Table 1 Enzymatic activity of PARP/HDAC dual inhibitor B101–B602 against PARP1/2 and HDAC1/6.

From: Novel dual inhibitors of PARP and HDAC induce intratumoral STING-mediated antitumor immunity in triple-negative breast cancer

Cpds.

IC50 (nM)

IC50 (μM)

PARP1

PARP2

HDAC1

HDAC6

B101

13.15

4.08

0.12

> 10

B102

19.01

2.13

1.69

> 10

B201

7.55

13.78

0.06

> 10

B202

10.25

34.18

0.16

> 10

B301

11.43

70.39

> 10

> 10

B302

12.67

56.98

> 10

> 10

B401

ND

ND

> 10

> 10

B402

ND

ND

> 10

> 10

B501

ND

ND

> 10

> 10

B502

ND

ND

> 10

> 10

B601

ND

ND

> 10

> 10

B602

ND

ND

> 10

> 10

Olaparib

0.35

0.08

ND

ND

Vorinostat

ND

ND

0.01

0.04

Chidamide

ND

ND

0.04

> 10

  1. ND compound not detected against the enzyme.
Back to article page