BTB-1 is a novel small molecule inhibitor of the mitotic motor protein Kif18A, which was identified by Catarinella et al. during a highthroughput screen against Kif18A’s MT-stimulated ATPase activity, with an IC50 of 1.7–1.9 M . It is selective within the kinesin subgroup of Kif4, Eg5, MKLP-1, MKLP-2, MPP1, CENP-E and MCAK, and during in vitro motility assays Kif18A’s MT gliding ability was blocked by the addition of BTB-1 in a reversible manner. BTB-1 was found to be ATP competitive and MT uncompetitive, only inhibiting the ATPase activity of the MT-bound motor protein. BTB-1 could serve as a valuable tool in disentangling the nature of Kif18A’s double functionality within mitosis and assessing for potential therapeutic utilities.
MedKoo Cat#: 406243
Name: BTB-1
CAS#: 86030-08-2
Chemical Formula: C12H8ClNO4S
Exact Mass: 296.9863
Molecular Weight: 297.71
Elemental Analysis: C, 48.41; H, 2.71; Cl, 11.91; N, 4.70; O, 21.50; S, 10.77
The following data is based on the product molecular weight 297.71 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
