in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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126 in vitro pharmacology 2011 catalog ❚ protein-SERINE/THREONINE kinases [CMGC] CLK2 Source human recombinant (insect cells) Substrate ATP + biotinyl-βAβAβAAGAGKRREILSRRPS YRK (10 nM) Measured product phospho-biotinyl-βAβAβAAGAGKRREILSRR Ref. 2019 PSYRK Detection method HTRF Q 3 weeks Reference Ro-318220 (IC Included in: 50 : 75 nM) Comprehensive kinase profile Nayler, O. et al. (1998) J. Biol. Chem., 273: 34341-34348. enzyme activity (% of control) 100 50 0 Ro-318220 staurosporine K252a H-89 -10 -9 -8 -7 -6 -5 -4 -3 log [drug] (M) DYRK1a Ref. 2781 Q 3 weeks Included in: Organ safety profile Comprehensive kinase profile Source human recombinant Substrate ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide (100 nM) Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide Detection method LANCE Reference staurosporine (IC 50 : 16 nM) Himpel, S. et al. (2000) J. Biol. Chem., 275: 2431-2438. -12 -11 -10 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -6 -10 -7 -9 -8 -6 -5 -4 -11 -10 -6 -5 -12 -9 -8 -7 DYRK2 Ref. 2788 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant Substrate ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide (100 nM) Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide Detection method LANCE Reference staurosporine (IC 50 : 1100 nM) Taira, N. et al. (2007) Mol. Cell., 25: 725-738. DYRK3 Ref. 1963 Q 3 weeks Source human recombinant (insect cells) Substrate ATP + biotinyl-MBP (40 nM) Measured product phospho-biotinyl-MBP Detection method HTRF Reference staurosporine (IC 50 : 37 nM) Li, K. et al. (2002) J. Biol. Chem., 277: 47052-47060. enzyme activity (% of control) 100 50 staurosporine Ro-318220 K252a 0 H-89 -8 -7 -6 -4 -9 -5 log [drug] (M) DYRK4 Ref. 1962 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant (insect cells) Substrate ATP + biotinyl-MBP (80 nM) Measured product phospho-biotinyl-MBP Detection method HTRF Reference hymenialdisine (IC 50 : 149 nM) Li, K. et al. (2002) J. Biol. Chem., 277: 47052-47060. enzyme activity (% of control) -10 -9 -8 -7 -6 -5 -4 100 -9 -8 -7 -6 -5 -4 50 0 -10 -9 -5 -8 -7 -6 -4 log [drug] (M) hymenialdisine staurosporine Bis 10 EGCG ❚ Assays converted from HTRF ® to LANCEUltra ® technology A majority of our kinase assays have been converted from HTRF ® to LANCEUltra ® technology. Both technologies are TR-FRET with the difference in europium labelling: europium cryptate for HTRF ® and europium chelate for LANCEUltra ® . Assays are converted following a standard procedure consisting of time course experiment, Km determination and pharmacology characterization of the enzyme by inhibiting its activity with known inhibitors. IC 50 values obtained for known inhibitors are compared to literature and to those obtained using HTRF ® technology. If all values are in agreement with the previous ones, LANCE ® technology is validated for the kinase of interest. This conversion allows us to standardize and automate our kinase assays providing shorter turnaround times for both profiling and screening experiments.
protein-SERINE/THREONINE kinases [CMGC] ❚ 127 ERK 1 Ref. 2914 Q 3 weeks Included in: Organ safety profile Comprehensive kinase profile Source human recombinant (E.coli) Substrate ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide (50 nM) Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide Detection method LANCE Reference staurosporine (IC 50 : 1.3 µM) Yung, Y. et al. (2001) J. Biol. Chem., 276: 35280-35289. Cerep services Receptors ERK 2 (P42 mapk ) Ref. 2878 Q 3 weeks Included in: ExpresS Diversity kinase profile BioPrint ® profile Organ safety profile Comprehensive kinase profile Source human recombinant (E.coli) Substrate ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide (100 nM) Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide Detection method LANCE Reference staurosporine (IC 50 : 539 nM) Bardwell, A.J. et al. (2003) Biochem. J., 370: 1077-1085. Ion channels Transporters ERK 1/2 cellul ar Ref. 3101 Ref. 3106 Q 3 weeks Activator effect Inhibitor effect Source Measured product Detection method A431 cells phosphorylation AlphaScreen Activator effect Control EGF (10 nM) Reference EGF (EC 50 : 0.098 nM) Inhibitor effect Stimulant EGF (0.1 nM) Reference AG1478 (IC 50 : 39 nM) Zhang, Y.G. et al.(2008) Int. J. Oncol., 33: 595-602. [Solvent] must be kept 0.1% Kinases Epigenetic & DNA-related enzymes ERK 5 (MAPK7) Ref. 2680 Q 3 weeks Included in: Comprehensive kinase profile GSK3a Ref. 2842 Q 3 weeks Included in: Comprehensive kinase profile GSK3b Ref. 2879 Q 3 weeks Included in: ExpresS Diversity kinase profile Organ safety profile Comprehensive kinase profile Source human recombinant Substrate ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide (100 nM) Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide Detection method LANCE Reference Ro-318220 (IC 50 : 40 nM) Mody, N. et al. (2003) Biochem. J., 372: 567-575. Source human recombinant Substrate ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide (100 nM) Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide Detection method LANCE Reference staurosporine (IC 50 : 28 nM) Meijer, L. et al. (2003) Chem. Biol., 10: 1255-1266. Source human recombinant Substrate ATP + Ulight-CFFKNIVTPRTPPPSQGK-amide (100 nM) Measured product phospho-Ulight-CFFKNIVTPRTPPPSQGKamide Detection method LANCE Reference staurosporine (IC 50 : 50 nM) Meijer, L. et al. (2003) Chem. Biol., 10: 1255-1266. Other enzymes Specialized cellular assays 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
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65 prostanoid ❚ EP 4 - agonist ra
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67 proteinase-activated ❚ PAR2 ce
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serotonin ❚ 69 5-HT 1A cellul ar
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71 serotonin ❚ 5-HT 2B - agonist
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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 and 116: 115 KDR kinase (VEGFR2) Ref. 2864 Q
Page 117 and 118: 117 TRKB Ref. 2902 Q 3 weeks Includ
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: 125 CDK6 (cycD3) Ref. 2909 Q 3 week
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
Page 167 and 168: 167 phosphatase SHP2 (PTPN11) Sourc
Page 169 and 170: 169 caspase-3 ❚ Cysteine protease
Page 171 and 172: 171 proteases [aspartic proteases]
Page 173 and 174: 173 proteases [metalloproteases]
Page 175 and 176: 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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in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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