Inhibition of in vitro Tubulin Assembly

IN VITRO TUBULIN ASSEMBLY, IC50 (mM)

DRUG

30°, 0.8 M Glu (no MgCl2)

37°, 1.0 M Glu, 1mM MgCl2

Hemiasterlin

1.0 ± 0.02

2.9 ± 0.10

Hemiasterlin A

1.1 ± 0.10

3.1 ± 0.04

Hemiasterlin C

1.3 ± 0.01

3.2 ± 0.50

Dolastatin 10

0.6 ± 0.05

1.6 ± 0.30

Cryptophycin 1

1.1 ± 0.10

3.3 ± 0.60

Cryptophycin 1 and all three hemiasterlins inhibit in vitro tubulin assembly similarly, approximately half as potently as dolastatin 10.


 


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