SD-36

SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM) . SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase[1]. SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[2429877-44-9]

UNSPSC

12352005

Hazard Statement

H315-H319-H320

Target

Apoptosis; PROTACs; STAT

Type

Reference compound

Related Pathways

Apoptosis; JAK/STAT Signaling; PROTAC; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/sd-36.html

Purity

99.73

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C([C@@H](NC([C@@H]1CC[C@H](CCN(C(CCCCCC#CC2=CC=CC3=C2CN(C4CCC(NC4=O)=O)C3=O)=O)C[C@@H]5NC(C6=CC(C=C(C(F)(P(O)(O)=O)F)C=C7)=C7N6)=O)N1C5=O)=O)CCC(N)=O)NC(C8=CC=CC=C8)C9=CC=CC=C9

Molecular Formula

C59H62F2N9O12P

Molecular Weight

1158.15

Precautions

P264-P280-P302+P352-P305+P351+P338-P362

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.