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. 2021 May 19;133(26):14778–14784. doi: 10.1002/ange.202103711

Table 2.

Inhibition of AspH variants by 2OG oxygenase inhibitors.

Entry

Inhibitor

AspH

variant

IC50 [μM][a]

1

MnCl2

wt [17]

5.1±1.1

H679A

23.1±8.6

H725A

>40

2

CoCl2

wt [17]

0.4±0.2

H679A

1.5±0.2

H725A

3.0±0.5

3

NiSO4

wt [17]

0.17±0.08

H679A

2.7±0.4

H725A

1.8±0.4

4

Zn(OAc)2

wt [17]

0.05±0.01

H679A

0.16±0.01

H725A

0.16±0.01

5

N‐oxalyl‐glycine (NOG)

wt [17]

1.1±0.3

H679A

inactive

H725A

inactive

6

Pyridine‐2,4‐dicarboxylic acid

(2,4‐PDCA)

wt [17]

0.03±0.01

H679A

0.13±0.01

H725A

11.2±1.4

[a] Mean of two independent runs (n=2; mean ± SD). H679A/H725A AspH inhibition assays were performed as described in the Supporting Information Section 2 using 0.1 μM AspH variant and 4.0 μM hFX‐EGFD186‐124‐4Ser (Supporting Figure S2a); the assays were of good quality as high S/N ratios and Z′‐factors [19] (>0.5 for each plate) manifest (Supporting Figure S9).