SH5-07

SH5-07 is a STAT3 inhibitor (K_i = 10.46 µM).¹ It is selective for STAT3 over STAT1 (K_i = >100 µM). SH5-07 prevents constitutively active STAT3 DNA binding in NIH3T3 fibroblast nuclear extracts (IC₅₀ = 3.9 µM).² It is cytotoxic to AR230 and imatinib-resistant AR230 chronic myeloid leukemia (CML) cells (IC₅₀s = 8.1 and 7 µM, respectively) and a variety of glioblastoma cancer stem cells (CSCs; IC₅₀s = 0.195-1.12 µM).^3,1 SH5-07 reduces tumor growth in MDA-MB-231 breast cancer and U-251MG glioblastoma mouse xenograft models when administered at doses of 3 and 5 mg/kg, respectively.² It is also active against T. gondii when used at a concentration of 5 µM.⁴

WARNING This product is not for human or veterinary use.

1. Haftchenary, S., Luchman, H.A., Jouk, A.O., et al. Potent targeting of the STAT3 protein in brain cancer stem cells: A promising route for treating glioblastoma. ACS Med. Chem. Lett. 4(11), 1102-1107 (2013).

2. Yue, P., Lopez-Tapia, F., Paladino, D., et al. Hydroxamic acid and benzoic acid-based STAT3 inhibitors suppress human glioma and breast cancer phenotypes in vitro and in vivo. Cancer Res. 76(3), 652-663 (2016).

3. Ali, A.M., Gómez-Biagi, R.F., Rosa, D.A., et al. Disarming an electrophilic warhead: Retaining potency in tyrosine kinase inhibitor (TKI)-resistant CML lines while circumventing pharmacokinetic liabilities. ChemMedChem 11(8), 850-861 (2016).

4. Li, S., Ying, Z., Xue, Y., et al. Effects of different drugs and hormone treatment on Toxoplasma gondii glutathione S-transferase 2. Parasit. Vectors 15(1), 461 (2022).