Inhibitor SourceBook™ Second Edition

Phosphorylation/Dephosphorylation
Cyclin-Dependent Kinase (Cdk) Inhibitors, continued
Product Cat. No. Comments Size Price
N Cdk /2 Inhibitor III 217714 A cell-permeable triazolo-diamine compound that displays anti-proliferative properties
in various human cancer cells (IC 50 = 20 nM, 35 nM and 92 nM in HCT- 6, HeLa and A375
cells, respectively). Acts as a highly potent ATP-competitive inhibitor of Cdk /B and Cdk2/
A (IC 50 = 600 pM and 500 pM) with selectivity over VEGF-R2 and GSK-3b
(IC 50 = 32 nM and 40 nM). Only minimally affects a panel of kinases tested (IC 50 = .0 mM,
.6 mM, 2.8 mM, 5.2 mM, 8.9 mM, > 0 mM, and > 00 mM for ERK-2, PDGF-Rb, CKI, PKA,
CaMKII, EGF-R or insulin kinase-b, and CKII, respectively).
Cdk /5 Inhibitor 217720 (3-Amino-1H-pyrazolo[3,4-b]quinoxaline)
A selective and potent inhibitor of Cdk and Cdk5 (IC 50 = 600 nM for Cdk /cyclin B and
400 nM for Cdk5/p25 respectively).
Cdk2 Inhibitor I 219442 (YSFVHHGFFNFRVSWREMLA)
A potent inhibitor of Cdk2 (K d = 38 nM).
Cdk2 Inhibitor II 219445 (Compound 3)
A potent and selective inhibitor of Cdk2 (IC 50 = 60 nM).
Cdk2 Inhibitor III 238803 [2(bis-(Hydroxyethyl)amino)-6-(4-methoxybenzylamino)-9-isopropyl-purine]
A cell-permeable, selective, reversible, ATP-competitive inhibitor of Cdk2/cyclin A and
Cdk2/cyclin E (IC 50 = 500 nM).
N Cdk2 Inhibitor IV,
NU6 40
238804 A highly cell-permeable purine compound that acts as a selective and ATP-competitive
inhibitor of Cdks (IC 50 = 6.6 mM, 0.4 mM, 5.5 mM, 5 mM, and 3.9 mM for Cdk /B, Cdk2/
A, Cdk4/D, Cdk5/p25, and Cdk7/H, respectively), and displays anticancer properties.
Shown to cause cell cycle arrest at G 2 -M phase, and induce apoptosis by activating
caspases and downregulating survivin. Further, synergistically potentiates paclitaxel
cytotoxicity and apoptotic response in HeLa, OAW42/e, and OAW42/Surv cells.
Cdk2/5 Inhibitor 219448 [N 4 -(6-Aminopyrimidin-4-yl)-sulfanilamide, HCI; PNU 112455A]
An aminopyrimidine derivative that acts as a selective inhibitor of Cdk2/cyclin E and
Cdk5/p25 (K i = 2 mM). The inhibition is competitive with respect to ATP.
Cdk2/Cyclin Inhibitory
Peptide I
Cdk2/Cyclin Inhibitory
Peptide II
238801 (Tat-LFG; YGRKKRRQRRRGPVKRRLFG)
A cell-permeable peptide inhibitor derived from the consensus sequence, PVKRRLFG,
that serves as the docking site for Cdk2/cyclin complexes. Blocks the phosphorylation of
substrates by Cdk2/cyclin A and Cdk2/cyclin E complexes.
238802 (Tat-LDL; YGRKKRRQRRRGPVKRRLDL)
A cell-permeable peptide inhibitor derived from the cell-cycle regulatory transcription
factor, E2F, that is derived from the Cdk2/cyclin A binding motif. Blocks the
phosphorylation of substrates by Cdk2/cyclin A and Cdk2/cyclin E complexes.
Cdk4 Inhibitor 219476 {2-Bromo-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione}
A cell-permeable, potent, selective ATP-competitive inhibitor of Cdk4/cyclin D
(IC 50 = 76 nM).
N Cdk4 Inhibitor II, NSC
625987
219477 [1,4-Dimethoxy-9-thio(10H)-acridone]
A potent, substrate-competitive inhibitor of Cdk4/cyclin D (IC 50 = 200 nM). Displays
~500-fold greater selectivity for Cdk4/cyclin D over Cdc2/cyclin A (Cdk /cyclin A),
Cdk2/cyclin A, and Cdk2/cyclin E (IC 50 > 00 mM).
Compound 52 234503 [2-(2-Hydroxyethylamino)-6-(3-chloroanilino)-9-isopropylpurine]
A potent, cell-permeable, and selective inhibitor of the cell cycle-regulating kinase,
Cdc28p (IC 50 = 7 mM), and the related Pho85p kinase (IC 50 = 2 mM).
mg $88
5 mg $ 8
mg $ 23
6 Orders Phone 800 854 34 7
Calbiochem • Inhibitor SourceBook
Fax 800 776 0999
Web www.emdbiosciences.com/calbiochem
mg
5 mg
mg
5 mg
$39
$ 23
$58
$200
5 mg $ 39
5 mg $93
500 mg $ 0
500 mg $ 0
mg $84
5 mg $ 8
mg $65
Fascaplysin, Synthetic 341251 A cell-permeable, potent, ATP-competitive inhibitor of Cdk4/cyclin D (IC 50 = 350 nM). mg $79
GSK-3 Inhibitor IX 361550 BIO; (2'Z,3'E)-6-Bromoindirubin-3'-oxime
A cell-permeable, highly potent, selective, reversible, and ATP-competitive inhibitor of
GSK-3a/b (IC 50 = 5 nM). At higher concentrations, inhibits Cdk2/cyclin A (IC 50 = 300 nM)
and Cdk5/p25 (IC 50 = 83 nM).
InSolution GSK-3
Inhibitor IX
Hymenialdisine, Stylissa
damicornis
mg $95
361552 A 0 mM (500 mg/ 40 ml) solution of GSK-3 Inhibitor IX (Cat. No. 36 550) in DMSO. 500 mg $63
400085 {4-(2-Amino-4-oxo-2-imidazolidin-5-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo
2,3-c]azepin-8-one; HD; 10Z-Hymenialdisine}
A cell-permeable, ATP-competitive inhibitor of MEK- (IC = 6 nM), Cdk /cyclin B
50
(IC = 22 nM); Cdk2/cyclin E (IC = 40 nM); Cdk5/p35 (IC = 28 nM); and GSK-3b
50 50 50
(IC = 0 nM).
50
500 mg $207