=C5)C6=CC=CC=C6

Molecular Formula

C40H44F2N7O9P

Molecular Weight

835.79

References & Citations

[1]Bai L, et al. A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo. Cancer Cell. 2019 Nov 11;36 (5) :498-511.e17.