Table 1.

Properties of putative BCL2 inhibitors

The good
BH3 mimetic	proposed targets	Induces NOXA in cells	Activates the ISR	Kills CLL cells ex vivo	Kill platelets ex vivo	ref
ABT-737/ABT263	BCL2, BCLXL	NO	NO	YES	YES	2,3
ABT-199	BCL2	NO	NO	YES	NO	6
WEHI-539	BCLXL	NO	NO	NO	YES	16
A-1155463	BCLXL	NO	NO	NO	YES	45

The bad
putative BH3 mimetics	proposed targets	Induces NOXA in cells	Activates the ISR	Kills CLL cells ex vivo	Kill platelet ex vivo	ref to drug	ref to criticism
gossypol & AT-101	pan-BCL2	YES	YES	NO	NO	20	10,18
apogossypol	pan-BCL2	YES	YES	NO	nd	46	10
S1	pan-BCL2	YES	YES	NO	NO	47	10,17
HA14-1	BCL2	YES	YES	NO	nd	48	10
2 methoxy antimycin A3	BCL2, BCLXL	YES	YES	NO	nd	49	10
obtaoclax (GX15-070)	pan-BCL2	YES	YES	NO	nd	50	10
BXI-61	BCLXL	YES	YES	NO	NO	51	N/A
BXI-72	BCLXL	YES	YES	NO	NO	51	N/A
TW37	BCL2, BCLXL, MCL1	YES	nd	nd	nd	52	53
MIM1	MCL1	YES	YES	NO	nd	22	N/A
UMI-77	MCL1	YES	YES	NO	nd	54	N/A

ISR: integrated stress response

nd: not determined

N/A: RSS and AE unpublished observations