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Submit ReviewSTING Degrader SP23 New
Description: Selective STING Degrader (PROTAC®)
Chemical Name: (2E)-N1-[6-[[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]hexyl]-N4-[4-[[(5-nitro-2-furanyl)carbonyl]amino]phenyl]-2-butenediamide
Purity: ≥98% (HPLC)
Biological Activity for STING Degrader SP23
STING Degrader SP23 is a selective stimulator of interferon gene (STING) Degrader (PROTAC®; DC50 = 3.2 μM). Comprises the STING inhibitor (C-170), joined by a linker to a CRBN ligand Pomalidomide (Cat. No. 6302). It does not degrade JAK2, STAT3, PI3K, AKT and TLR4 in THP-1 cells. STING Degrader SP23 dose dependently reduces the levels of IFN-β, IL-6, and CXCL10 triggered by cGAMP in THP-1 cells; it also modulates the downstream signals of the STING signaling pathway in vivo. STING Degrader SP23 has high anti-inflammatory efficacy in a cisplatin-induced acute kidney injury mouse model.
Negative control STING Degrader N-Me-SP23 (Cat. No. 8054) also available.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Technical Data for STING Degrader SP23
| M. Wt | 699.68 |
| Formula | C34H33N7O10 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2762552-74-7 |
| PubChem ID | 164886634 |
| InChI Key | TXNQXRGOKABDOB-FOCLMDBBSA-N |
| Smiles | O=C1C2=C(NCCCCCCNC(/C=C/C(NC3=CC=C(C=C3)NC(C4=CC=C(N(=O)=O)O4)=O)=O)=O)C=CC=C2C(N1C5C(NC(CC5)=O)=O)=O |
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.
Solubility Data for STING Degrader SP23
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 69.97 | 100 |
Preparing Stock Solutions for STING Degrader SP23
The following data is based on the product molecular weight 699.68. 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 | 1.43 mL | 7.15 mL | 14.29 mL |
| 5 mM | 0.29 mL | 1.43 mL | 2.86 mL |
| 10 mM | 0.14 mL | 0.71 mL | 1.43 mL |
| 50 mM | 0.03 mL | 0.14 mL | 0.29 mL |
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Product Datasheets for STING Degrader SP23
References for STING Degrader SP23
References are publications that support the biological activity of the product.
Liu et al (2022) Novel CRBN-recruiting proteolysis-targeting chimeras as degraders of stimulator of interferon genes with in vivo anti- inflammatory efficacy. J.Med.Chem. 65 6593 PMID: 35452223
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Citations for STING Degrader SP23
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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* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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Epigenetics Scientific Review
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Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
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