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Item number | Size | Datasheet | Manual | SDS | Delivery time | Quantity | Price |
---|---|---|---|---|---|---|---|
BPS-78388 | 384 rxns | - | - |
3 - 15 business days* |
3,444.00€
|
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You can also order by e-mail: info@biomol.com
Larger quantity required? Request bulk
You can also order by e-mail: info@biomol.com
Larger quantity required? Request bulk
Covalent conjugation to ubiquitin (Ub) is one of the major post-translational modifications... more
Product information "CBL-B-driven Tyro3 Ubiquitination Intrachain TR-FRET Assay Kit"
Covalent conjugation to ubiquitin (Ub) is one of the major post-translational modifications regulating 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 E2^¼Ub conjugate and a substrate protein. This step ensures the transfer of Ub from E2^¼Ub to the substrate, leading to its mono- or poly-ubiquitination. Casitas B-lineage lymphoma proto-oncogene-b (CBL-B) is the RING-type E3 ligase that functions as a negative regulator of T cell activation and of growth factor receptor and non-receptor tyrosine kinase signaling. It contains an N-terminal tyrosine kinase binding (TKB) domain comprised of a four-helix bundle, a calcium binding EF-hand and a Src homology (SH2) domain, followed by a linker helical region and the RING domain, responsible for its catalytic function. Additionally, CBL-B contains proline-rich regions mediating the association with tyrosine- and serine phosphorylation sites, and a ubiquitin-associated (UBA)/leucine zipper domain for dimerization. CBL-B interacts with a large number of target proteins implicated in the control of cell proliferation, differentiation, and cell morphology. The ubiquitin ligase activity of CBL-B is up-regulated by the phosphorylation of Tyrosine (Tyr) 363, which is located in the helix linker between the TKB and RING domains. Phosphorylation of Tyr363 opens CBL-B from its auto-inhibitory confirmation, allowing E2 and substrates to bind to CBL-B. CBL-B is phosphorylated for example by receptor-type tyrosine kinase Tyro3, which also serves as a substrate for CBL-B ubiquitylation both in vitro and in vivo. It utilizes a Europium cryptate-labeled Ub (donor) and a Cy5-labeled Ub (acceptor) to complete the TR-FRET pairing. Since both the TR-FRET donor and acceptor are incorporated into poly-ubiquitin chains, 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. Of note, the assay kit does not detect mono-ubiquitination. Figure 1. CBL-B-driven Tyro3 ubiquitination intrachain TR-FRET Assay Kit schematic
Keywords: | CBLB, RNF56, Nbla00127, RING finger protein 56, SH3-binding protein CBL-B, Signal transduction protein CBL-B, E3 ubiquitin-protein ligase CBL-B, RING-type E3 ubiquitin transferase CBL-B, Casitas B-lineage lymphoma proto-oncogene b, |
Supplier: | BPS Bioscience |
Supplier-Nr: | 78388 |
Properties
Application: | CBL-B Ub ligase inhibitor screening, drug discovery, HTS, IC50 determination, real-time kinetics |
Species reactivity: | human |
Format: | Homog. |
Database Information
KEGG ID : | K22517 | Matching products |
UniProt ID : | Q13191 | Matching products |
Gene ID | GeneID 868 | Matching products |
Handling & Safety
Storage: | -80°C |
Shipping: | -80°C (International: °C) |
Caution
Our products are for laboratory research use only: Not for administration to humans!
Our products are for laboratory research use only: Not for administration to humans!
Information about the product reference will follow.
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