Table 1.

Published G2 checkpoint abrogators

G2-Specific Target (IC50 in nm)Other Targets (IC50 in nm)
Caffeine (52, 54)ATM (200,000), ATR (1,100,000)Adenosine receptor (21,000) etc.
Pentoxifylline (73)ATM, ATR
Staurosporin (60)CHK1 (8)PKC (5), CDC2 (6)
UCN-01 (60, 66, 74, 75)CHK1 (7), CHK2 (>1,000) (10)aPKC (4), PDK1 (33)
Go6976 (59)CHK1 (similar UCN-01, cellbPKC (20-fold less UCN-01, cellb)
SB-218078 (60)CHK1 (15)CDC2 (250)
ICP-1 (61)CHK1 (5-fold less UCN-01)
CEP-3891 (64)CHK1 (4), CHK2 (300,000)TrkA (9)
Debromohimenialdesine (65)CHK1 (3000), CHK2 (3,500)
TAT-S216A (5)CHK1 (∼30,000), CHK2 (∼30,000)
CEP-6367 (64)CHK2 (20), CHK1 (300)MLK3 (19)
PD0166285 (68)Wee1 (24), Myt1 (72)
Okadaic acid (76)PP2A (0.5)PP1 (60–500)
Fostriecin (70, 77)PP2A (40) (3.2)PP1 (4,000) (131,000)
13-Hydroxy-15-ozoapatlin (72)unknown
Isogranulatimide (67)unknown
  • a IC50 for immunoprecipitated CHK2 from HCT116 66.

  • b MDA-MD-231.