in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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116 in vitro pharmacology 2011 catalog ❚ protein-tyrosine kinases [Rtk] PDGFRb kinase Ref. 2900 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant (insect cells) Substrate ATP + Ulight-Poly GAT[EAY(1:1:1)]n (25 nM) Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n Detection method LANCE Reference staurosporine (IC 50 : 1 nM) Baxter, R.M. et al. (1998) J. Biol. Chem., 273: 17050-17055. Ret kinase Ref. 1593 Q 3 weeks Included in: Organ safety profile Comprehensive kinase profile Source human recombinant (insect cells) Substrate ATP + biotinyl-bAbAbAAEEEEYFELVAKKK (100 nM) Measured product phospho-biotinyl-bAbAbAAEEEEYFELVAKKK Detection method HTRF Reference staurosporine (IC 50 : 8 nM) Borrello, M.G. et al. (1996) Mol. Cell. Biol., 16: 2151-2163. -9 -8 -7 -6 -5 -4 enzyme activity (% of control) 100 50 staurosporine SU4312 SU4984 0 PD153035 -10 -9 -8 -7 -6 -5 -4 -11 log [drug] (M) Ron kinase Ref. 3067 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant Substrate ATP + Ulight-TK peptide (20 nM) Measured product phospho-Ulight-TK peptide Detection method LANCE Reference staurosporine (IC 50 : 470 nM) Santoro, M.M. et al. (1998) Oncogene, 17: 741-749. -10 -9 -8 -7 -6 -5 -4 -8 -7 -6 -5 -9 -4 -9 -8 -7 -6 -5 -4 -8 -7 -6 -5 -4 -11 -10 -9 -8 -7 -6 -5 -4 PD153035 staurosporine AG1478 AG825 Ros kinase Ref. 1594 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant (Sf21 cells) Substrate ATP + biotinyl-bAbAbAAAEEEYMMMFAKKK (75 nM) Measured product phospho-biotinyl-bAbAbAAAEEEYMMFAKKK Detection method HTRF Reference staurosporine (IC 50 : 7.6 nM) Birchmeier C. et al. (1990) Proc. Natl. Acad. Sci. USA, 87: 4799-4803. -9 -8 -7 -6 -5 -4 enzyme activity (% of control) 100 50 staurosporine PD153035 0 K252a -9 -8 -7 -6 -5 -4 -10 log [drug] (M) -11 -10 -9 -8 -7 -6 -5 -4 TIE2 kinase Ref. 2736 Q 3 weeks Included in: Organ safety profile Comprehensive kinase profile Source human recombinant Substrate ATP + Ulight-Poly GT [EY(4:1)]n (50 nM) Measured product phospho-Ulight-Poly GT [EY(4:1)]n Detection method LANCE Reference staurosporine (IC 50 : 260 nM) Deng, S-J. et al. (2001) Comb. Chem. High Throughput Screen., 4: 525-533. -10 -9 -8 -7 -6 -5 -4 -9 -8 -7 -6 -5 -4 -4 -9 -8 -7 -6 -5 -8 -7 -6 -5 -4 -11 -10 -9 -8 -7 -6 -5 -4 PD153035 staurosporine AG1478 AG825 TRKA Ref. 2901 Q 3 weeks Included in: ExpresS Diversity kinase profile Organ safety profile Comprehensive kinase profile Source human recombinant (insect cells) Substrate ATP + Ulight-Poly GAT[EAY(1:1:1)]n (5 nM) Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n Detection method LANCE Reference staurosporine (IC 50 : 5.5 nM) Angeles, T.S. et al. (1998) Arch. Biochem. Biophys., 349: 267-274.
117 TRKB Ref. 2902 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant Substrate ATP + Ulight-Poly GAT[EAY(1:1:1)]n (5 nM) Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n Detection method LANCE Reference staurosporine (IC 50 : 3.3 nM) Middlemas, D.S. et al. (1994) J. Biol. Chem., 269: 5458-5466. protein-tyrosine kinases [Rtk] ❚ Cerep services Receptors TRKC Ref. 3080 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant Substrate ATP + Ulight-TK peptide (50 nM) Measured product phospho-Ulight-TK peptide Detection method LANCE Reference staurosporine (IC 50 : 1.7 nM) Robinson, L.L. et al. (2003) J. Clin. Endocrinol. Metab., 88: 3943-3951. Ion channels Transporters Tyro3/Sky kinase Ref. 3081 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant Substrate ATP + Ulight-TK peptide (50 nM) Measured product phospho-Ulight-TK peptide Detection method LANCE Reference staurosporine (IC 50 : 6.1 nM) Lan, Z. et al. (2000) Blood, 95: 633-638. Kinases Epigenetic & DNA-related enzymes VEGFR kinase cellul ar Ref. 2696 Activator effect Ref. 2697 Inhibitor effect Q 3 weeks Source HUV-EC-C cells Measured product impedance Detection method cellular dielectric spectroscopy Activator effect Control VEGF (1 nM) Reference VEGF (EC 50 : 0.029 nM) Inhibitor effect Stimulant VEGF (0.1 nM) Reference VEGF receptor tyrosine kinase inhibitor II (IC 50 : 168 nM) Furet, P. et al. (2003) Bioorg. Med. Chem. Lett., 13: 2967-2971. [Solvent] must be kept 0.1% Other enzymes Specialized cellular assays selected cerep assays ❚ Biochemical kinase assays Kinase assays are enzymatic assays mostly using activated kinases. Those are usually full length kinase or cytoplasmic domain of RTK. Assays are designed to be as close as possible to ATP and substrate Km. The technology used to measure substrate phosphorylation is TR-FRET (HTRF ® or LANCE ® ). A few assays are cascade of activation. ❚ Cellular kinase assays In order to complement our existing biochemical assay platform, we have implemented cellular kinase assays. These assays allow to confirm inhibitors activity in a relevant cellular background and profile their selectivity against multiple signaling pathways. - Cellular kinase phosphorylation assays Cellular kinase phosphorylation assays are developed using AlphaScreen ® Surefire ® assay kits. The assays are optimized for directly measuring kinase activation following treatment of cells with activators of signaling pathways. - Cellular tyrosine kinase receptor activity assays We have demonstrated that the impedance-based technology can be used to monitor the activity of the main tyrosine kinase receptor families. These label-free assays allow the identification of inhibitors targeting either the ligand binding domain or the kinase domain. These assays can be developed in virtually any cancer cell lines or primary cells. As an example, we have developed and validated the EGFR cellular assay in the following cancer cell lines: A431, HELA and MDA-MB-231. ❚ Binding kinase assays See page 107. Standard profiles Testing conditions Ordering information Assay list & index
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in vitro pharmacology 2011 catalog
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Cerep services p. 4 Receptors [GPC
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5 ❚ tool-box for cell-based assay
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7 ❚ profile design Cerep offers a
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9 ❚ data online A powerful web-ba
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11 in vitro pharmacology assays Rec
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13 Cerep services receptors Recept
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15 Adenosine ❚ A 2B - antagonist
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17 alpha 1B - antagonist radioligan
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19 adrenergic ❚ alpha 2C - antago
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adrenergic ❚ 21 beta 3 cellul ar
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-12 -11 -10 -9 -8 -7 -6 -5 -4 -3 bo
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adykinin ❚ 25 B 2 cellul ar Ref.
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27 ❚ cannabinoid CB 1 - agonist r
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29 chemokines ❚ CCR2 cellul ar Re
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31 cholecystokinin ❚ CCK 2 (CCK B
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33 dopamine ❚ D 2S - antagonist r
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dopamine ❚ 35 D 5 cellul ar Ref.
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37 Cerep services ❚ Free fatty ac
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39 galanin ❚ GAL 2 - agonist radi
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41 ❚ Growth hormone-releasing hor
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43 H 3 - agonist radioligand Source
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45 leukotrienes ❚ CysLT 2 (LTC 4
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melanin concentrating hormone ❚
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49 ❚ melatonin Cerep services MT
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51 M 2 - antagonist radioligand bin
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53 muscarinic ❚ M 5 - antagonist
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55 NK 3 - agonist radioligand bindi
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neuropeptide y ❚ 57 Y 1 cellul a
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59 Cerep services ❚ opioid and op
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61 NOP (ORL1) - agonist radioligand
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63 platelet activating factor ❚ P
Page 65 and 66: 65 prostanoid ❚ EP 4 - agonist ra
Page 67 and 68: 67 proteinase-activated ❚ PAR2 ce
Page 69 and 70: serotonin ❚ 69 5-HT 1A cellul ar
Page 71 and 72: 71 serotonin ❚ 5-HT 2B - agonist
Page 73 and 74: 73 5-HT 7 - agonist radioligand bin
Page 75 and 76: 75 ❚ thyrotropin releasing hormon
Page 77 and 78: 77 ❚ vasopressin Cerep services O
Page 79 and 80: 79 Cerep services receptors Recept
Page 81 and 82: 81 LXRb - agonist radioligand bindi
Page 83 and 84: 83 Cerep services receptors Recept
Page 85 and 86: 85 gaba ❚ GABA A1 (a1, b2, g2) -
Page 87 and 88: 87 glycine (strychnine-insensitive)
Page 89 and 90: 89 ❚ Melatonin MT 3 (ML 2 ) - ago
Page 91 and 92: 91 ❚ Sigma Cerep services sigma (
Page 93 and 94: 93 Cerep services [Voltage-gated ch
Page 95 and 96: voltage-gated channels [K + channel
Page 97 and 98: transient receptor potential channe
Page 99 and 100: 99 kainate - agonist radioligand bi
Page 101 and 102: 101 ❚ purinergic channels Cerep s
Page 103 and 104: 103 Cerep services transporters Rec
Page 105 and 106: 105 norepinephrine ❚ norepinephri
Page 107 and 108: 107 Cerep services Kinases Receptor
Page 109 and 110: 109 DDR2 kinase Ref. 2783 Q 3 weeks
Page 111 and 112: 111 protein-tyrosine kinases [Rtk]
Page 113 and 114: 113 FLT-3 kinase Ref. 2866 Q 3 week
Page 115: 115 KDR kinase (VEGFR2) Ref. 2864 Q
Page 119 and 120: 119 protein-tyrosine kinases [Ctk]
Page 121 and 122: 121 JAK1 Ref. 2619 Q 3 weeks Includ
Page 123 and 124: 123 TXK Ref. 2786 Q 3 weeks Include
Page 125 and 126: 125 CDK6 (cycD3) Ref. 2909 Q 3 week
Page 127 and 128: protein-SERINE/THREONINE kinases [C
Page 129 and 130: 129 JNK3 Ref. 2916 Q 3 weeks Includ
Page 131 and 132: 131 CaMK1d Ref. 2922 Q 3 weeks Incl
Page 133 and 134: 133 MAPKAPK2 Ref. 3367 Q 3 weeks I
Page 135 and 136: 135 PhKg1 Ref. 2745 Q 3 weeks Inclu
Page 137 and 138: 137 ❚ protein-SERINE/THREONINE ki
Page 139 and 140: 139 MSK1 Ref. 1724 Q 3 weeks Source
Page 141 and 142: 141 PKCe Ref. 2044 Q 3 weeks PKCz R
Page 143 and 144: 143 ROCK2 Ref. 2884 Q 3 weeks Inclu
Page 145 and 146: 145 COT kinase (MAP3K8) Ref. 2003 Q
Page 147 and 148: 147 MKK6/p38a (mutant active) Ref.
Page 149 and 150: 149 ❚ protein-SERINE/THREONINE ki
Page 151 and 152: 151 RAF-1/MEK1 Ref. 1703 Q 3 weeks
Page 153 and 154: 153 other kinases ❚ MYT1 kinase R
Page 155 and 156: 155 other kinases ❚ TBK1 Ref. 33
Page 157 and 158: 157 Cerep services Epigenetic & DNA
Page 159 and 160: 159 HDACs ❚ HDAC3 Ref. 2083 Q 3 w
Page 161 and 162: 161 HDACs ❚ sirtuin 3 Source Subs
Page 163 and 164: 163 Cerep services Other enzymes Re
Page 165 and 166: 165 phosphatases ❚ phosphatase LA
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167 phosphatase SHP2 (PTPN11) Sourc
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169 caspase-3 ❚ Cysteine protease
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171 proteases [aspartic proteases]
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173 proteases [metalloproteases]
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phosphodiesterases ❚ 175 PDE4A 1
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177 no synthases ❚ inducible NOS
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179 ❚ Monoamine & neurotransmitte
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181 Cerep services ❚ Transduction
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183 miscellaneous enzymes ❚ carbo
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185 Specialized cellular assays The
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187 ion transport systems ❚ Na +
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189 cytokine secretion ❚ IL-2 sec
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191 expression of endothelial adhes
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193 PDGF-stimulated Balb/c 3T3 prol
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195 cerep Standard profiles ExpresS
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197 ❚ Cellular functional GPCR pr
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Cerep standard profiles ❚ 199 Dr
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Cerep standard profiles ❚ 201 Sa
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203 testing conditions Binding, enz
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205 The reference compound for each
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207 ordering information Quotation
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209 REQUESTED COMPOUND INFORMATION
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shipment instructions ❚ 211 For
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213 assay list & index
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215 CDK5/p35 124 CDK6 (cycD3) 125 C
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217 MMP-3 172 MMP-7 172 MMP-8 172 M
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contacts ❚ france [Laboratories]
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