Inhibitor SourceBook™ Second Edition

More documents

Recommendations

Info

Phosphorylation/Dephosphorylation Selected Cdk Inhibitors (IC 50 in mM) Product Cat. No. Cdk1 Cdk2 Cdk4 Cdk5 Alsterpaullone 26870 0.035 – – – Alsterpaullone, 2-Cyanoethyl 2687 0.000230 – 0.030 Aloisine A 28 25 0. 5 (B) 0. 2 (A), 0.40 (E) 0.20 (p25), 0. 6 (p35) Aloisine A, RP 06 28 35 0.70 (B) .50 (p35) N Aminopurvalanol A 64640 0.033 0.033 (A), 0.028 (E) 0.020 (p35) Bohemine 203600 .0 0.80 (E) – – Cdk Inhibitor, p35 2 9457 0. 0 0.80 (E) – – Cdk Inhibitor 2 7695 5.8 – – 25.0 Cdk Inhibitor, CGP745 4A 2 7696 0.025 (B) – – – Cdk Inhibitor III 2 7697 28.8 (B) – – – N Cdk /2 Inhibitor II, NU6 02 2 77 3 0.0095 (B) 0.0054 (A3) .6 (D ) – Cdk /5 Inhibitor 2 7720 0.60 (B) – – 0.40 (p25) Cdk2 Inhibitor I 2 9442 – 0.038 a – – Cdk2 Inhibitor II 2 9445 0.78 0.060 – – Cdk2 Inhibitor III 238803 4.2 (B) 0.5 (A and E) 2 5.0 (D ) – Cdk2/5 Inhibitor 2 9448 – 2.0 b – 2.0 b N Cdk4 Inhibitor 2 9476 2. (B) 0.52 (E) 0.076 (D ) – N Cdk4 Inhibitor II, NSC 625987 2 9477 > 00 (A) > 00 (E) 0.20 (D ) – Fascaplysin, Synthetic 34 25 > 00 > 50 (A and E) 0.35 (D ) 20.0 Hymenialdisine, Stylissa damicornis 400085 0.022 0.040 (E) 0.028 Indirubin-3’-monoxime 402085 0. 8 - - 0. 0 Indirubin-3’-monoxime, 5-Iodo- 402086 0.025 - - 0.020 Indirubin-3’-monoxime-5-sulphonic Acid 402088 0.005 - - 0.007 Kenpaullone 422000 0.40 (B) 0.68 (A), 7.5 (E) - 0.85 Olomoucine 495620 7.0 (B) 7.0 (A and E) > 000 (D) 3.0 (p35) Olomoucine II 49562 0.02 (B) Olomoucine, Iso 495622 > 500 (B) > 000 (D) > 000 (p35) Olomoucine, N 9 -Isopropyl- 495623 2.0 Oxindole I 499600 0.2 0.0 (E) 4.90 Protein Kinase inhibitor, DMAP 476493 300 (B) Purvalanol A 540500 0.004 (B) 0.07 (A), 0.035 (E) 0.075 (p35) Roscovitine 557360 0.65 0.7 (A and E) > 000 0.2 (p35) Roscovitine, (S)-Isomer 557362 0.80 (B) Staurosporine 569397 0.009 0.007 - - SU95 6 572650 0.04 (B) 0.022 (A) 0.20 (D ) WHI-P 80, Hydrochloride 68 500 .0 Key: a = K d ; b = K i . Letters in parentheses refer to associated cyclins or Cdks. 4 Orders Phone 800 854 34 7 Calbiochem • Inhibitor SourceBook Fax 800 776 0999 Web www.emdbiosciences.com/calbiochem
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). 50 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 Technical Support Phone 800 628 8470 E-mail calbiochem@emdbiosciences.com 5
Page 1 and 2: Inhibitor SourceBook Second Editio
Page 3 and 4: Calbiochem • Inhibitor SourceBook
Page 7 and 8: Akt (Protein Kinase B) Inhibitors,
Page 9 and 10: Calmodulin-Dependent Protein Kinase
Page 11 and 12: Casein Kinase (CK) Inhibitors Casei
Page 13 and 14: Checkpoint Kinase Inhibitors Eukary
Page 15: Cyclin-Dependent Kinase (Cdk) Inhib
Page 19 and 20: Cyclin-Dependent Kinase (Cdk) Inhib
Page 21 and 22: Glycogen Synthase Kinase-3 (GSK-3)
Page 23 and 24: Glycogen Synthase Kinase Inhibitors
Page 25 and 26: c-Jun N-Terminal Kinase (JNK/SAP Ki
Page 27 and 28: Mitogen-Activated Protein (MAP) Kin
Page 29 and 30: MAP Kinase Inhibitors, continued Ca
Page 31 and 32: Myosin Light Chain Kinase (MLCK) In
Page 33 and 34: Phosphatidylinositol 3-Kinase (PI 3
Page 37 and 38: Protein Kinase A (PKA; cAMP-Depende
Page 39 and 40: Isozyme Specificities of Selected P
Page 41 and 42: Protein Kinase C (PKC) Inhibitors,
Page 47 and 48: Protein Tyrosine Kinase (PTK) Inhib
Page 57 and 58: Raf Kinase Inhibitors Raf kinases a
Page 59 and 60: Rho Kinase (ROCK) Inhibitors, conti
Page 61 and 62: Protein Phosphatase Inhibitors Calb
Page 63 and 64: Protein Phosphatase Inhibitors, con
Page 65 and 66: Apoptosis Caspase Inhibitors Activa
Page 67 and 68:
Caspase Inhibitors, continued Produ
Page 69 and 70:
Other Selected Inhibitors of Apopto
Page 71 and 72:
Calbiochem • Inhibitor SourceBook
Page 73 and 74:
DNA Methyltransferase Inhibitors DN
Page 75 and 76:
Histone Acetylase and Deacetylase I
Page 77 and 78:
Related Products Histone Deacetylas
Page 79 and 80:
Nuclear Import/Export Inhibitors, c
Page 81 and 82:
Page 83 and 84:
Telomerase Inhibitors, continued Ca
Page 85 and 86:
Topoisomerase Related Inhibitors, c
Page 87 and 88:
Lipid Signaling Acetyl-CoA Carboxyl
Page 89 and 90:
Cyclooxygenase (COX) Inhibitors, co
Page 91 and 92:
HMG-CoA (3-Hydroxy-3-Methylglutaryl
Page 93 and 94:
Lipoxygenase (LOX) Inhibitors Lipox
Page 95 and 96:
Phospholipase Inhibitors Several si
Page 97 and 98:
Sphingomyelinase Inhibitors Ceramid
Page 99 and 100:
Amyloidogenesis Inhibitors Calbioch
Page 101 and 102:
Secretase Inhibitors Deposition of
Page 103 and 104:
Secretase Inhibitors Calbiochem •
Page 105 and 106:
Page 107 and 108:
Glutathione S-Transferase (GST) Inh
Page 109 and 110:
Guanylate Cyclase Inhibitors, conti
Page 111 and 112:
Characteristics of various forms of
Page 113 and 114:
Nitric Oxide Synthase (NOS) Inhibit
Page 115 and 116:
Proteases Anthrax Lethal Factor (LF
Page 117 and 118:
the ratio of active (76 kDa) to ina
Page 119 and 120:
Collagenase Inhibitors (Also see Ma
Page 121 and 122:
Matrix Metalloproteinase (MMP) Inhi
Page 123 and 124:
Matrix Metalloproteinase Inhibitors
Page 125 and 126:
Tissue Inhibitors of Matrix Metallo
Page 127 and 128:
Protease Inhibitors The proper func
Page 129 and 130:
Protease Inhibitors, continued Calb
Page 131 and 132:
Protease Inhibitors, continued Calb
Page 133 and 134:
Protease Inhibitors, continued Sele
Page 135 and 136:
Protease Inhibitor Cocktails, conti
Page 137 and 138:
N Animal-Free Protease Inhibitor Co
Page 139 and 140:
Proteasome and Ubiquitination Pathw
Page 141 and 142:
Transmembrane receptors of various
Page 143 and 144:
Angiotensin-Converting Enzyme (ACE)
Page 145 and 146:
ATPase Inhibitors, continued Calbio
Page 147 and 148:
Page 149 and 150:
Inhibitors of Glycoprotein Processi
Page 151 and 152:
Heat Shock Protein Inhibitors Heat
Page 153 and 154:
Inhibitors of Mitochondrial Functio
Page 155 and 156:
NF-kB Activation Inhibitors NF-kB,
Page 157 and 158:
NF-kB Activation Inhibitors, contin
Page 159 and 160:
Phosphodiesterase (PDE) Inhibitors
Page 161 and 162:
Plasminogen Activator Inhibitors Ti
Page 163 and 164:
Protein Synthesis Inhibitors, conti
Page 165 and 166:
Sonic Hedgehog Signaling Inhibitors
Page 167 and 168:
Why can’t I make serial dilutions
Page 169 and 170:
Calpastatin, Human, Recombinant, Do
Page 171 and 172:
InSolution Microcystin-LR, Microcys
Page 173 and 174:
RNA Polymerase III Inhibitor ......
Page 175 and 176:
324875 ............................
Page 177 and 178:
Trademarks CALBIOCHEM®
Page 179 and 180:
Your #1 Resource for Inhibitors! We
show all

Inhibitor SourceBook™ Second Edition

You also want an ePaper? Increase the reach of your titles

Delete template?

Save as template?