VER 155008 (Synonyms: adenosine-derived inhibitor, VER155008, VER-155008) |
Catalog No.GC16966
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Synonyms | adenosine-derived inhibitor, VER155008, VER-155008 | ||
| Chemical Name | 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 | ||
| Formula | C25H23Cl2N7O4 | M.Wt | 556.4 |
| Solubility | ≥ 27.8mg/mL in DMSO, ≥ 4.65 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -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 | 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 |
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: >99.50% 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.)