in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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146 in vitro pharmacology 2011 catalog ❚ protein-SERINE/THREONINE kinases [STE] MEKK3 (MAP3K3) Ref. 2760 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG (25 nM) Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL AGCG Detection method LANCE Reference staurosporine (IC 50 : 6.2 nM) Samanta, A.K. et al. (2004) J. Biol. Chem., 279: 7576-7583. MEKK4 (MAP3K4) Ref. 2759 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG (25 nM) Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL AGCG Detection method LANCE Reference staurosporine (IC 50 : 110 nM) Chi, H. et al. (2005) Proc. Natl. Acad. Sci. USA, 102: 3846-3851. MINK Ref. 2113 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant (insect cells) Substrate ATP + biotinyl-bAbAbAAAARARTSSFAEPG (200 nM) Measured product phospho-biotinyl-bAbAbAAAARARTSSFAEPG Detection method HTRF Reference Bis 10 (IC 50 : 27 nM) Nicke, B. et al. (2005) Mol. Cell., 20: 673-685. enzyme activity (% of control) 100 50 0 Bis 10 staurosporine H-89 SB202190 -8 -7 -5 -4 -10 -9 -6 log [drug] (M) MKK4/JNK1 Ref. 1927 Q 3 weeks Included in: Organ safety profile Source mouse recombinant (E. coli) Substrate ATP + inactive JNK1 (0.19 µg/ml) Measured product phospho-ATF-2 Detection method HTRF Reference staurosporine (IC 50 : 36 nM) Han, J. et al. (1996) J. Biol. Chem., 271: 2886-2891. -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -10 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -6 -10 -7 -9 -8 -6 -5 -4 -12 -11 -10 -7 -6 -5 -9 -8 MKK4/JNK2 Ref. 1953 Q 3 weeks Source mouse recombinant Substrate ATP + inactive JNK2 (MAPK9) (0.05 µg/mL) Measured product phospho-ATF-2 Detection method HTRF Reference staurosporine (IC 50 : 41 nM) Han, J. et al. (1996) J. Biol. Chem., 271: 2886-2891. enzyme activity (% of control) 100 50 staurosporine SP600125 0 SB202190 -9 -8 -7 -6 -5 -4 log [drug] (M) MKK6 Ref. 2931 Q 3 weeks Included in: ExpresS Diversity kinase profile Comprehensive kinase profile Source human recombinant Substrate ATP + inactive p38a (50 nM) Measured product phospho-p38a Detection method LANCE Reference -11 -10 -9 -8 -7 -6 -5 -4 -10 staurosporine (IC 50 : 11 nM) Han, J. et al. (1996) J. Biol. Chem., 271: 2886-2891. -9 -8 -7 -6 -5 -4 -3 -10 -9 -8 -7 -6 -5 -4 -8 -7 -6 -5 -4 -10 -9 -8 -7 -6 -5 -10 -9 -8 -7 -6 -5 -4 -3
147 MKK6/p38a (mutant active) Ref. 1679 Q 3 weeks Source human recombinant Substrate ATP + inactive p38a (0.75 nM) Measured product phospho-ATF-2 Detection method HTRF Reference staurosporine (IC 50 : 29 nM) Han, J. et al. (1996) J. Biol. Chem., 271: 2886-2891. protein-SERINE/THREONINE kinases [STE] ❚ enzyme activity (% of control) 100 50 0 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) staurosporine SP600125 U0126 SB202190 Cerep services Receptors MST1 kinase (STK4) Ref. 2585 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant (Sf9 cells) Substrate ATP + Ulight-FLGFTYVAP (200 nM) Measured product phospho-Ulight-FLGFTYVAP Detection method LANCE Reference staurosporine (IC 50 : 14.5 nM) Ura, S. et al. (2001) Proc. Natl. Acad. Sci. USA, 98: 10148-10153. Ion channels Transporters MST2 kinase Ref. 2761 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG (100 nM) Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL AGCG Detection method LANCE Reference staurosporine (IC 50 : 13 nM) Lee, K.K. et al. (2001) J. Biol. Chem., 276: 19276-19285. Kinases Epigenetic & DNA-related enzymes MST3 kinase Ref. 2748 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant Substrate ATP + CREBtide (CKRREILSRRPSYRK) (25 nM) Measured product phospho-CREBtide (CKRREILSRRPSYRK) Detection method LANCE Reference staurosporine (IC 50 : 5 nM) Huang, C.Y. et al. (2002) J. Biol. Chem., 277: 34367-34374. Other enzymes Specialized cellular assays MST4 kinase Ref. 3366 Q 3 weeks Included in: ExpresS Diversity kinase profile Comprehensive kinase profile Source Substrate human recombinant ATP + Ulight-PKC (50 nM) Measured product phospho-Ulight-PKC Detection method LANCE Reference staurosporine (IC 50 : 5.7 nM) Qian, Z. et al. (2001) J. Biol. Chem., 276: 22439-22445. Standard profiles Testing conditions NIK Ref. 2325 Q 3 weeks Included in: Comprehensive kinase profile Source human recombinant (Sf9 cells) Substrate ATP + biotinyl-βAβAβAAGAGKRREILSRRPSYRK (30 nM) Measured product phospho-biotinyl-βAβAβAAGAGKRREILSRRPS YRK Detection method HTRF Reference Ro-318220 (IC 50 : 120 nM) Park, G.Y. et al. (2006) J. Biol. Chem., 281: 18684-18690. 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
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75 ❚ thyrotropin releasing hormon
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77 ❚ vasopressin Cerep services O
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81 LXRb - agonist radioligand bindi
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85 gaba ❚ GABA A1 (a1, b2, g2) -
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87 glycine (strychnine-insensitive)
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89 ❚ Melatonin MT 3 (ML 2 ) - ago
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91 ❚ Sigma Cerep services sigma (
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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 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: 145 COT kinase (MAP3K8) Ref. 2003 Q
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
Page 177 and 178: 177 no synthases ❚ inducible NOS
Page 179 and 180: 179 ❚ Monoamine & neurotransmitte
Page 181 and 182: 181 Cerep services ❚ Transduction
Page 183 and 184: 183 miscellaneous enzymes ❚ carbo
Page 185 and 186: 185 Specialized cellular assays The
Page 187 and 188: 187 ion transport systems ❚ Na +
Page 189 and 190: 189 cytokine secretion ❚ IL-2 sec
Page 191 and 192: 191 expression of endothelial adhes
Page 193 and 194: 193 PDGF-stimulated Balb/c 3T3 prol
Page 195 and 196: 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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