AK59是一种通过HERC4（一种HECT结构域E3连接酶）发挥作用的STING降解剂。
Sample solution is provided at 25 µL, 10mM.
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AK59 is a STING degrader leveraging HERC4, a HECT-domain E3 ligase [1]. AK59 inhibits the cGAS/STING signaling pathway by promoting STING degradation through the ubiquitin-proteasome system (UPS) [2]. AK59 is frequently used in biochemical experiments to screen STING inhibitors and STING mutant-specific degraders [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.
AK59是一种通过HERC4（一种HECT结构域E3连接酶）发挥作用的STING降解剂[1]。AK59通过泛素-蛋白酶体系统（UPS）促进STING降解，从而抑制cGAS/STING信号通路[2]。AK59被广泛用于生化实验中，以筛选STING抑制剂和STING突变体特异性降解剂[3]。
| Cell experiment [1]: | |
Cell lines | THP1 cells |
Preparation Method | THP1 cells were cultured in RPMI 1640 medium containing 10% fetal bovine serum (FBS), 2mM l-glutamine, 25mM Hepes, 1mM sodium pyruvate, and 50U/ml penicillin and 100mg/ml streptomycin at 37℃ in the presence of 5% CO2. 2×106 per well in a six-well plate were seeded and treated with different concentrations of AK59 (1, 2, 5, 7.5, 10µM) for 16h. Subsequently, Western blot analysis was conducted. |
Reaction Conditions | 1, 2, 5, 7.5, 10µM; 16h |
Applications | AK59 treatment significantly reduced STING protein expression in THP1 cells in a dose-dependent manner. |
References: | |
| Cas No. | SDF | ||
| 分子式 | C21H14F3N3O2S | 分子量 | 429.41 |
| 溶解度 | DMSO : 116.67 mg/mL (271.70 mM; Need ultrasonic) | 储存条件 | -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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