AK59 |
カタログ番号GC74005
One-Click Copy Product Info
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AK59は、HECTドメインE3リガーゼであるHERC4を利用するSTING分解剤である。
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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AK59は、HECTドメインE3リガーゼであるHERC4を利用するSTING分解剤である[1]。AK59は、ユビキチン-プロテアソームシステム（UPS）を通じて、STING分解を促進することで、cGAS/STINGシグナル伝達経路を阻害する[2]。AK59は、STING阻害剤とSTING変異体特異性分解剤をスクリーニングするための生化学実験に広く使われている[3]。
References:
[1] Mutlu M, Schmidt I, Morrison A I, et al. Small molecule induced STING degradation facilitated by the HECT ligase HERC4[J]. Nature communications, 2024, 15(1): 4584.
[2] Zhang Y, Li L, Xu J, et al. A Novel Paradigm for Targeting Challenging Targets: Advancing Technologies and Future Directions of Molecular Glue Degraders[J]. Molecules, 2026, 31(3): 459.
[3] Zhao H Y, Zhang L, Liu Z, et al. Design of potent small-molecule stimulator of interferon gene inhibitor and stimulator of interferon gene mutant-specific degrader[J]. Journal of Medicinal Chemistry, 2025, 68(11): 11100-11126.
| 細胞実験[1]: | |
細胞株 | THP1細胞 |
準備方法 | 37℃、5% CO2の存在下で、10%のウシ胎児血清（FBS）、2mMのl-グルタミン、25mMのHepes、1mMのピルビン酸ナトリウム、50U/mlのペニシリンと100mg/mlのストレプトマイシンを含有するRPMI 1640培地でTHP1細胞を培養した。2×106/ウェルを6ウェルのプレートに播種し、様々な濃度のAK59（1、2、5、7.5、10µM）で16時間処理した。その後、ウエスタンブロット分析を行った。 |
反応条件 | 1、2、5、7.5、10µM；16時間 |
アプリケーション | AK59の処理により、THP1細胞で、STINGタンパク質の発現が用量依存的に著しく減少した。 |
References: | |
| Cas No. | SDF | ||
| Formula | C21H14F3N3O2S | M.Wt | 429.41 |
| 溶解度 | DMSO : 116.67 mg/mL (271.70 mM; Need ultrasonic) | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3288 mL | 11.6439 mL | 23.2878 mL |
| 5 mM | 465.8 μL | 2.3288 mL | 4.6576 mL |
| 10 mM | 232.9 μL | 1.1644 mL | 2.3288 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)