VER-82576
Based on 5 publication(s) in Google Scholar
VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.76%
- CAS 番号: 847559-80-2
- 分子式: C21H23Cl2N5O2S
- 分子量:480.41
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Customer Validation & Images
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RT-PCR
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生物活性
製品説明
IC50 & Target
[1]|
HSP90β 58 nM (IC50) |
GRP94 4.1 μM (IC50) |
TRAP-1 5.5 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | GI50 |
0.038 μM
Compound: 34d
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Growth inhibition of human A375 cells after 24 hrs by SRB assay
Growth inhibition of human A375 cells after 24 hrs by SRB assay
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[PMID: 19610616] |
| BT-474 | GI50 |
0.053 μM
Compound: 34d
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Growth inhibition of human BT474 cells after 24 hrs by SRB assay
Growth inhibition of human BT474 cells after 24 hrs by SRB assay
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[PMID: 19610616] |
| HCT-116 | GI50 |
0.12 μM
Compound: 34d
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Growth inhibition of human HCT116 cells after 24 hrs by SRB assay
Growth inhibition of human HCT116 cells after 24 hrs by SRB assay
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[PMID: 19610616] |
| MCF7 | GI50 |
0.118 μM
Compound: 34d
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Growth inhibition of human MCF7 cells after 24 hrs by SRB assay
Growth inhibition of human MCF7 cells after 24 hrs by SRB assay
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[PMID: 19610616] |
| PC-3M | GI50 |
1.05 μM
Compound: 34d
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Growth inhibition of human PC3M cells after 24 hrs by SRB assay
Growth inhibition of human PC3M cells after 24 hrs by SRB assay
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[PMID: 19610616] |
| T-24 | GI50 |
0.145 μM
Compound: 34d
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Growth inhibition of human T24 cells after 24 hrs by SRB assay
Growth inhibition of human T24 cells after 24 hrs by SRB assay
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[PMID: 19610616] |
| U-87MG ATCC | GI50 |
0.857 μM
Compound: 34d
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Growth inhibition of human U87MG cells after 24 hrs by SRB assay
Growth inhibition of human U87MG cells after 24 hrs by SRB assay
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[PMID: 19610616] |
体外実験
VER-82576 (NVP-BEP800) is a potent and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β and is >70-fold selective against Grp94 and Trap-1, with IC50s of 4.1 ± 1.1 and 5.5 ± 0.48 μM. VER-82576 potently inhibits the proliferation of tumor cells, with GI50s ranging from 38 nM in A375 cells to 1050 nM in PC3 cells, with an average GI50 of 245 nM. VER-82576 (250-1250 nM) depletes client proteins in human cancer cell lines in vitro[1]. VER-82576 (NVP-BEP800; 200 nM) shows no significant effect on the ionizing radiation (IR) dose-response curves of A549 cells, and is less toxic to SNB19 cells. VER-82576 in combination with IR results in more severe DNA damage in both A549 and SNB19 cell lines than each treatment alone and also protracts the kinetics of DNA damage repair in SNB19 cells[2]. VER-82576 (NVP-BEP800; 0.05, 0.1 or 0.2 μM) dose-dependently decreases the viability and induces apoptosis of glioblastoma cells. VER-82576 (0.2 μM) suppresses the expression of IKKβ protein but does not alter the levels of IKKβ mRNA in T98G cells. VER-82576 (0.2 μM) suppresses the expression of heat shock protein 70[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
化学情報
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CAS 番号 847559-80-2
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性状 Solid
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分子量 480.41
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分子式 C21H23Cl2N5O2S
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Color White to off-white
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SMILES
O=C(C1=CC2=C(N=C(N=C2S1)N)C3=CC(OCCN4CCCC4)=C(C=C3Cl)Cl)NCC
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別名
NVP-BEP800
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Theranostics
Hsp90 inhibitor HSP990 in very low dose upregulates EAAT2 and exerts potent antiepileptic activity. [Abstract]2020 Jul 9;10(18):8415-8429. PMID: 32724478 -
Cell Rep
DUSP4 promotes esophageal squamous cell carcinoma progression by dephosphorylating HSP90β. [Abstract]2023 May 2;42(5):112445. PMID: 37141098 -
Int J Mol Sci
2023 Nov 4;24(21):15971. PMID: 37958953
VER-82576 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Nov 4;24(21):15971. [Abstract]
The relative mRNA level of the TGEV M gene was determined by qRT-PCR treated with the HSP90 inhibitors VER-82576 (0, 250, 500, 1000 nM).
VER-82576 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Nov 4;24(21):15971. [Abstract]
N protein level was determined by Western blot treated with the HSP90 inhibitors VER-82576 (0, 250, 500, 1000 nM).
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J Biol Chem
2024 Jan;300(1):105536. PMID: 38092149 -
Vet Microbiol
HSP90 inhibitors 17-AAG and VER-82576 inhibit porcine deltacoronavirus replication in vitro. [Abstract]2022 Feb:265:109316. PMID: 34954542
溶剤 & 溶解度
体外:
DMSO : 6.2 mg/mL (12.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
純度とドキュメンテーション
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データシート (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Massey AJ, et al. Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800. Mol Cancer Ther. 2010 Apr;9(4):906-19. [Content Brief]
[2]. Niewidok N, et al. Hsp90 Inhibitors NVP-AUY922 and NVP-BEP800 May Exert a Significant Radiosensitization on Tumor Cells along with a Cell Type-Specific Cytotoxicity. Transl Oncol. 2012 Oct;5(5):356-69. Epub 2012 Oct 1. [Content Brief]
[3]. Wu J, et al. Irradiation facilitates the inhibitory effect of the heat shock protein 90 inhibitor NVP-BEP800 on the proliferation of malignant glioblastoma cells through attenuation of the upregulation of heat shock protein 70. Exp Ther Med. 2014 Sep;8(3) [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0816 mL | 10.4078 mL | 20.8156 mL | 52.0389 mL |
| 5 mM | 0.4163 mL | 2.0816 mL | 4.1631 mL | 10.4078 mL | |
| 10 mM | 0.2082 mL | 1.0408 mL | 2.0816 mL | 5.2039 mL |
VER-82576 関連分類
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