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产品介绍 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 X-linked inhibitor of apoptosis (XIAP) protein is a RING-containing E3 Ub ligase which has the ability to directly regulate caspases and suppress apoptotic cell death pathways. An increased expression level of XIAP has been shown for many cancer types and is associated with cancer cell migration. Like most E3 ligases, XIAP ubiquitinates itself. The XIAP intrachain TR-FRET Assay Kit is a sensitive high-throughput screening (HTS) TR-FRET Assay Kit, designed to measure XIAP 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 XIAP, 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.
询价产品介绍 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 von Hippel-Lindau protein (VHL) interacts with Elongins B and C, Cullin 2, and Ring Box Protein 1 (Rbx1) to form the functional E3 Ub ligase complex where it functions as a substrate recognition entity. Most of the tumor-derived mutations within VHL disrupt its tumor suppressor role by compromising its substrate receptor function and generally whole VHL complex Ub ligase activity. VHL complex not only targets the alpha subunits of the heterodimeric transcription factor hypoxia inducible factor (HIF) for ubiquitylation and proteasomal degradation, but it is involved in many other biological processes related to tumor growth. That is why it is an attractive potential drug target in cancer immunotherapy. Like most E3 ligases, VHL complex can ubiquitinate itself. The VHL intrachain TR-FRET Assay Kit is a sensitive high-throughput screening (HTS) TR-FRET Assay Kit, designed to measure VHL 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 VHL, 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.
询价产品介绍 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 2 (SMURF2) 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 SMURF2 and especially its Ub ligase activity is an attractive potential drug target in cancer immunotherapy. Like most E3 ligases, SMURF2 ubiquitinates itself. The SMURF2 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 SMURF2, 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.
询价产品介绍 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.
询价产品介绍 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.
询价产品介绍 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.
询价背景介绍 The pandemic coronavirus disease 2019 (COVID-19) is caused by Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). As a first step of the viral replication strategy, the virus attaches to the host cell surface before entering the cell. The Spike protein binds to the Angiotensin-Converting Enzyme 2 (ACE2) receptor found on the surface of type I and II pneumocytes, endothelial cells, and ciliated bronchial epithelial cells. Drugs targeting the interaction between the Spike protein of SARS-CoV-2 and human ACE2 may offer some protection against the viral infection. SARS-CoV-2 (B.1.617.2.1), also known as Delta plus variant, was first identified in March, 2021 in several genome samples from India of the Delta variant (B.1.617.2). This variant contains an additional K417N mutation, as well as all the mutations of the Delta variant (T19R, G142D, R158G, L452R, T478K D614G and P681R plus a deletion E156/F157 in the Spike protein) that may lead to higher transmissibility and infectivity. 产品介绍 The Spike S1 (B.1.617.2.1; Delta Plus Variant) (SARS-CoV-2): ACE2 TR-FRET Assay is designed to measure the inhibition of the binding between SARS-CoV-2 Spike S1 (B.1.617.2.1; Delta Plus Variant) and human ACE2 in a homogeneous 384 reaction format. This TR-FRET-based assay requires no time-consuming washing steps, making it especially suitable for high throughput screening applications. The assay procedure is straightforward and simple; the test inhibitor compound is incubated with biotinylated Spike S1, Eu-labeled ACE2, and dye-labeled acceptor for one hour. Then the TR-FRET signal is measured using a fluorescence reader capable of measuring Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET).
询价背景介绍 The pandemic coronavirus disease 2019 (COVID-19) is caused by Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). As a first step of the viral replication strategy, the virus attaches to the host cell surface before entering the cell. The Spike protein binds to the Angiotensin-Converting Enzyme 2 (ACE2) receptor found on the surface of type I and II pneumocytes, endothelial cells, and ciliated bronchial epithelial cells. Drugs targeting the interaction between the Spike protein of SARS-CoV-2 and human ACE2 may offer some protection against the viral infection. This SARS-CoV-2 Spike S1 mutant contains three critical mutations K417T, E484K, and N501Y found in the P.1 variant (Gamma variant) originally discovered in Brazil. 产品介绍 The Spike S1 (K417T, E484K, N501Y) (SARS-CoV-2): ACE2 TR-FRET Assay is designed to measure the inhibition of the binding between SARS-CoV-2 Spike S1 (K417T, E484K, N501Y) and human ACE2 in a homogeneous 384 reaction format. This TR-FRET-based assay requires no time-consuming washing steps, making it especially suitable for high throughput screening applications. The assay procedure is straightforward and simple; the test inhibitor compound is incubated with biotinylated Spike S1, Eu-labeled ACE2, and dye-labeled acceptor for one hour. Then the TR-FRET signal is measured using a fluorescence reader capable of measuring Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET).
询价背景介绍 The pandemic coronavirus disease 2019 (COVID-19) is caused by Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). As a first step of the viral replication strategy, the virus attaches to the host cell surface before entering the cell. The Spike protein binds to the Angiotensin-Converting Enzyme 2 (ACE2) receptor found on the surface of type I and II pneumocytes, endothelial cells, and ciliated bronchial epithelial cells. Drugs targeting the interaction between the Spike protein of SARS-CoV-2 and human ACE2 may offer some protection against the viral infection. The SARS-CoV-2 variant B.1.429, also known as Epsilon Variant, was first discovered in California, United States. It contains mutations W152C, and L452R and D614G. 产品介绍 The Spike S1 (B.1.429; Epsilon Variant) (SARS-CoV-2): ACE2 TR-FRET Assay is designed to measure the inhibition of the binding between SARS-CoV-2 Spike S1 (B.1.429; Epsilon Variant) and human ACE2 in a homogeneous 384 reaction format. This TR-FRET-based assay requires no time-consuming washing steps, making it especially suitable for high throughput screening applications. The assay procedure is straightforward and simple; the test inhibitor compound is incubated with biotinylated Spike S1, Eu-labeled ACE2, and dye-labeled acceptor for one hour. Then the TR-FRET signal is measured using a fluorescence reader capable of measuring Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET).
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