IMAP® Substrate Finder Kits from Molecular Devices

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ItemIMAP® Substrate Finder Kits
CompanyMolecular Devices
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Molecular Devices

3860 N First Street

San Jose, California 95134

United States

Phone: 408-747-1700

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Website: www.moleculardevices.com

(1) Application and Cross-Validation of a High-Throughput SPR Method for Characterizing Covalent Binding LigandsACS OmegaJuly 15, 2025Wei Zhou, Xuecheng Ye, Suraj Pandey, Xinlin DuMetal Ion Affinity-Based Fluorescence Polarization (IMAP FP) Binding Assay for MK2 Inhibitors The IMAP Fluorescence Polarization (FP) Screening Express Kit with a Progressive Binding System (Molecular Devices)

(2) Interleukin‐1 receptor‐associated kinase 4 (IRAK4) is a critical regulator of inflammatory signalling through toll‐like receptors 4 and 7/8 in murine and human lungsBritish Journal of PharmacologyNovember 1, 2024Ian Sayers, Dhruma Thakker, Charlotte Billington, Stefan Kreideweiss, Marc A. Grundl, Thierry Bouyssou, Sven Thamm, Sebastian Kreuz, Ian P. Halland purified by affinity chromatography. In vitro inhibition of IRAK4 activity was measured using the IMAP Fluorescence Polarization Technology (Molecular Devices). Briefly, BI1543673 was dissolved in DMSO and

(3) A Novel PDE10A Inhibitor for Tourette Syndrome and Other Movement DisordersCellsJuly 22, 2024Randall D. Marshall, Frank S. Menniti, Mark A. TepperGL (GE Healthcare). The inhibition of PDE10A by EM-221, MP-10, and TAK-063 was determined using the IMAP TR-FRET Screening Express system (Molecular Devices). The assay was performed in a 384-well white plate

(4) Dual TTK/PLK1 inhibition has potent anticancer activity in TNBC as monotherapy and in combinationFrontiers in oncologyJanuary 1, 2024Zanini E, Forster-Gross N, Bachmann F, Brüngger A, McSheehy P, Litherland K, Burger K, Groner AC, Roceri M, Bury L, et al.full-length TTK enzyme activity was determined using an Immobilized Metal Assay for Phosphochemicals (IMAP®) assay (Molecular Devices). Inhibition of full-length PLK1 enzyme activity was determined using LANCE

(5) Comparative biochemical kinase activity analysis identifies rivoceranib as a highly selective VEGFR2 inhibitorCancer Chemotherapy and PharmacologyJune 1, 2023Seong Jang, Bill Strickland, Lynda Finis, Jeffrey J. Kooijman, Janneke J. T. M. Melis, Guido J. R. Zaman, Jan Van Tornoutsingle well of a polystyrene 384-well black microplate. After incubating for 1 h at room temperature, IMAP-binding reagent (IMAP Screening Express kit; Molecular Devices) was added to the well and incubated

(6) Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of SchizophreniaJournal of medicinal chemistryJanuary 26, 2023Layton ME, Kern JC, Hartingh TJ, Shipe WD, Raheem I, Kandebo M, Hayes RP, Huszar S, Eddins D, Ma B, et al.Materials and Methods PDE Biochemical Assays Phosphodiesterase (PDE) activity was determined using an IMAP FP kit (Molecular Devices, Sunnyvale, CA) as previously described (Huang et al., 2002). Human PDE10A2

(7) Novel Non-Cyclooxygenase Inhibitory Derivative of Sulindac Inhibits Breast Cancer Cell Growth In Vitro and Reduces Mammary Tumorigenesis in RatsCancers (Basel)January 20, 2023Heather N. Tinsley, Bini Mathew, Xi Chen, Yulia Y. Maxuitenko, Nan Li, Whitney M. Lowe, Jason D. Whitt, Wei Zhang, Bernard D. Gary, Adam B. Keeton, et al.measuring absorbance at 590 nm. PDE activity was measured using the Molecular Devices (San Diego, CA, USA) IMAP fluorescence polarization assay as previously described [15]. Recombinant PDE5 was purchased from BPS

(8) Identification and development of a subtype-selective allosteric AKT inhibitor suitable for clinical developmentScientific reportsSeptember 20, 2022Page N, Wappett M, O'Dowd CR, O'Rourke M, Gavory G, Zhang L, Rountree JSS, Jordan L, Barker O, Gibson H, et al.respectively as per activity assay protocol. ALM301 was profiled using the Fluorescent Polarisation (FP) iMAP Screening Express kit (Molecular Devices) using the FAM-Crosstide substrate [5FAM-GRPRTSSFAEG-OH] (Molecular

(9) Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain InhibitorJournal of Medicinal ChemistryMay 12, 2022Duncan C. Miller et al.Protocol Preparation of Assay Buffer (1×) The 0.01% Tween-20 5× stock was supplied as part of the IMAP FP progressive binding system kit (Molecular Devices R7436) and was diluted to 1× using Milli-Q H2O.

(10) Characterization of Competitive Inhibitors of Plasmodium falciparum cGMP‐Dependent Protein Kinase**ChemBioChemApril 5, 2022Tyler Eck, Mariana Laureano Laureano de Souza, Melvin Delvillar, Kutub Ashraf, Rammohan R. Yadav Yadav Bheemanaboina, Ramappa Chakrasali, Tamara Kreiss, John J. Siekierka, David P. Rotella, Purnima Bhanot, et al.calculate Km and Ki. To our knowledge, this is the first reported modification of the simple ‘mix and read’ IMAP assay, developed by Molecular Devices, for use in kinetic measurements. Using the kinetic IMAP assay,

(11) Reduced nitric oxide bioavailability impairs myocardial oxygen balance during exercise in swine with multiple risk factorsBasic Research in CardiologyDecember 1, 2021Jens van de Wouw, Oana Sorop, Ruben W. A. van Drie, Jaap A. Joles, A. H. Jan Danser, Marianne C. Verhaar, Daphne Merkus, Dirk J. DunckerUSA). Overall phosphodiesterase and phosphodiesterase 5 activity in the myocardium was measured using a IMAP assay (PDE(5) IMAP FP PDE evaluation kit, Molecular Devices, San José, CA, USA). Data analysis and

(12) Suppression of Colon Tumorigenesis in Mutant Apc Mice by a Novel PDE10 Inhibitor that Reduces Oncogenic β-CateninCancer prevention research (Philadelphia, Pa.)November 1, 2021Lee KJ, Chang WL, Chen X, Valiyaveettil J, Ramirez-Alcantara V, Gavin E, Musiyenko A, Madeira da Silva L, Annamdevula NS, Leavesley SJ, et al.Assays PDE assays were performed using recombinant PDE isozymes (BPS Bioscience) in conjunction with the IMAP FP Screening Express Kit (Molecular Devices Inc,), as described previously (27). To determine enzyme

(13) A Novel Selective PKR Inhibitor Restores Cognitive Deficits and Neurodegeneration in Alzheimer Disease Experimental ModelsJournal of Pharmacology and Experimental TherapeuticsSeptember 1, 2021Matilde Lopez-Grancha et al.cosubstrates (ATP, ds poly IC) in the absence of inhibitor compound. Activity on Cdk9 was measured by binding (IMAP technology, Molecular Devices) revealed by fluorescent polarization. 8 Downloaded from jpet.aspetjournals.org

(14) Discovery of trisubstituted pyrazolines as a novel scaffold for the development of selective phosphodiesterase 5 inhibitorsBioorganic ChemistryNovember 1, 2020Mohammad Abdel-Halim, Heather Tinsley, Adam B. Keeton, Mohammed Weam, Noha H. Atta, Mennatallah A. Hammam, Amr Hefnawy, Rolf W. Hartmann, Matthias Engel, Gary A. Piazza, et al.of the substrate at a wavelength of 590 nm. 4.2.2. PDE assay PDE activity was measured using the IMAP fluorescence polarization assay (Molecular Devices Inc.) according to the manufacturer’s specifications.

(15) Anti-Inflammatory Effects of the Novel PIM Kinase Inhibitor KMU-470 in RAW 264.7 Cells through the TLR4-NF-κB-NLRP3 PathwayInternational journal of molecular sciencesJuly 20, 2020Baek HS, Min HJ, Hong VS, Kwon TK, Park JW, Lee J, Kim S.(Carlsbad, CA, USA), Abcam (Cambridge, UK), and Millipore (Burlington, MA, USA), respectively. The IMAP™ FP Screening Express Kit was obtained from Molecular Devices (San Jose, CA, USA). The 5-FAM-labelled

(16) Increased lysosomal biomass is responsible for the resistance of triple-negative breast cancers to CDK4/6 inhibitionScience advancesJune 1, 2020Fassl A, Brain C, Abu-Remaileh M, Stukan I, Butter D, Stepien P, Feit AS, Bergholz J, Michowski W, Otto T, et al.and human CDK2/cyclin A (catalog nos. 14-450 and 14-448, respectively, Millipore) was monitored using IMAP-FP assays (Molecular Devices, CA) by following the phosphorylation of Tamra-Histone H1-derived peptide

(17) Identification of a Selective PDE4B Inhibitor From Bryophyllum pinnatum by Target Fishing Study and In Vitro Evaluation of Quercetin 3-O-α-L-Arabinopyranosyl-(1→2)-O-α-L-RhamnopyranosideFrontiers in PharmacologyJanuary 22, 2020Estela M. G. Lourenço, Júlia M. Fernandes, Vinícius de F. Carvalho, Raphael Grougnet, Marco A. Martins, Alessandro K. Jordão, Silvana M. Zucolotto, Euzébio G. Barbosathis work. PDE4 Activity In Vitro Evaluation Human PDE4A and PDE4B activities were measured using an IMAP TR-FRET protocol (kit from Molecular Devices, Sunnyvale, CA, USA) according to the instructions of the

(18) A Novel Phosphodiesterase 1 Inhibitor DSR-141562 Exhibits Efficacies in Animal Models for Positive, Negative, and Cognitive Symptoms Associated with SchizophreniaThe Journal of pharmacology and experimental therapeuticsDecember 1, 2019Enomoto T, Tatara A, Goda M, Nishizato Y, Nishigori K, Kitamura A, Kamada M, Taga S, Hashimoto T, Ikeda K, et al.PDE4 catalytic domain, PDE5 catalytic domain, PDE7A, PDE8A, PDE9A, PDE10A, and PDE11A were used for IMAP FP assays (Molecular Devices, Sunnyvale, CA). The IMAP FP assay was performed according to the standard

(19) In Vitro and in Vivo antitumor activity and the mechanism of siphonodictyal B in human colon cancer cellsCancer MedicineSeptember 1, 2019Sonoko Chikamatsu, Ken Saijo, Hiroo Imai, Koichi Narita, Yoshifumi Kawamura, Tadashi Katoh, Chikashi Ishioka0.01% Tween‐20, 2 mmol/L DTT, pH 7.4) and incubated in a 384‐well black plate at room temperature. IMAP binding reagent (IMAP Screening Express kit; Molecular Devices, CA, USA) was added and incubated for

(20) Functional divergence caused by mutations in an energetic hotspot in ERK2Proceedings of the National Academy of SciencesJuly 30, 2019Clinton A. Taylor et al.as above. To measure ppERK2 activity toward ERKtide-FAM (NH3+-IPTTPITTTYFFF[K-5FAM]-COO−) using the IMAP fluorescence polarization assay (IMAP FP Kit; Molecular Devices), 3 nM ppERK2 was incubated with 500

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IMAP® Substrate Finder Kits from Molecular Devices

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IMAP® Substrate Finder Kits from Molecular Devices

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