2. PROTAC Immunology/Inflammation
  3. PROTACs Cyclic GMP-AMP Synthase
  4. PROTAC cGAS degrader-1

PROTAC cGAS degrader-1 (Compound TH35) is an effective and selective cGAS PROTAC degrader, with DC50 values of 0.9 μM and 4.6 μM in THP-1 and RAW 264.7 cells, respectively. PROTAC cGAS degrader-1 can inhibit the activation of cGAS signaling induced by dsDNA. PROTAC cGAS degrader-1 has anti-inflammatory activity and can be used in the research of cGAS-related inflammatory diseases. (Pink: cGAS inhibitor (HY-133916); Black: Linker (HY-W411604); Blue: E3 ligase ligand (HY-43722))

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

PROTAC cGAS degrader-1

PROTAC cGAS degrader-1 Chemical Structure

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Customer Review

Based on 1 publication(s) in Google Scholar

PROTAC cGAS degrader-1 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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  • References

  • Customer Review

Description

PROTAC cGAS degrader-1 (Compound TH35) is an effective and selective cGAS PROTAC degrader, with DC50 values of 0.9 μM and 4.6 μM in THP-1 and RAW 264.7 cells, respectively. PROTAC cGAS degrader-1 can inhibit the activation of cGAS signaling induced by dsDNA. PROTAC cGAS degrader-1 has anti-inflammatory activity and can be used in the research of cGAS-related inflammatory diseases. (Pink: cGAS inhibitor (HY-133916); Black: Linker (HY-W411604); Blue: E3 ligase ligand (HY-43722))[1]

Molecular Weight

714.60

Formula

C36H33Cl2N7O5
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC(C2=NN(C=C2)C)=C3C(NC4=C3CN(CC4)C(CNC(CCCC#CC5=C(C6=CC=C5)CN(C6=O)C7CCC(NC7=O)=O)=O)=O)=C1Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (139.94 mM; Need ultrasonic; 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 1.3994 mL 6.9969 mL 13.9938 mL
5 mM 0.2799 mL 1.3994 mL 2.7988 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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 1.3994 mL 6.9969 mL 13.9938 mL 34.9846 mL
5 mM 0.2799 mL 1.3994 mL 2.7988 mL 6.9969 mL
10 mM 0.1399 mL 0.6997 mL 1.3994 mL 3.4985 mL
15 mM 0.0933 mL 0.4665 mL 0.9329 mL 2.3323 mL
20 mM 0.0700 mL 0.3498 mL 0.6997 mL 1.7492 mL
25 mM 0.0560 mL 0.2799 mL 0.5598 mL 1.3994 mL
30 mM 0.0466 mL 0.2332 mL 0.4665 mL 1.1662 mL
40 mM 0.0350 mL 0.1749 mL 0.3498 mL 0.8746 mL
50 mM 0.0280 mL 0.1399 mL 0.2799 mL 0.6997 mL
60 mM 0.0233 mL 0.1166 mL 0.2332 mL 0.5831 mL
80 mM 0.0175 mL 0.0875 mL 0.1749 mL 0.4373 mL
100 mM 0.0140 mL 0.0700 mL 0.1399 mL 0.3498 mL
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PROTAC cGAS 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 cGAS degrader-1PROTAC cGAS degrader1PROTAC cGAS degrader 1PROTACsCyclic GMP-AMP SynthasecGASTHP-1RAW 264.7Ulcerative colitis modelInhibitorinhibitorinhibit

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