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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.

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.