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Acts as a molecular glue to induce proteosomal degradation of mRNA splicing factor RBM39 (also designated CAPERα, HCC1, FSAP59, and RNPC2), via binding to DCAF15. Acts as a pre-mRNA splicing modulator (SPLAMs; splicing inhibitor sulfonamides), causes aberrant pre-mRNA splicing. Suppresses proliferation of cancer cell lines. Reduces viability of HCT-116 cells (IC50 = 0.56 μM). Induces cell cycle arrest in the G1 phase in cancer cell lines. Also a high affinity carbonic anhydrase isozyme XII (hCA XII) inhibitor (Ki = 3.0-5.7 nM).
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 385.84. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.59 mL||12.96 mL||25.92 mL|
|5 mM||0.52 mL||2.59 mL||5.18 mL|
|10 mM||0.26 mL||1.3 mL||2.59 mL|
|50 mM||0.05 mL||0.26 mL||0.52 mL|
References are publications that support the biological activity of the product.
Han et al (2017) Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15. Science 28 356 PMID: 28302793
Uehara et al (2017) Selective degradation of splicing factor CAPERa by anticancer sulfonamides. Nat.Chem.Biol. 13 675 PMID: 28437394
Ozawa et al (2001) E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo. Eur.J.Cancer. 37 2275 PMID: 11677118
Owa et al (1999) Discovery of novel antitumor sulfonamides targeting G1 phase of the cell cycle. J.Med.Chem. 42 3789 PMID: 10508428
Di et al (2018) Function, clinical application, and strategies of Pre-mRNA splicing in cancer. Cell Death Differ. doi: 10.1038/s41418- PMID: 30464224
Vullo et al (2005) Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs? Bioorg.Med.Chem.Lett. 15 963 PMID: 15686894
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
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Targeted Protein Degradation Research Product Guide
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
- Active Degraders (e.g. PROTACs)
- Degrader Building Blocks
- Custom Degrader Services
- UPS Proteins and Assays
- Assays for Protein Degradation
Programmed Cell Death Poster
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia