2. PROTAC Immunology/Inflammation
  3. PROTACs STING
  4. PROTAC STING Degrader-1

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: CRBN ligand (HY-10984); Black: linker (HY-W015883)).

For research use only. We do not sell to patients.

PROTAC STING Degrader-1 Chemical Structure

PROTAC STING Degrader-1 Chemical Structure

CAS No. : 2762552-74-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

PROTAC STING Degrader-1 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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: CRBN ligand (HY-10984); Black: linker (HY-W015883))[1][2][3].

In Vitro

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.

PROTAC STING Degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: THP-1 cells
Concentration: 0, 0.3, 0.625, 1.25, 2.5, 5, 10, 20, 30, 40 μM
Incubation Time: 2, 4, 8, 12, 24, 48, 72 h
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.
Parmacokinetics
Species Dose Route Indicator value
Rat 2 mg/kg i.v. AUC0-t 257 ng·h/mL
Rat 20 mg/kg p.o. AUC0-t 52.21 ng·h/mL
Rat 2 mg/kg i.v. AUC 258 ng·h/mL
Rat 20 mg/kg p.o. AUC0-∞ 55.68 ng·h/mL
Rat 2 mg/kg i.v. MRT0-t 1.74 hr
Rat 20 mg/kg p.o. MRT0-t 7.60 hr
Rat 2 mg/kg i.v. MRT0-∞ 1.95 hr
Rat 20 mg/kg p.o. MRT0-∞ 11.67 hr
Rat 2 mg/kg i.v. T1/2 3.86 hr
Rat 20 mg/kg p.o. T1/2 7.36 hr
Rat 2 mg/kg i.v. Tmax 0.083 hr
Rat 20 mg/kg p.o. Tmax 3.71 hr
Rat 2 mg/kg i.v. CL 6.80 L/h/kg
Rat 20 mg/kg p.o. CL 429.44 L/h/kg
Rat 2 mg/kg i.v. Vz 38.01 L/kg
Rat 20 mg/kg p.o. Vz 4480.43 L/kg
Rat 2 mg/kg i.v. Cmax 318.2 ng/mL
Rat 20 mg/kg p.o. Cmax 8.37 ng/mL
Rat 20 mg/kg p.o. F 2.15 %
In Vivo

PROTAC STING Degrader-1 (Compound SP23) (30-60 mg/kg, i.p. 1 h prior to Cisplatin (HY-17394) injection, same time each day for 4 d) significantly alleviates the ischemic symptoms and the kidney weights reduces dramatically and dose-dependently in Cisplatin-induced acute kidney injury C57BL/6J mouse model[1].
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.

Animal Model: Cisplatin-induced acute kidney injury C57BL/6J mouse model[1]
Dosage: 30 and 60 mg/kg
Administration: Intraperitoneal injection (i.p.) 1 h prior to Cisplatin injection, same time each day for 4 d
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.
Animal Model: DSS-induced colitis in 8-weeks C57BL/6J mice[3]
Dosage: 10 and 30 mg/kg
Administration: Intraperitoneal injection (i.p.) for 7 consecutive days
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.
Molecular Weight

699.67

Formula

C34H33N7O10
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4292 mL 7.1462 mL 14.2925 mL
5 mM 0.2858 mL 1.4292 mL 2.8585 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PROTAC STING Degrader-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC STING Degrader-12762552-74-7PROTAC STING Degrader1PROTAC STING Degrader 1PROTACsSTINGStimulator of Interferon GenesTMEM173MITAERISMPYSanti-inflammatorystimulator of interferon geneskidney injuryIBDInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PROTAC STING Degrader-1
Cat. No.:
HY-150608
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB) Italian - IT (251 KB) Portuguese - PT (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.