Bis-T-23

Bis-T-23 is a promoter of dynamin oligomerization. It was originally discovered to inhibit phosphatidylserine-induced dynamin 1 GTPase activity (IC50 = 1.7 µM) but promotes dynamin oligomerization in COS-7 cells in an actin-dependent manner when used at a concentration of 30 µM and increases dynamin 1 GTPase activity in a cell-free assay in a concentration-dependent manner. In vivo, Bis-T-23 decreases proteinuria in several rodent models of kidney disease, including acute kidney injury, chronic kidney disease, and diabetic nephropathy. It also inhibits HIV-1 integrase (IC50s = 0.4, 0.16, and 2 µM for 3'-processing, strand transfer, and disintegration activities, respectively), is selective for HIV-1 integrase over calf thymus topoisomerase I at 100 µM, and has antiviral activity in HIV-infected CEM cells (EC50 = 15.6 µM). InChI: InChI=1S/C23H20N4O8/c24-10-14(4-12-6-16(28)20(32)17(29)7-12)22(34)26-2-1-3-27-23(35)15(11-25)5-13-8-18(30)21(33)19(31)9-13/h4-9,28-33H,1-3H2,(H,26,34)(H,27,35)/b14-4+,15-5+ InChIKey: AAPVOSBVTLGGOU-VHUAAIQRSA-N SMILES: OC1=CC(/C=C(C(NCCCNC(/C(C#N)=C/C2=CC(O)=C(O)C(O)=C2)=O)=O)\C#N)=CC(O)=C1O