Table 4 Quantification of inhibition of mycolate containing products by GSK3011724A.

From: Identification of KasA as the cellular target of an anti-tubercular scaffold

Inhibitor

Inhibitor concentration (μM)

FAMEs

α-MAMEs

k-MAMEs

TDM

TMM

  

c.p.m.

% Relative to control

c.p.m.

% Relative to control

c.p.m.

% Relative to control

c.p.m.

% Relative to control

c.p.m.

% Relative to control

Control

0

9,796

100

4,029

100

7,641

100

3,149

100

1,425

100

GSK3011724A

0.25

16,207

165

3,438

85

7,147

94

ND

ND

ND

ND

 

0.5

17,780

182

3,026

75

6,651

87

864

27

911

64

 

1

16,478

168

2,488

62

4,925

64

874

28

893

63

 

2

18,268

186

1,806

45

4,407

58

ND

ND

ND

ND

 

4

ND

ND

ND

ND

ND

ND

652

21

951

67

Control

0

10,231

100

4,156

100

6,722

100

—*

—*

—*

—*

TLM

95

15,334

150

2,721

65

3,727

55

817

26

704

49

INH

1.5

16,926

165

1,426

34

1,808

27

642

20

552

39

  1. α-MAMEs, α-mycolate acid methyl esters; FAMEs, fatty acid methyl esters; INH, isoniazid; k-MAMEs, keto-mycolic acid methyl esters; ND, not determined; TDM, trehalose dimycolate; TLM, thiolactomycin; TMM, trehalose monomycolate.
  2. Quantification of [14C]-labelled products were determined by excising spots directly from TLC plates (Fig. 2a, left and middle panels, and Fig. 2b) and subjecting them to scintillation counting using 10 ml of EcoScintA.
  3. *Control values as reported above.