Catalog number: 421 - 78428
Product Category: Business & Industrial > Science & Laboratory
Size: 384 rxns.
78301
Covalent conjugation to ubiquitin (Ub) is one of the major post-translational modifications that regulates protein stability, function, and localization. Ubiquitination is the concerted action of three enzymes: a Ub-activating enzyme (E1), a Ub-conjugating enzyme (E2), and a Ub ligase (E3). The specificity and efficiency of ubiquitination are largely determined by the E3 enzyme, which directs the last step of the Ub-conjugating cascade by binding to both an E2~Ub conjugate and a substrate protein. This step ensures the transfer of Ub from E2~Ub to the substrate, leading to its mono- or poly-ubiquitination.The Cereblon (CRBN) protein via its interaction with the DNA damage-binding protein-1 (DDB1), Cullin 4 (Cul4A or Cul4B), and regulator of Cullins 1 (RoC1) forms the functional E3 Ub ligase complex. In this complex, Cereblon functions as a substrate receptor that mediates the ubiquitination and subsequent proteasomal degradation of target proteins. Cereblon complex is involved in many biological processes including cell proliferation and apoptosis. That is why it has been employed for targeted protein degradation in the treatment of cancer. Like most E3 ligases, Cereblon complex ubiquitinates itself and this auto-ubiquitination promotes its Ub ligase activity.The Cereblon intrachain TR-FRET Assay Kit is a sensitive high-throughput screening (HTS) TR-FRET Assay Kit, designed to measure Cereblon auto-ubiquitination activity in a homogeneous 384 reaction format. It utilizes a Europium cryptate-labeled Ub (donor) as well as Cy5-labeled Ub (acceptor) to complete the TR-FRET pairing. Since both the TR-FRET donor and acceptor are incorporated into poly-ubiquitin chains formed on Cereblon, this FRET-based assay requires no time-consuming washing steps, making it especially suitable for HTS applications as well as real-time kinetics analyses of polyubiquitination.
78302
Covalent conjugation to ubiquitin (Ub) is one of the major post-translational modifications that regulates protein stability, function, and localization. Ubiquitination is the concerted action of three enzymes: a Ub-activating enzyme (E1), a Ub-conjugating enzyme (E2), and a Ub ligase (E3). The specificity and efficiency of ubiquitination are largely determined by the E3 enzyme, which directs the last step of the Ub-conjugating cascade by binding to both an E2~Ub conjugate and a substrate protein. This step ensures the transfer of Ub from E2~Ub to the substrate, leading to its mono- or poly-ubiquitination.The human Mouse double minute 2 homolog (MDM2) is an E3 Ub ligase and the master regulator of tumor suppressor proteins such as p53. Thus, high activity of MDM2 can promote tumor formation by targeting tumor suppressor proteins for proteasomal degradation, enabling cancer cell survival and proliferation. That is why MDM2 is an attractive potential drug target in cancer immunotherapy. Like most E3 ligases, MDM2 ubiquitinates itself and this auto-ubiquitination stimulates MDM2 Ub ligase activity.The MDM2 intrachain TR-FRET Assay Kit is a sensitive high-throughput screening (HTS) TR-FRET Assay Kit, designed to measure MDM2 auto-ubiquitination activity in a homogeneous 384 reaction format. It utilizes a Europium cryptate-labeled Ub (donor) as well as Cy5-labeled Ub (acceptor) to complete the TR-FRET pairing. Since both the TR-FRET donor and acceptor are incorporated into poly-ubiquitin chains formed on MDM2, this FRET-based assay requires no time-consuming washing steps, making it especially suitable for HTS applications as well as real-time kinetics analyses of polyubiquitination.
78303
Covalent conjugation to ubiquitin (Ub) is one of the major post-translational modifications that regulates protein stability, function, and localization. Ubiquitination is the concerted action of three enzymes: a Ub-activating enzyme (E1), a Ub-conjugating enzyme (E2), and a Ub ligase (E3). The specificity and efficiency of ubiquitination are largely determined by the E3 enzyme, which directs the last step of the Ub-conjugating cascade by binding to both an E2~Ub conjugate and a substrate protein. This step ensures the transfer of Ub from E2~Ub to the substrate, leading to its mono- or poly-ubiquitination.The SMAD ubiquitination regulatory factor 1 (SMURF1) is a HECT-type E3 Ub ligase that regulates TGF-β/BMP pathways via ubiquitination of key signal transducers (SMAD1, SMAD2, or SMAD5), or TGF-β receptor I. SMURFs play a critical role in cell-type specification, tissue and organ development by regulating planar cell polarity signaling and convergent extension. SMURFs can also accelerate tumor progression, invasion, and metastasis as they regulate ubiquitination and subsequent proteasomal degradation of tumor-suppressing proteins including p53 as well as various cell signaling proteins. That is why SMURF1 and especially its Ub ligase activity is an attractive potential drug target in cancer immunotherapy. Like most E3 ligases, SMURF1 ubiquitinates itself.The SMURF1 intrachain TR-FRET Assay Kit is a sensitive high-throughput screening (HTS) TR-FRET Assay Kit, designed to measure SMURF1 auto-ubiquitination activity in a homogeneous 384 reaction format. It utilizes a Europium cryptate-labeled Ub (donor) as well as Cy5-labeled Ub (acceptor) to complete the TR-FRET pairing. Since both the TR-FRET donor and acceptor are incorporated into poly-ubiquitin chains formed on SMURF1, this FRET-based assay requires no time-consuming washing steps, making it especially suitable for HTS applications as well as real-time kinetics analyses of polyubiquitination.
32631
The WDR9 TR-FRET Assay Kit is designed to measure the inhibition of the binding of WDR9,_x000D_also known as BRWD1, to its substrate in a homogeneous 384 reaction format. This FRETbased_x000D_assay requires no time-consuming washing steps, making it especially suitable for high_x000D_throughput screening applications. The assay procedure is straightforward and simple; a sample_x000D_containing terbium-labeled donor, dye-labeled acceptor, WDR9, substrate, and an inhibitor is_x000D_incubated for 2 hours. Then, the fluorescence intensity is measured using a fluorescence_x000D_reader.
32632
The BPTF TR-FRET Assay Kit is designed to measure the inhibition of the binding of BPTF,_x000D_also known as FALZ, to its substrate in a homogeneous 384 reaction format. This FRET-based_x000D_assay requires no time-consuming washing steps, making it especially suitable for high_x000D_throughput screening applications. The assay procedure is straightforward and simple; a sample_x000D_containing terbium-labeled donor, dye-labeled acceptor, BPTF, substrate, and an inhibitor is_x000D_incubated for 2 hours. Then, the fluorescence intensity is measured using a fluorescence_x000D_reader.
50222
The BCL-2 TR-FRET Assay Kit is designed to measure the inhibition of BCL-2_x000D_binding to its ligand in a homogeneous 384 reaction format. This FRET-based assay requires no_x000D_time-consuming washing steps, making it especially suitable for high throughput screening_x000D_applications. The assay procedure is straightforward and simple; a sample containing terbiumlabeled_x000D_donor, dye-labeled acceptor, BCL-2, peptide ligand, and an inhibitor is incubated for 120_x000D_minutes. Then, the fluorescence intensity is measured using a fluorescence reader.