Bis-T-23

Bis-T-23 is a promoter of dynamin oligomerization.¹ 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.^2,1 In vivo, Bis-T-23 decreases proteinuria in several rodent models of kidney disease, including acute kidney injury, chronic kidney disease, and diabetic nephropathy.³ 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).⁴

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1. Wang, Y., Cai, W., Cheng, Y., et al. Regulation of dynamin oligomerization in cells: The role of dynamin-actin interactions and its GTPase activity. Traffic 15(8), 819-838 (2014).

2. Hill, T., Odell, L.R., Edwards, J.K., et al. Small molecule inhibitors of dynamin I GTPase activity: Development of dimeric tyrphostins. J. Med. Chem. 48(24), 7781-7788 (2005).

3. Schiffer, M., Teng, B., Gu, C., et al. Pharmacological targeting of actin-dependent dynamin oligomerization ameliorates chronic kidney disease in diverse animal models. Nat. Med. 21(6), 601-609 (2015).

4. Mazumder, A., Gazit, A., Levitzki, A., et al. Effects of tyrphostins, protein kinase inhibitors, on human immunodeficiency virus type 1 integrase. Biochemistry 34(46), 15111-15122 (1995).