A potent activator of PKM2 (pyruvate kinase M2) with IC50 of 92 nM; shows no activity on PKM1 in vitro; binds to PKM2 at the subunit interaction interface site that is distinct from that of the endogenous activator FBP; inhibits xenograft tumor growth and orally bioactive.
1. Anastasiou D, et al. Nat Chem Biol. 2012 Oct;8(10):839-47.
2. Qi W, et al. Nat Med. 2017 Apr 24. doi: 10.1038/nm.4328.
3. Witney TH, et al. Sci Transl Med. 2015 Oct 21;7(310):310ra169.
M.Wt | 372.4645 | |
Formula | C17H16N4O2S2 | |
CAS No. | 1221186-53-3 | |
Storage |
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Solubility |
DMSO: ≥ 28 mg/mL |
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Chemical Name/SMILES | 5H-Thieno[2',3':4,5]pyrrolo[2,3-d]pyridazin-5-one, 6-[(3-aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)- |
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