VER 155008 (Synonyms: adenosine-derived inhibitor, VER155008, VER-155008) |
カタログ番号GC16966
One-Click Copy Product Info
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VER 155008は強力で、アデノシン由来の熱ショックタンパク質70（Hsp70）ファミリーの阻害剤であり、Hsp70、熱ショックコグネイトタンパク質70（Hsc70）とグルコース調節タンパク質78（Grp78）に対するIC50値はそれぞれ0.5μM、2.6μMと2.6μMである。
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は強力で、アデノシン由来の熱ショックタンパク質70（Hsp70）ファミリーの阻害剤であり、Hsp70、熱ショックコグネイトタンパク質70（Hsc70）とグルコース調節タンパク質78（Grp78）に対するIC50値はそれぞれ0.5μM、2.6μMと2.6μMである[1]。VER 155008はHsp70 ATPaseの活性を阻害し、細胞周期停止、アポトーシス、腫瘍特異性細胞死を誘発することでその作用を発揮し、通常は抗癌（例：前立腺癌や乳癌など）と抗ウイルス研究に使われる[2,3,4]。
In vitro（体外）実験で、VER 155008（20μM）で211HとH28細胞を48時間処理したところ、G1期で細胞の割合が著しく増えた（211H細胞で69.9%から82.7%に；H28細胞で77%から85.2%に）[5]。VER 155008（25μM）でA549とH1975細胞を2日間処理したところ、5-bromo-2'-deoxyuridine（BrdU）陽性細胞の割合を著しく低下させ、細胞の増殖の阻害を示唆した[6]。
In vivo（体内）実験で、PC12腫瘍を持つヌードマウスにVER 155008（40mg/kg；毎日一回）を2週間腹腔内注射したところ、腫瘍の体積と重量が著しく減少した[7]。VER 155008（25mg/kg）をBALB/cマウスに単回静脈内注射したところ、血漿半減期が0.6時間で、クリアランス率は49mL/min/kgであった[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.
| 細胞実験[1]: | |
細胞株 | A549とH1975細胞 |
準備方法 | A549とH1975細胞を25μM VER 155008で2日間処理し、その後は10μM BrdUと1時間インキュベートした。BrdU陽性細胞を抗BrdU FITC抗体で検出した。 |
反応条件 | 25μM；2日間 |
アプリケーション | VER 155008の処理は、BrdU陽性細胞の割合を著しく減らし、細胞の増殖を阻害した。 |
| 動物実験 [2]: | |
動物モデル | PC12腫瘍細胞を異種移植したヌードマウス |
準備方法 | PC12細胞（1×106個の細胞）をヌードマウスに皮下注射した。腫瘍が80-150mm3に達した時、マウスにVER 155008（40mg/kg）を2週間、毎日一回腹腔内注射した。腫瘍の体積を毎日測定した。 |
投与形態 | 40mg/kg；毎日一回；2週間；腹腔内注射 |
アプリケーション | VER 155008の処理は、腫瘍の体積を著しく減らした。 |
References: | |
| Cas No. | 1134156-31-2 | SDF | |
| 同義語 | 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 |
| 溶解度 | ≥ 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 |
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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
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- 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.)