UORSY Tubulin Inhibitors

Microtubules affect cell shape, motility, transport and mitosis,1 which make them desirable targets for anticancer treatment. Microtubule inhibitors, with both destabilizing and stabilizing action mechanisms, are known as antimitotic drugs.2 However, resistance to a range of tubulin-binding agents, as a consequence of β-tubulin mutations, has remained an unresolved issue.3

For creating a tubulin inhibitors library, we docked our screening compound library against crystal structures of the known protein-tubulin complexes (4YJ2, 5C8Y, 5CA1).4,5 The docking was performed into the binding site of colchicine-derived inhibitors resulting in a set of 2023 compounds.

     

Physicochemical profiles of UORSY tubulin inhibitors:

300<MW<400; 2<HbA<8; 0<HbD<4; -1<logP<5; 0<Fsp3<0.7; 2<RotBonds<9, 19<TPSA<165.

UORSY tubulin inhibitors are available in stock and could be delivered within 2 weeks in any customer-preferred format: as powders, dry films or DMSO solutions formatted in vials, 96 or 384-well plates. All compounds have a minimum purity of 90% assessed by 1H NMR; analytical data is provided.

For more information, please contact us at screenlibs@uorsy.com

1 Eva Nogales, Annu Rev Biomol Struct, 2001, 30, 397-420.
2 Edith A. Perez, Mol Cancer Ther, 2009, 8(8), 2086-2095.
3 Maria Kavallaris, Nat Rev Cancer, 2010, 10(3), 194-204.
4 Yuxi Wang et al, Febs J, 2016, 283, 102-111.
5 Dan E. McNamara et al, Protein Sci, 2015, 24, 1164-1172.

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