STING Degrader SP23

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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)
Datasheet
Citations
Reviews
Literature (2)

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, PI 3-K, 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) and STING/TMEM173 antibodies validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF6516 and NBP3-18816.

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.

Select a batch to recalculate based on the batch molecular weight:
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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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

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