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SD-36

Cat. No. M21159

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SD-36 Structure
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1mg USD 1080  USD1080 In stock
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Biological Activity

SD-36 is a potent STAT3 PROTAC degradation agent (Kd=~50 nM) with a high selectivity compared to other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). Induction of STAT3 degradation resulted in strong inhibition of its transcriptional network in leukemia and lymphoma cells. SD-36 inhibited the growth of a subset of acute myeloid leukemia and anaplastic large cell lymphoma cell lines by inducing cell cycle arrest and/or apoptosis. SD-36 achieved complete and durable tumor regression in multiple xenograft mouse models with well-tolerated dosing schedules. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase.

Chemical Information
Molecular Weight 1158.15
Formula C59H62F2N9O12P
CAS Number 2429877-44-9
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage -20°C, sealed
References

[1] Vassiliki Sinopoulou, et al. Cochrane Database Syst Rev. Interventions for the management of abdominal pain in Crohn's disease and inflammatory bowel disease

[2] Shiqi Kong, et al. J Cell Mol Med. SD-36 promotes growth inhibition and induces apoptosis via suppression of Mcl-1 in glioma

[3] Haibin Zhou, et al. J Med Chem. Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein

[4] Longchuan Bai, et al. Cancer Cell. A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo

[5] Mehdi Kargarfard, et al. Arch Phys Med Rehabil. Randomized Controlled Trial to Examine the Impact of Aquatic Exercise Training on Functional Capacity, Balance, and Perceptions of Fatigue in Female Patients With Multiple Sclerosis

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Keywords: SD-36 supplier, PROTAC, inhibitors, activators

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