Inhibitor SourceBook™ Second Edition

Cyclin-Dependent Kinase (Cdk) Inhibitors
Calbiochem • Inhibitor SourceBook
Phosphorylation/Dephosphorylation
Product Cat. No. Comments Size Price
Aloisine A 128125 {7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine; RP107}
A potent, cell-permeable, selective, reversible, and ATP-competitive inhibitor of Cdks
(IC 50 = 50 nM for Cdk /cyclin B, 20 nM for Cdk2/cyclin A, 400 nM for Cdk2/cyclin E,
and 60 nM for Cdk5/p35). Also inhibits GSK-3 (IC 50 = 500 nM for GSK-3a and .5 mM
for GSK-3b), JNK (IC 50 ~3– 0 mM), ERKs (IC 50 = 8 mM for ERK and 22 mM for ERK2),
PIM (IC 50 > 0 mM), and insulin receptor tyrosine kinase (IC 50 = 60 mM).
Aloisine, RP 06 128135 {7-n-Butyl-6-(4-methoxyphenyl)[5H]pyrrolo[2,3-b]pyrazine; RP106}
A cell-permeable, potent, selective, ATP-competitive inhibitor of Cdk /cyclin B
(IC 50 = 700 nM), Cdk5/p25 (IC 50 = .5 mM), and GSK-3 (IC 50 = 920 nM).
Alsterpaullone 126870 {9-Nitro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one}
A potent inhibitor of Cdk /cyclin B (IC 50 = 35 nM). Also inhibits the activity of Cdk5/p25dependent
phosphorylation of DARPP-32. One of the most active paullones that acts by
competing with ATP for binding to GSK-3b and inhibits the phosphorylation of tau.
N Alsterpaullone,
2-Cyanoethyl
126871 An Alsterpaullone (Cat. No. 26870) derivative that acts as a highly potent and ATPcompetitive
preferential inhibitor of Cdk /B and GSK-3b (IC 50 = 230 pM and 800 pM,
respectively; [ATP] = 5 mM), and displays ~37-fold greater selectivity over Cdk5/p25
(IC 50 = 30 nM). Shown to inhibit other kinases in a commercially available testing screen
panel (pIC 50 = -logIC 50 [M]; pIC 50 ~ 7.5, 7.0, 7.0, 6.5, 6.5, 6.0, and 6.0 for Cdk2/A, Cdk4/D ,
GSK-3b, PDGFRb, Src, VEGFR-2, and VEGFR-3, respectively; [ATP] = mM).
N Aminopurvalanol A 164640 [(2R)-2-((6-((3-Amino-5-chlorophenyl)amino)-9-(1-methylethyl)-9H-purin-2-yl)amino)-
3-methyl-1-butanol; NG-97]
A cell-permeable, 2,6,9-trisubstituted purine analog with antitumor properties
(GI 50 ~ .8 mM in the NCI 60-cell panel in vitro activity screen, potently inhibits the
growth of KM 2 colon cancer cells with a GI 50 of 30 nM). Acts as a reversible and ATPcompetitive
inhibitor of Cdks (IC 50 = 33 nM for Cdk /cyclin B and Cdk2/cyclin A, 28 nM
for Cdk2/cyclin E, and 20 nM for Cdk5/p35), and displays ~ 00-fold greater selectivity
over a panel of kinases tested (IC 50 ≥ 2.4 mM).
Bohemine 203600 {[6-Benzylamino-2-(3-hydroxypropylamino)-9-isopropylpurine}
A synthetic, cell-permeable, Cdk inhibitor (IC 50 = mM) that is structurally similar to
Olomoucine (Cat. No. 495620) and Roscovitine (Cat. No. 557360).
N Cdc2-Like Kinase
Inhibitor, TG003
219479 [Clk Inhibitor, TG003; (Z)-1-(3-Ethyl-5-methoxy-2,3-dihydrobenzothiazol-
2-ylidene)propan-2-one]
A cell-permeable dihydrobenzothiazolo compound that acts as a potent, specific,
reversible, and ATP-competitive inhibitor of Clk-family of kinases (K i = 0 nM for mClk /
Sty; IC 50 = 5 nM, 20 nM, 200 nM, and > 0 mM for mClk4, mClk , mClk2, and mClk3,
respectively). Does not affect the activities of SRPK , SRPK2, PKA, or PKC up to mM.
Cdk Inhibitor, p35 219457 [2-(3-Hydroxypropylamino)-6-(o-hydroxybenzylamino)-9-isopropylpurine]
An analog of Olomoucine (Cat. No. 495620) that acts as a potent inhibitor of Cdk
(IC 50 = 00 nM) and Cdk2 (IC 50 = 80 nM).
Cdk Inhibitor 217695 [3-(2-Chloro-3-indolylmethylene)-1,3-dihydroindol-2-one]
A selective, ATP-competitive inhibitor of Cdk /cyclin B (IC 50 = 5.8 mM for Cdk and
25 mM for Cdk5). Does not affect the activity of GSK-3b even at 00 mM
concentrations. Binds to the ATP pocket in the Cdk active site.
Cdk Inhibitor,
CGP745 4A
217696 [N-(cis-2-Aminocyclohexyl)-N-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine;
CGP74514A]
A cell-permeable, potent, and selective inhibitor of Cdk /cyclin B (IC = 25 nM).
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Cdk Inhibitor III 217697 {Ethyl-(6-hydroxy-4-phenylbenzo[4,5]furo[2,3-b])pyridine-3-carboxylate}
A cell-permeable and selective inhibitor of Cdk /cyclin B (IC 50 = 28.8 mM).
N Cdk /2 Inhibitor II,
NU6 02
217713 [6-Cyclohexylmethoxy-2-(4´-sulfamoylanilino)purine]
A 2,6-disubstituted purine compound that acts as a potent and ATP-competitive
inhibitor of Cdk /cyclin B and Cdk2/cyclin A3 (IC 50 = 9.5 nM and 5.4 nM). Displays greater
selectivity for Cdk /2 over other kinases tested (IC 50 = 600 nM, 800 nM, 900 nM, and
.6 mM for ROCKII, PDK , DYRK A and Cdk4/D , respectively). Shown to inhibit human
MCF-7 breast carcinoma cell growth with a GI 50 of 8 mM.
5 mg $90
5 mg $73
mg $83
mg $ 39
5 mg $ 52
mg
5 mg
$60
$ 46
5 mg $84
mg $72
5 mg $ 0
5 mg $ 26
mg
5 mg
mg
5 mg
$84
$299
$57
$ 45
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