|CRBN (D8H3S) Rabbit mAb 71810||20 µl||
||H M R||55||Rabbit IgG|
|CUL4A Antibody 2699||20 µl||
||H Mk||80, 82||Rabbit|
|DDB-1 (D4C8) Rabbit mAb 6998||20 µl||
||H M R Mk||127||Rabbit IgG|
|RBX1 (D3J5I) Rabbit mAb 11922||20 µl||
||H M R Mk||13||Rabbit IgG|
|NEDD8 (19E3) Rabbit mAb 2754||20 µl||
||H M R Mk||9||Rabbit IgG|
|Ubiquitin (E4I2J) Rabbit mAb 43124||20 µl||
|Anti-rabbit IgG, HRP-linked Antibody 7074||100 µl||
Monoclonal antibodies are produced by immunizing animals with synthetic peptides corresponding to residues surrounding Pro44 of human CRBN protein, Gly832 of human DDB-1 protein, Gly35 of human ubiquitin protein, the amino terminus of human NEDD8 protein, and the carboxy terminus of human RBX1 protein. Polyclonal antibodies are produced by immunizing animals with a synthetic peptide corresponding to residues surrounding Ser12 of human CUL4A. Antibodies are purified by peptide affinity chromatography.
Targeted protein degradation is an experimental method of drug-based protein targeting that leverages endogenous E3 ubiquitin ligases and the ubiquitin proteasome system (UPS) to selectively degrade target proteins. It is being actively explored as a therapeutic strategy to target and degrade specific proteins that contribute to disease progression (1). This approach differs from traditional small-molecule therapeutics that seek to suppress disease proteins (e.g., kinases) by sterically blocking catalytic domains. Protein-targeting chimeras (PROTACs) are the prototypical protein "degraders”. PROTACs are bivalent chemical ligands that induce proximity between a target protein and an E3 ubiquitin ligase, resulting in ubiquitination of the target protein, and its subsequent degradation by the UPS (2,3). Cereblon (CRBN) is the substrate-recognition component of a Cullin-RING-ubiquitin ligase complex (CRL4/CRBN) that was among the first to be recognized for its therapeutic potential via targeted protein degradation (4). The CRL4/CRBN complex is comprised of CRBN, DDB-1, RBX1, and the scaffold protein CUL4A; its ligase activity is dynamically regulated via the covalent modification (neddylation) of CUL4A by NEDD8 (5). In unrelated mechanistic studies of multiple myeloma drugs, it was revealed that phthalimides (e.g., thalidomide, lenalidomide) promoted CRBN-dependent recruitment, ubiquitination, and proteasomal degradation of the immunological transcription factors Ikaros (IKZF1) and Aiolos (IKZF3) (6). The discovery that phthalimides were functioning as PROTACs, by eliciting the selective degradation of what were previously considered "undruggable" protein targets, led to a rapid acceleration and expansion of research into targeted protein degradation, with the promise of novel therapies for diseases deemed largely intractable using conventional small-molecule therapies (7-9).
Explore pathways related to this product.
Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.
Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.