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Luceome Factsheet KinaseSeekerTM Luceome Biotechnologies Kinase Profiling Service 1665 E. 18th St, Suite 106 Tucson, Arizona 85719 Ph: (520) 495-0161 www.luceome.com Luceome Biotechnologies provides a split luciferase based high throughput assay for profiling of small Features & Benets molecules against a panel of kinases at cellular ATP 409 kinases - Choose from preset concentrations, enabling discovery of effective and kinase panels or build your own safer pharmaceuticals. Our KinaseSeeker Profiling panel Service now includes full-length kinases, enabling Full-Length Kinases: Evaluate discovery of conformation and activation state impact of kinase conformation senstive kinase inhibtors. The use of full-length and activation state on kinase constructs also allows identification of compound inhibition allosteric inhibitors that bind the PIF-pocket (PDK1), PH domain (AKTs), SH domains (SFKs), etc. Binding Assay: Identify active site directed and allosteric KinaseSeekerTM Technology inhibitors Luminescence detection: Low KinaseSeeker is a homogeneous binding assay false positives from uorescent where the displacement of an active site dependent compounds probe by the drug candidate is measured by a Fast: 10-12 day turnaround time change in luminescence signal. Luminescence readout translates into a highly sensitive and robust Economical: Contact us for assay with low background and minimal pricing ([email protected]) interference from test compounds. ASSAY PRINCIPLE: Cell-free Complex Driven Kinase Activity Inhibited Protein Expression Light Production - Disassembled Luciferase Inhibitor Probe Scaold Protein Kinase HO S S O S S N N OH N N O + ATP + O2 O + LIGHT J. Am. Chem. Soc. 2010, 132, 11727 - 11735 LUCEOME 1 Biotechnologies c Luceome Biotechnologies, LLC. All Rights Reserved. KinaseSeekerTM Luceome Biotechnologies Kinase Profiling Service 1665 E. 18th St, Suite 106 Tucson, Arizona 85719 Ph: (520) 495-0161 www.luceome.com Available Screening Options: (i) Inhibition at single inhibitor dose (ii) Dose response titrations - (IC 50 ) determination (iii) Compound library screening (iv) Custom assay development Selectivity Proling Library Screening IC50 Determination 1.2 PKC-412 H 1.0 N O AKT1 100 0.8 ALU 80 e 0.6 N v N i O 60 t a H l PKA 40 e 0.4 AKT1 A R O B PIM1 % Inhibition 20 N C 0.2 O D 0 E 1 2 3 F 0.0 4 4 5 6 5 6 G 1 10 100 1000 10 10 10 7 8 H 9 10 [PKC-412] (nM) Ghosh et al., J. Am. Chem. Soc. 2010, 132, 11727-11735 Ghosh et al., J. Med. Chem. 2012, 55, 1526-1537 Available Panels: (i) Full-Length Kinase Panel (112 wild-type full-length kinases distributed across kinome) (ii) Tyrosine Kinase Panel (126 wild-type kinase-domain and full-length tyrosine kinases) (iii) Mixed panel (50 select kinases distributed across kinome) (iv) Plasmodium falciparum Panel (9 Plasmodium falciparum kinases) (v) Complete panel of 409 kinases (vi) A la Carte: Pick kinases of your choice and build your own panel Contact: Reena Zutshi, Ph.D. Ph: (520) 495-0161 [email protected] LUCEOME 2 Biotechnologies c Luceome Biotechnologies, LLC. All Rights Reserved. KinaseSeeker™ Complete Panel (409 Kinases) Kinase Group Kinase Group AAK1 Other ACVR1B TKL ABL1 TK ACVR2A TKL ABL1 full-length TK ACVR2B TKL ABL1 (E255K) TK AKT1 AGC ABL1 (E255V) TK AKT1 full-length AGC ABL1 (F317I) TK AKT2 AGC ABL1 (F317L) TK AKT2 full-length AGC ABL1 (F359V) TK AKT2 (S474A) AGC ABL1 (G250E) TK AKT2 (S474D) AGC ABL1 (H396P) TK AKT2 (T309A, S474A) AGC ABL1 (H396R) TK AKT2 (T309D, S474D) AGC ABL1 (L248R) TK AKT3 AGC ABL1 (L248V) TK AKT3 full-length AGC ABL1 (L387M) TK ALK TK ABL1 (M351T) TK AMPK CAMK ABL1 (Q252H) TK AMPK2 CAMK ABL1 (Q252R) TK AMPKa1 full-length CAMK ABL1 (T315F) TK AURKA Other ABL1 (T315I) TK AURKB Other ABL1 (T315N) TK AURKC Other ABL1 (Y253F) TK AXL TK ABL1 (Y253H) TK BIKE Other ABL2 TK BLK TK ACVR1 TKL BLK full-length TK ACVR1 intracellular module TKL BMX TK Legend: Full-Length: Construct contains Full-length kinase Intracellular Module: Construct contains Cytoplasmic Region in Receptor Tyrosine Kinases Page 1 of 9 KinaseSeeker™ Complete Panel (409 Kinases) Kinase Group Kinase Group BRAF TKL CASK full-length CAMK BRAF (T599E, S602D) TKL CDK1 CMGC BRAF (T599E, V600E, S602D) TKL CDK19 CMGC BRAF (V600E) TKL CDK2 - Cyclin E1 CMGC BRSK2 CAMK CDK3 CMGC BTK TK CDK4 CMGC BTK full-length TK CDK5 CMGC CAMK1 CAMK CDK6 CMGC CAMK1D CAMK CDK7 CMGC CAMK1D full-length CAMK CDK8 CMGC CAMK1G CAMK CDK9 CMGC CAMK1G full-length CAMK CDKL2 CMGC CAMK2A CAMK CDKL3 CMGC CAMK2A full-length CAMK CDKL5 CMGC CAMK2B CAMK CDKL5 full-length CMGC CAMK2B full-length CAMK CHK1 CAMK CAMK2D CAMK CHK2 CAMK CAMK2D full-length CAMK CK1d CK1 CAMK2G CAMK CK1d full-length CK1 CAMK2G full-length CAMK CK2a2 Other CAMKK1 Other CLK1 CMGC CAMKK1 full-length Other CLK1 full-length CMGC CAMKK2 Other CLK2 CMGC CAMKK2 full-length Other CLK2 full-length CMGC CASK CAMK CLK3 CMGC Legend: Full-Length: Construct contains Full-length kinase Intracellular Module: Construct contains Cytoplasmic Region in Receptor Tyrosine Kinases Page 2 of 9 KinaseSeeker™ Complete Panel (409 Kinases) Kinase Group Kinase Group CLK3 full-length CMGC EGFR del L747-P753 Ins S TK CSF1R TK EPHA1 TK CSF1R intracellular module TK EPHA1 intracellular module TK CSK TK EPHA2 TK CSK full-length TK EPHA2 intracellular module TK DAPK1 CAMK EPHA3 TK DAPK1 full-length CAMK EPHA3 intracellular module TK DAPK2 CAMK EPHA4 TK DAPK3 CAMK EPHA4 intracellular module TK DCLK2 CAMK EPHA5 TK DDR1 TK EPHA5 intracellular module TK DDR1 intracellular module TK EPHA6 TK DDR2 TK EPHA6 intracellular module TK DDR2 intracellular module TK EPHA7 TK DMPK AGC EPHA7 intracellular module TK DRAK1 CAMK EPHA8 TK DRAK2 CAMK EPHA8 intracellular module TK DYRK1A CMGC EPHB2 TK EGFR TK EPHB3 TK EGFR intracellular module TK EPHB3 intracellular module TK EGFR (G719C) TK EPHB4 TK EGFR (G719S) TK EPHB4 intracellular module TK EGFR (L858R) TK EPHB6 TK EGFR (L858R) intracellular module TK ERBB2 TK EGFR (L861Q) TK ERBB2 intracellular module TK Legend: Full-Length: Construct contains Full-length kinase Intracellular Module: Construct contains Cytoplasmic Region in Receptor Tyrosine Kinases Page 3 of 9 KinaseSeeker™ Complete Panel (409 Kinases) Kinase Group Kinase Group ERBB3 TK FLT3 (R834Q) TK ERBB4 intracellular module TK FLT4 TK ERK5 CMGC FLT4 intracellular module TK FAK TK FRK TK FAK full-length TK FRK full-length TK FER TK FYN TK FES TK FYN full-length TK FGFR2 TK GCN2 STE FGFR2 intracellular module TK GRK7 AGC FGFR3 TK GRK7 full-length AGC FGFR3 intracellular module TK GSK3A CMGC FGFR3 (G697C) TK GSK3A full-length CMGC FGFR4 TK GSK3B CMGC FGR TK HCK TK FGR full-length TK HCK full-length isoform1 TK FLT1 TK HCK full-length isoform2 TK FLT1 intracellular module TK HIPK4 CMGC FLT2 TK HIPK4 full-length CMGC FLT2 intracellular module TK IGF1R TK FLT3 TK IGF1R intracellular module TK FLT3 (D835H) TK IKKe Other FLT3 (D835Y) TK IKKe full-length Other FLT3 (ITD) TK INSR TK FLT3 (K663Q) TK INSR intracellular module TK FLT3 (N841I) TK INSRR TK Legend: Full-Length: Construct contains Full-length kinase Intracellular Module: Construct contains Cytoplasmic Region in Receptor Tyrosine Kinases Page 4 of 9 KinaseSeeker™ Complete Panel (409 Kinases) Kinase Group Kinase Group IRAK3 TKL MAP3K10 TKL IRAK3 full-length TKL MAP3K11 TKL ITK TK MAP3K2 STE JAK2 TK MAP3K9 TKL JAK3 TK MAP4K1 STE KIT TK MAP4K2 STE KIT intracellular module TK MAP4K2 full-length STE KIT (A829P) intracellular module TK MAP4K3 STE KIT (D816H) intracellular module TK MAP4K5 STE KIT (D816V) intracellular module TK MAP4K5 full-length STE KIT (D820E) intracellular module TK MAP4K6 STE KIT (D820Y) intracellular module TK MAPK11 CMGC KIT (L576P) intracellular module TK MAPK12 CMGC KIT (N822K) intracellular module TK MAPK13 CMGC KIT (T670E) intracellular module TK MAPK14 CMGC KIT (T670I) intracellular module TK MAPK9 full-length CMGC KIT (V559D) intracellular module TK MARK1 CAMK KIT (V654A) intracellular module TK MARK1 full-length CAMK KIT (Y823D) intracellular module TK MARK2 CAMK LCK TK MARK2 full-length CAMK LCK full-length TK MARK3 CAMK LIMK1 TKL MARK4 CAMK LYN TK MELK CAMK LYN full-length TK MET TK MAK CMGC MET intracellular module TK Legend: Full-Length: Construct contains Full-length kinase Intracellular Module: Construct contains Cytoplasmic Region in Receptor Tyrosine Kinases Page 5 of 9 KinaseSeeker™ Complete Panel (409 Kinases) Kinase Group Kinase Group MET (M1250T) TK NTRK1 TK MET (Y1235D) TK NTRK2 TK MKNK2 CAMK NTRK2 intracellular module TK MSK1 AGC NTRK3 TK MSK1 full-length AGC NTRK3 intracellular module TK MSK2 AGC NUAK1 CAMK MSK2 full-length AGC NUAK1 full-length CAMK MST1 STE PAK1 STE MST1 full-length STE PAK1 (T423A) STE MST1R/RON TK PAK1 (T423E) STE MST2/STK3 STE PAK4 STE MST2/STK3 full-length STE PAK7 STE MST3 STE PCTK1 CMGC MST3 full-length STE PCTK2 CMGC MUSK TK PDGFRA TK MUSK intracellular module TK PDGFRA intracellular module TK MYLK CAMK PDGFRA (D842V) TK MYLK2 CAMK PDGFRA (D846Y) TK MYLK2 full-length CAMK PDGFRA (T674I) TK MYLK4 CAMK PDGFRB TK MYLK4 full-length CAMK PDGFRB intracellular module TK MYT1 Other PDK1 AGC MYT1 full-length Other PDK1 full-length AGC NEK5 Other PfARK1 P. falciparum NEK9 Other PfCDPK2 P. falciparum Legend: Full-Length: Construct contains Full-length kinase Intracellular Module: Construct contains Cytoplasmic Region in Receptor Tyrosine Kinases Page 6 of 9 KinaseSeeker™ Complete Panel (409 Kinases) Kinase Group Kinase Group PfCDPK5 P. falciparum PKG1 full-length AGC PfGSK3 P. falciparum PKG2 AGC PfNEK1 P. falciparum PKN3 AGC PfNEK3 P. falciparum PKX1 AGC PfPK5 P. falciparum PLK1 Other PfPK6
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