Description
BTB-1 (86030-08-2) is a selective, ATP-competitive and reversible inhibitor of mitotic kinesin Kif18A, IC50=1.7 mM.1,2 Binds to an allosteric site near Kif18A loop 5 preventing a range of conformational changes thereby blocking motor function.3 Inhibits the differentiation of mouse bone marrow cells to dendritic cells.4 Suppresses the replication of influenza A virus, inhibiting activation of AKT, p38 MAPK, SAPK and RanBP3 leading to the prevention of nuclear export of viral ribonucleoprotein complexes. Greatly improves the viability of IAV-infected mice.5
References
[1] MARIO CATARINELLA. BTB-1: A Small Molecule Inhibitor of the Mitotic Motor Protein Kif18A†[J]. Angewandte Chemie International Edition, 2009, 48 48: 9072-9076. DOI:
10.1002/anie.200904510[2] JOACHIM BRAUN. Synthesis and Biological Evaluation of Optimized Inhibitors of the Mitotic Kinesin Kif18A[J]. ACS Chemical Biology, 2014, 10 2: 554-560. DOI:
10.1021/cb500789h[3] JULIA LOCKE. Structural basis of human kinesin-8 function and inhibition.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2017: E9539-E9548. DOI:
10.1073/pnas.1712169114[4] Kinesin family member KIF18A is a critical cellular factor that regulates the differentiation and activation of dendritic cells
[5] YONG-BIN CHO. Selective and ATP-competitive kinesin KIF18A inhibitor suppresses the replication of influenza A virus[J]. JOURNAL OF CELLULAR AND MOLECULAR MEDICINE, 2020, 24 10: 5463-5475. DOI:
10.1111/jcmm.15200
