PROTAC STING Degrader-1
Based on 1 publication(s) in Google Scholar
PROTAC STING Degrader-1 is a PROTAC degrader targeting the STING pathway with a DC50 of 3.2 μM. PROTAC STING Degrader-1 exerts high anti-inflammatory efficacy. PROTAC STING Degrader-1 can be used to study diseases such as acute kidney injury and inflammatory bowel diseases (IBDs).
(Pink: STING ligand (HY-138682); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W015883)).
For research use only. We do not sell to patients.
- Purity: 98.26%
- CAS No.: 2762552-74-7
- Formula: C34H33N7O10
- Molecular Weight:699.67
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PROTAC STING Degrader-1
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Biological Activity
PROTAC STING Degrader-1 (Compound SP23) (2.5-20 μM) downregulates the downstream signals of STING pathway (IFN-β, IL-6, and CXCL10) triggered by cGAMP in THP-1 cells[1].
PROTAC STING Degrader-1 (1.25-30 μM, 24 h) does not degrade other inflammation-related proteins (JAK2, STAT3, PI3K, AKT, and TLR4) in THP-1 cells[1].
PROTAC STING Degrader-1 (0-40 μM, 2-72 h) degrades STING dose- and time-dependently in THP-1 cells[1].
PROTAC STING Degrader-1 (1.1-30 μM) shows no cytotoxicity in LO2, HEK293A, and C17.2 at doses below 10 μM, but displays a slight cytotoxicity at 30 μM in HEK293A and C17.2 cells[1].
PROTAC STING Degrader-1 (Compound SP23) reduces the production of proinflammatory cytokines and transcription of ISGs in the colon tissues of mice[3].
PROTAC STING Degrader-1 exhibits a dose-dependent degradation efficacy of STING in NCM460 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 cells
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Concentration:0, 0.3, 0.625, 1.25, 2.5, 5, 10, 20, 30, 40 μM
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Incubation Time:2, 4, 8, 12, 24, 48, 72 h
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Result:Exhibited the highest degradation efficiency with a DC50 of 3.2 μM.
Degradation occurred at 4 h and reached maximum degradation at 48 h.
| Species | Dose | Route | AUC | MRT | T1/2 | Tmax | Clearance (CL) | Vz | Plasma Concentration | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat | 2 mg/kg | i.v. | 257 ng·h/mL | 1.74 h | 3.86 h | 0.083 h | 6.80 L/h/kg | 38.01 L/kg | 318.2 ng/mL | / |
| Rat | 20 mg/kg | p.o. | 52.21 ng·h/mL | 7.60 h | 7.36 h | 3.71 h | 429.44 L/h/kg | 4480.43 L/kg | 8.37 ng/mL | 2.15 % |
PROTAC STING Degrader-1 (Compound SP23) (10-30 mg/kg, i.p., 7 consecutive days) ameliorates the severity of DSS-induced colitis in C57BL/6J mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cisplatin-induced acute kidney injury C57BL/6J mouse model[1]
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Dosage:30 and 60 mg/kg
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Administration:Intraperitoneal injection (i.p.) 1 h prior to Cisplatin injection, same time each day for 4 d
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Result:Resulted in survival rates of 89% (30 mg/kg) and 100% (60 mg/kg).
Decreased body weights of mice.
Reduced the levels of blood urea nitrogen and creatinine.
Improved the renal blood flow and reduced kidney swelling.
Significantly alleviated the kidney damages.
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Animal Model:DSS-induced colitis in 8-weeks C57BL/6J mice[3]
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Dosage:10 and 30 mg/kg
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Administration:Intraperitoneal injection (i.p.) for 7 consecutive days
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Result:Reduced body weight and intestinal mucosal destruction.
Ameliorated the colon shortening.
Showed a lower disease activity index in mice.
Led to a significant increase in total immune cells (CD45+).
Decreased the macrophage M1 polarization and downregulated the mRNA levels of M1 macrophage marker genes (iNOS and CD86).
Increased the tight junction proteins.
Downregulated the NLRP3 and cleaved-Capase 1 induced by DSS in mice.
Abrogated the mRNA level of NLRP3 and IL-18.
Chemical Information
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CAS No. 2762552-74-7
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Appearance Solid
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Molecular Weight 699.67
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Formula C34H33N7O10
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Color Light yellow to yellow
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SMILES
O=C(NCCCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)/C=C/C(NC4=CC=C(NC(C5=CC=C([N+]([O-])=O)O5)=O)C=C4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 100 mg/mL (142.92 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Liu J, et al. Novel CRBN-Recruiting Proteolysis-Targeting Chimeras as Degraders of Stimulator of Interferon Genes with In Vivo Anti-Inflammatory Efficacy. J Med Chem. 2022 May 12;65(9):6593-6611. [Content Brief]
[2]. Rongxiang Ma, et al., Discovery of novel rigid STING PROTAC degraders as potential therapeutics for acute kidney injury, European Journal of Medicinal Chemistry, Volume 290, 2025, 117539, ISSN 0223-5234. [Content Brief]
[3]. Shuai Xu, et al., PROTAC based STING degrader attenuates acute colitis by inhibiting macrophage M1 polarization and intestinal epithelial cells pyroptosis mediated by STING-NLRP3 axis, International Immunopharmacology, Volume 141, 2024, 112990, ISSN 1567-5769. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4292 mL | 7.1462 mL | 14.2925 mL | 35.7311 mL |
| 5 mM | 0.2858 mL | 1.4292 mL | 2.8585 mL | 7.1462 mL | |
| 10 mM | 0.1429 mL | 0.7146 mL | 1.4292 mL | 3.5731 mL | |
| 15 mM | 0.0953 mL | 0.4764 mL | 0.9528 mL | 2.3821 mL | |
| 20 mM | 0.0715 mL | 0.3573 mL | 0.7146 mL | 1.7866 mL | |
| 25 mM | 0.0572 mL | 0.2858 mL | 0.5717 mL | 1.4292 mL | |
| 30 mM | 0.0476 mL | 0.2382 mL | 0.4764 mL | 1.1910 mL | |
| 40 mM | 0.0357 mL | 0.1787 mL | 0.3573 mL | 0.8933 mL | |
| 50 mM | 0.0286 mL | 0.1429 mL | 0.2858 mL | 0.7146 mL | |
| 60 mM | 0.0238 mL | 0.1191 mL | 0.2382 mL | 0.5955 mL | |
| 80 mM | 0.0179 mL | 0.0893 mL | 0.1787 mL | 0.4466 mL | |
| 100 mM | 0.0143 mL | 0.0715 mL | 0.1429 mL | 0.3573 mL |
PROTAC STING Degrader-1 Related Classifications
HY-150608 Related Classifications
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