VER 155008是一种强效的，源自腺苷的热休克蛋白70（Hsp70）家族抑制剂，对Hsp70、热休克同源蛋白70（Hsc70）和葡萄糖调节蛋白78（Grp78）的IC50值分别为0.5μM、2.6μM和2.6μM。
Cas No.:1134156-31-2
Sample solution is provided at 25 µL, 10mM.
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VER 155008 is a potent, adenosine-derived inhibitor of the heat shock protein 70 (Hsp70) family, with IC50 values of 0.5μM, 2.6μM, and 2.6μM against Hsp70, heat shock cognate protein 70 (Hsc70), and glucose-regulated protein 78 (Grp78), respectively[1]. VER 155008 exerts its effects by inhibiting Hsp70 ATPase activity, inducing cell cycle arrest, apoptosis, and tumor-specific cell death, and is commonly used in anti-cancer (e.g., prostate and breast cancer) and antiviral research[2,3,4].
In vitro, treatment with VER 155008 (20μM) for 48h in 211H and H28 cells significantly increased the proportion of cells in the G1 phase (from 69.9% to 82.7% in 211H cells; from 77% to 85.2% in H28 cells)[5]. VER 155008 (25μM) treatment in A549 and H1975 cells for 2 days significantly reduced the percentage of 5-bromo-2'-deoxyuridine (BrdU)-positive cells, indicating inhibition of cell proliferation[6].
In vivo, intraperitoneal injection of VER 155008 (40mg/kg; once daily) for two weeks in PC12 tumor-bearing nude mice significantly reduced tumor volume and tumor weight[7]. A single intravenous dose of VER 155008 (25mg/kg) in BALB/c mice resulted in a plasma half-life of 0.6h and a clearance rate of 49mL/min/kg[1].
References:
[1] MASSEY A J, WILLIAMSON D S, BROWNE H, et al. A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells[J]. Cancer Chemotherapy and Pharmacology, 2010, 66(3): 535-545.
[2] BUDINA-KOLOMETS A, BALABURSKI G M, BONDAR A, et al. Comparison of the activity of three different HSP70 inhibitors on apoptosis, cell cycle arrest, autophagy inhibition, and HSP90 inhibition[J]. Cancer Biology & Therapy, 2014, 15(2): 194-199.
[3] WENG J R, HUA C H, CHEN C H, et al. Anti-apoptotic activity of Japanese encephalitis virus NS5 protein in human medulloblastoma cells treated with interferon-β[J]. Journal of Microbiology, Immunology and Infection, 2018, 51(4): 456-464.
[4] YU B, YANG H, ZHANG X, et al. Visualizing and quantifying the effect of the inhibition of HSP70 on breast cancer cells based on laser scanning microscopy[J]. Technology in Cancer Research & Treatment, 2018, 17: 1533033818785274.
[5] SAKAI K, INOUE M, MIKAMI S, et al. Functional inhibition of heat shock protein 70 by VER‐155008 suppresses pleural mesothelioma cell proliferation via an autophagy mechanism[J]. Thoracic Cancer, 2021, 12(4): 491-503.
[6] WEN W, LIU W, SHAO Y, et al. VER-155008, a small molecule inhibitor of HSP70 with potent anti-cancer activity on lung cancer cell lines[J]. Experimental Biology and Medicine, 2014, 239(5): 638-645.
[7] XU F, LIN D, JIANG W, et al. HSP70 inhibitor VER155008 suppresses pheochromocytoma cell and xenograft growth by inhibition of PI3K/AKT/mTOR and MEK/ERK pathways[J]. International Journal of Clinical and Experimental Pathology, 2019, 12(7): 2585.
VER 155008是一种强效的，源自腺苷的热休克蛋白70（Hsp70）家族抑制剂，对Hsp70、热休克同源蛋白70（Hsc70）和葡萄糖调节蛋白78（Grp78）的IC50值分别为0.5μM、2.6μM和2.6μM[1]。VER 155008通过抑制Hsp70 ATP酶活性，诱导细胞周期停止、细胞凋亡和肿瘤特异性细胞死亡发挥作用，通常用于抗癌（如前列腺癌和乳腺癌等）和抗病毒研究[2,3,4]。
在体外，VER 155008（20μM）处理211H和H28细胞48h，G1期细胞比例显著增加（211H从69.9%增加到82.7%；H28从77%增加到85.2%）[5]。VER 155008（25μM）处理A549和H1975细胞2天，5-bromo-2’-deoxyuridine（BrdU）阳性细胞百分比显著降低，细胞增殖被抑制[6]。
在体内，VER 155008（40mg/kg; once daily）通过腹腔注射治疗PC12荷瘤裸鼠2周，肿瘤体积显著减小且肿瘤重量也显著减轻[7]。VER 155008（25mg/kg）通过单次静脉注射处理BALB/c小鼠，血浆半衰期为0.6h，清除率为49mL/min/kg[1]。
| Cell experiment [1]: | |
Cell lines | A549 and H1975 cells |
Preparation Method | A549 and H1975 cells were treated with 25μM VER 155008 for 2 days, then incubated with 10μM BrdU for 1h. BrdU-positive cells were detected by anti-BrdU FITC antibody. |
Reaction Conditions | 25μM; 2 days |
Applications | Treatment with VER 155008 significantly reduced the percentage of BrdU-positive cells and inhibited cell proliferation. |
| Animal experiment [2]: | |
Animal models | Nude mice xenografted with PC12 tumor cells |
Preparation Method | PC12 cells (1×106 cells) were injected subcutaneously into nude mice. When tumors reached 80-150mm3, mice were intraperitoneally injected with VER 155008 (40mg/kg) once daily for 2 weeks. Tumor volume were measured every day. |
Dosage form | 40mg/kg; once daily; 2 weeks; i.p. |
Applications | Treatment with VER 155008 significantly reduced tumor volume. |
References: | |
| Cas No. | 1134156-31-2 | SDF | |
| 别名 | adenosine-derived inhibitor, VER155008, VER-155008 | ||
| 化学名 | 4-[[(2R,3S,4R,5R)-5-[6-amino-8-[(3,4-dichlorophenyl)methylamino]purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methoxymethyl]benzonitrile | ||
| Canonical SMILES | C1=CC(=CC=C1COCC2C(C(C(O2)N3C4=C(C(=NC=N4)N)N=C3NCC5=CC(=C(C=C5)Cl)Cl)O)O)C#N | ||
| 分子式 | C25H23Cl2N7O4 | 分子量 | 556.4 |
| 溶解度 | ≥ 27.8mg/mL in DMSO, ≥ 4.65 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -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 | 1.7973 mL | 8.9863 mL | 17.9727 mL |
| 5 mM | 359.5 μL | 1.7973 mL | 3.5945 mL |
| 10 mM | 179.7 μL | 898.6 μL | 1.7973 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: >99.50% Appearance: A solid
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