Inhibitor SourceBook™ Second Edition

Phosphorylation/Dephosphorylation
Checkpoint Inhibitors
Product Cat. No. Comments Size Price
N Chk2 Inhibitor 220485 {5-(2-Amino-5-oxo-1,5-dihydroimidazol-4-ylidine)-3,4,5,10-2H-azepino[3,4-b]
indol-1-one, HCl}
A cell-permeable, potent inhibitor of Chk2 (IC 50 = 8 nM) with good selectivity over
MEK , Chk , CKId, PKCa, PKCbII, and CKII (IC 50 = 89 nM, 237 nM, .352 mM, 2.539 mM,
3.38 mM, and > 0.0 mM, respectively).
N Chk2 Inhibitor II 220486 [2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide]
A cell-permeable, potent, ATP-competitive inhibitor of Chk2 with an IC 50 of 5 nM and a
K i of 37 nM. Displays ~ 000-fold greater selectivity over Cdk /B and CKI (IC 50 = 2 mM
and 7 mM) and weakly affects the activities of a panel of 3 kinases ( < 25% inhibition
at 0 mM), including Chk .
Debromohymenialdisine,
Stylotella aurantium
252010 (DBH)
An alkaloid isolated from a shallow-water marine sponge that acts as a highly selective
inhibitor of checkpoint kinases Chk (IC 50 = 3 mM) and Chk2 (IC 50 = 3.5 mM). Inhibition is
competitive with respect to ATP and does not affect the activities of other kinases.
N Isogranulatimide 371957 (IGR)
A cell-permeable, potent, and ATP-competitive inhibitor of Chk (IC = 00 nM) and
50
GSK-3b (IC = 500 nM). Displays selectivity over G DNA damage checkpoint, Chk2,
50 2
Cdk , and DNA-PK (IC = 3 mM, 4 mM, 0 mM, and 0 mM, respectively). Only minimally
50
affects the activities of several other kinases tested including PKA, PKBa, and PKCb
(IC ≥ 40 mM).
50
N SB 2 8078 559402 [9,10,11,12,-Tetrahydro-9,12-epoxy-1H-diindolo(1,2,3-fg:3´,2´,1´-kl)pyrrolo
(3,4-i)(1,6)benzodiazocine-1,3(2H)-dione]
An indolocarbazole derivative that acts as a potent and selective inhibitor of checkpoint
kinase (Chk ) in vitro. Inhibits Chk phosphorylation of Cdc25C (IC = 5 nM).
50
SB-2 8078 is a much weaker inhibitor of Cdc2 (IC = 250 nM) and PKC (IC = mM).
50 50
N Scytonemin, Lyngbya
sp.
565715 A cell-permeable, selective, reversible, non-toxic, and mixed type inhibitor of polo-like
kinase (Plk ; IC 50 = 2.0 mM) and PKC bI (IC 50 = 3.4 mM) and exhibits anti-proliferative
and anti-inflammatory properties. Also inhibits several other cell cycle regulatory
kinases (IC 50 = 2.7, 3.0, .2, and .4 mM respectively for PKC bII , Cdk /B, Mytl, and Chk ).
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products and to request your free wall poster, visit our
Checkpoint Signaling and DNA Repair Interactive Pathways at:
www.calbiochem.com/checkpoint
500 mg $ 96
mg $93
00 mg $98
mg $ 39
mg $ 06
mg $98
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