AK59 |
Catalog No.GC74005
One-Click Copy Product Info
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AK59은 HECT 도메인 E3 리가제 HERC4를 활용하는 STING 분해제이다.
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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AK59은 HECT 도메인 E3 리가제 HERC4를 활용하는 STING 분해제이다. AK59은 유비퀴틴-프로테아좀 시스템(UPS)을 통해 STING 분해를 촉진해서 cGAS/STING 신호 전달 경로를 억제한다[2]. AK59은 STING 억제제 및 STING 돌연변이체 특이적 분해제를 선별하기 위한 생화학 실험에 일반적으로 사용된다[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.
| 세포 실험 [1]: | |
세포 라인 | THP1 세포 |
제조 방법 | THP1 세포는 10% 태아소 혈청(FBS)、2 mM L-글루타민、25 mM Hepes、1 mM 피루브산나트륨、50 U/ml 페니실린 및 100 mg/ml 스트렙토마이신이 포함된 RPMI 1640 배양지에서 37℃、5% CO₂ 조건 하에서 배양하였습니다. 6웰 판에 웰당 2×10⁶ 개의 세포를 접종하고 다양한 농도의 AK59 (1、2、5、7.5、10 µM)로 16시간 처리하였습니다. 이후 단백질 자극법을 시행하였습니다. |
반응 조건 | 1, 2, 5, 7.5, 10µM; 16 시간 동안 |
응용 분야 | AK59 처리는 용량 의존적으로 THP1 세포에서 STING 단백질 발현을 현저하게 감소시켰습니다. |
References: | |
| Cas No. | SDF | ||
| Formula | C21H14F3N3O2S | M.Wt | 429.41 |
| Solubility | 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.)