FXR Agonist Assay Kit (TR-FRET) BPS Bioscience

FXR Agonist Assay Kit (TR-FRET)

1222.5 EUR

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Katalognummer: 421 - 78131

Produktkategori: Företag och industri > Vetenskap och laboratorium

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FXR agonist 3 is an anti-NASH agent, acting by activating FXR. FXR agonist 3 inhibits COL1A1, TGF-β1, α-SMA and TIMP1 expression with anti-fibrogenic activity. FXR agonist 3 significantly reduces liver steatosis and inflammation, improves liver fibrosis level[1].

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HY-151959

FXR agonist 4

FXR agonist 4 (compound 10a) is an agonist of farnesoid X receptor (FXR) with an EC50 value of 1.05 μM. FXR agonist 4 effectively improves hyperlipidemia, hepatic steatosis, insulin resistance and hepatic inflammation in DIO mice. FXR agonist 4 can be used for the research of non-alcoholic fatty liver disease (NAFLD)[1].

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HY-153525

FXR agonist 5

FXR agonist 5 (compound 1) is a FXR agonist. FXR agonist 5 can be used for research in diseases or disorders caused by metabolic inflammation[1].

3597.52 €

78304

SMURF2 intrachain TR-FRET Assay Kit

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.

2430 €

78305

VHL intrachain TR-FRET Assay Kit

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.

2475 €

78306

XIAP intrachain TR-FRET Assay Kit

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.

2227.5 €

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