NSC 185058是一种ATG4B的合成抑制剂，IC50值为51μM。
Cas No.:39122-38-8
Sample solution is provided at 25 µL, 10mM.
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NSC 185058 is a synthetic inhibitor of the ATG4B, with an IC50 value of 51μM [1]. NSC 185058 inhibits autophagy, which in turn suppresses the activity of mTORC1 as well as the phosphorylation status of the P70S6K and 4EBP1, thereby preventing the increase in cellular protein anabolism[2]. NSC 185058 has been widely used to prevent the replication of Enterovirus 71 (EV71) and to inhibit the infection of virus-infected cells[3].
In vitro, NSC 185058 (100µM) treatment for 72 hours significantly reduced the protein content of ATG4B in A549 cells and inhibited cell proliferation[4]. Treatment with 10µM NSC 185058 for 6 days significantly inhibited the formation of osteoclasts induced by RANKL in mouse bone marrow cells, and induced cell death[5]. Treatment with 5µM NSC 185058 for 2 hours in combination with 3Gy ionizing radiation reduced the viability of mutant IDH1 glioma cells and increased cell radiosensitivity[6].
In vivo, NSC 185058 treatment via subcutaneous injection at a dose of 100mg/kg, every other day for 5 days, significantly inhibited the growth of Saos-2 osteosarcoma in mice within 30 days, without altering the body size of the mice[7].
References:
[1] Qiu Z, Kuhn B, Aebi J, et al. Discovery of fluoromethylketone-based peptidomimetics as covalent ATG4B (autophagin-1) inhibitors[J]. ACS medicinal chemistry letters, 2016, 7(8): 802-806.
[2] Ryan P J, Uranga S, Stanelle S T, et al. The autophagy inhibitor NSC185058 suppresses mTORC1-mediated protein anabolism in cultured skeletal muscle[J]. Scientific reports, 2024, 14(1): 8094.
[3] Sun Y, Zheng Q, Wang Y, et al. Activity-based protein profiling identifies ATG4B as a key host factor for enterovirus 71 proliferation[J]. Journal of Virology, 2019, 93(24): 10.1128/jvi. 01092-19.
[4] Ryan P J, Guerra B C, Uranga S, et al. ATG4B is required for mTORC1‐mediated anabolic activity and is associated with clinical outcomes in non‐small cell lung cancer[J]. FEBS Open Bio, 2026, 16(3): 570-583.
[5] Hiura F, Kawabata Y, Aoki T, et al. Inhibition of the ATG4-LC3 pathway suppressed osteoclast maturation[J]. Biochemical and biophysical research communications, 2022, 632: 40-47.
[6] Núñez F J, Banerjee K, Mujeeb A A, et al. Autophagy Upregulation in Mutant Isocitrate Dehydrogenase 1 (IDH1) Glioma Uncovers a Novel Therapeutic Target[J]. Research square, 2025: rs. 3. rs-7483444.
[7] Akin D, Wang S K, Habibzadegah-Tari P, et al. A novel ATG4B antagonist inhibits autophagy and has a negative impact on osteosarcoma tumors[J]. Autophagy, 2014, 10(11): 2021-2035.
NSC 185058是一种ATG4B的合成抑制剂，IC50值为51μM[1]。NSC 185058抑制自噬，进而抑制mTORC1 活性以及P70S6K和4EBP1的磷酸化状态，从而阻止细胞蛋白质合成代谢的增加[2]。NSC 185058已被广泛用于阻止肠道病毒71型(EV71)的复制，并抑制病毒对感染细胞的入侵[3]。
在体外，100μM的NSC 185058处理A549细胞72小时，显著降低了细胞中ATG4B的蛋白含量并抑制了细胞增殖[4]。使用10μM的NSC 185058处理小鼠骨髓细胞6天，显著抑制了RANKL诱导的破骨细胞形成，并诱导了细胞死亡[5]。将5μM的NSC 185058与3Gy电离辐射联合处理突变IDH1胶质瘤细胞2小时，降低了细胞活力并增加了细胞放射敏感性[6]。
在体内，每隔一天皮下注射100mg/kg剂量的NSC 185058，持续5天，在30天内显著抑制了小鼠体内Saos-2骨肉瘤的生长，且未改变小鼠的体型[7]。
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | A549 cells were cultured in RPMI-1640 medium containing 10% fetal bovine serum (FBS) in 5% CO2 at 37°C. Cells were placed in 96-well plates at a concentration of 1×104 cells per well. Using 0.1% DMSO as a control, cells received NSC 185058 (100μM) treatment for 72h. At the end of administration, the supernatant was discarded, and the viable cell numbers were measured and the protein synthesis rates were measured. |
Reaction Conditions | 100μM; 72h |
Applications | NSC 185058 treatment significantly reduced cell proliferation in A549 cells and resulted in decreased protein synthesis rates. |
| Animal experiment [2]: | |
Animal models | Immunodeficient nu/nu nude female mice |
Preparation Method | Immunodeficient nu/nu nude female mice (20-24g) were housed in a specialized animal care facility, in a room with constant temperature (25°C), humidity control, and a 12/12h light/dark cycle with free access to food and water. Mice were injected subcutaneously with 6×106 Saos-2 cells. Palpable Saos-2 tumors developed in 7 to 10 days, at which time, the mice were divided into 2 groups and injected i.p. every other day for 5 days, with either peanut oil vehicle or NSC 185058 (100mg/kg) dissolved in peanut oil. Over time, the tumor volumes and the body weight were measured. |
Dosage form | 100mg/kg; every other day for 5 days; i.p. |
Applications | NSC 185058 treatment significantly inhibited the growth of Saos-2 osteosarcoma in mice within 30 days, without altering the body size of the mice. |
References:
[1] Ryan P J, Guerra B C, Uranga S, et al. ATG4B is required for mTORC1‐mediated anabolic activity and is associated with clinical outcomes in non‐small cell lung cancer[J]. FEBS Open Bio, 2026, 16(3): 570-583.
[2] Akin D, Wang S K, Habibzadegah-Tari P, et al. A novel ATG4B antagonist inhibits autophagy and has a negative impact on osteosarcoma tumors[J]. Autophagy, 2014, 10(11): 2021-2035.
| Cas No. | 39122-38-8 | SDF | |
| Canonical SMILES | S=C(C1=NC=CC=C1)NC2=NC=CC=C2 | ||
| 分子式 | C11H9N3S | 分子量 | 215.27 |
| 溶解度 | DMSO : ≥ 125 mg/mL (580.67 mM) | 储存条件 | 4°C, protect from light |
| 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 | 4.6453 mL | 23.2266 mL | 46.4533 mL |
| 5 mM | 929.1 μL | 4.6453 mL | 9.2907 mL |
| 10 mM | 464.5 μL | 2.3227 mL | 4.6453 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。
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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