Table 1.

Kinetic properties of p97 mutants and IC₅₀ values of CB-5083 and NMS-873

Values shown are mean ± S.E. (n = 4).

	KM	kcat	kcat/KM	CB-5083	NMS-873
	μm	min−1	μm−1 min−1 × 10−3	nm	nm
WT	162 ± 22	13.4 ± 0.6	83 ± 12	8.4 ± 0.1	14 ± 1
MSP-1 mutants
R95G	88 ± 12	13 ± 0.5	147 ± 21	5.5 ± 0.1	10 ± 1
R155H	100 ± 13	21.5 ± 0.9	215 ± 29	3.3 ± 0.1	10 ± 1
NMS-873 mutants
A530T	91 ± 13	52 ± 2	572 ± 87	7.7 ± 0.1	46 ± 4
R567H	143 ± 17	21.6 ± 0.8	151 ± 18	8.1 ± 0.2	80 ± 8
K615V	173 ± 21	30 ± 1	173 ± 22	4.3 ± 0.4	97 ± 8
N616F	93 ± 11	15 ± 1	161 ± 19	14 ± 2	>4000a
L639F	123 ± 13	42 ± 1	341 ± 38	5.9 ± 0.1	140 ± 16
CB-5083 mutants
P472L	51 ± 7	55 ± 2	1084 ± 147	105 ± 10	569 ± 54
Q473P	95 ± 12	43 ± 2	446 ± 59	11.4 ± 0.8	14 ± 1
V474A	110 ± 17	52 ± 3	471 ± 77	34 ± 3	25 ± 3
G481A	280 ± 47	34 ± 2	123 ± 22	33 ± 3	47 ± 5
N660K	105 ± 11	8.4 ± 0.3	80 ± 9	202 ± 19	8 ± 0.8
T688A	94 ± 10	1.23 ± 0.04	13 ± 1	248 ± 31	36 ± 3

^a Activity inhibition was not observed over the concentration range tested.