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- 详细信息
- 询价记录
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
VER-155008
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1134156-31-2
- 规格：
10mg/100mg/1mg/5mg/50mg
| 规格： | 10mg | 产品价格： | ￥740.0 |
|---|---|---|---|
| 规格： | 100mg | 产品价格： | ￥4490.0 |
| 规格： | 1mg | 产品价格： | ￥222.0 |
| 规格： | 5mg | 产品价格： | ￥570.0 |
| 规格： | 50mg | 产品价格： | ￥2590.0 |
VER-155008是一种有效的Hsp70家族抑制剂。
| 基本信息 | |
| CAS | No.1134156-31-2 |
| 英文名称 | VER-155008 |
| 别名 | 5'-O-[(4-氰基苯基)甲基]-8-[[(3,4-二氯苯基)甲基]氨基]腺苷 |
| 分子式 | C25H23Cl2N7O4 |
| 分子量 | 556.4 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD18086892 |
| SMILES | O[C@@H]([C@H]([C@H](N1C(NCC2=CC=C(Cl)C(Cl)=C2)=NC3=C1N=CN=C3N)O4)O)[C@H]4COCC5=CC=C(C#N)C=C5 |
| 靶点 | HSP |
| 通路 | Cell Cycle;Metabolic Enzyme&Protease |
| 背景说明 | VER-155008是一种有效的Hsp70家族抑制剂。 |
| 生物活性 | VER-155008 is an inhibitor of Hsp70， with IC50s of 0.5 μM， 2.6 μM， and 2.6 μM for Hsp70， Hsc70 and Grp7， respectively， and with a Kd of 0.3 μM for Hsp70.[1-3] |
| In Vitro | VER-155008 is an inhibitor of Hsc70 and Hsp70， with IC50s of 0.5 μM， 2.6 μM， and 2.6 μM for Hsp70， Hsc70 and Grp7， respectively， a with a Kd of 0.3 μM for Hsp70， but shows no activities against Hsp90， with an IC50 of >200 μM. VER-155008 inhibits the proliferation of a variety of human colon and breast tumor cell lines， such as BT474， MB-468， HCT116 and HT29 cells， with GI50s of 10.4 μM， 14.4 μM， 5.3 μM， and 12.8 μM， respectively. VER-155008 (5-40 μM) induces client protein degradation in HCT116 and BT474 carcinoma cells. VER-155008 also induces apoptosis in human tumor cell lines[1]. VER-155008 (0.05-5 μM) reverses Aβ-induced axonal degeneration in cultured neurons[2]. VER-155008 (10 μM or 25 μM) inhibits Hsp70 and suppresses the proliferation of LNCaP95 cells. VER-155008 also reduces full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7) protein expression[3]. |
| 细胞实验 | VER-155008 (25 mg/kg， i.v.) exhibits plasma clearance in naive female BALB/c mice. VER-155008 (40 mg/kg， i.v.) also shows rapid plasma clearance， and reduces the tumor levels in the HCT116 tumor bearing nude BALB/c mice[1]. VER-155008 (10 μmol/kg/day， i.p.) rescues memory deficits， and reduces axonal swelling associated with amyloid plaques in 5XFAD mice. VER-155008 (89.9 μmol/kg/day， i.p.) penetrates into the brain after administration in 5XFAD mice. VER-155008 also decreases amyloid plaques and PHF-tau associated with amyloid plaques in 5XFAD mice[2]. |
| 细胞实验 | Embryos are removed from a pregnant ddY mouse at 14 days of gestation. Cells are treated with or without 10 μM Aβ25-35 for 3 days， followed by the addition of 0.05， 0.5， or 5 μM VER-155008 or vehicle solution (0.1% DMSO) for 4 days. The Aβ25-35 is incubated at 37°C for 4 days prior to treatment to facilitate aggregation. The cells are fixed with 4% paraformaldehyde and immunostained at 4°C for 24 h with antibodies against the axonal marker， mouse phosphorylated neurofilament heavy subunit， and against the neuronal marker， rabbit microtubule-associated protein 2. Alexa Fluor 488-conjugated goat anti-mouse IgG (1:400) and Alexa Fluor 568-conjugated goat anti-rabbit IgG (1:400) are used as secondary antibodies. Fluorescence images (864.98 μm × 645.62 μm) are captured using a fluorescence microscopy system. The lengths of the pNF-H-positive axons are measured using MetaMorph version 7.8[2]. |
| 动物实验 | Female BALB/c mice are dosed intravenously with 25 mg/kg VER-155008 into the lateral tail vein as a solution in 10% DMSO/5% Tween 80/85% saline (v/v/v). Animals are sacrificed at 5， 15 and 30 min， 1， 2， 4 and 6 h post dose[1]. |
| 数据来源文献 | [1]. Massey AJ， et al. A novel， small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells. Cancer Chemother Pharmacol. 2010 Aug;66(3):535-45. [2]. Yang X， et al. Heat Shock Cognate 70 Inhibitor， VER-155008， Reduces Memory Deficits and Axonal Degeneration in a Mouse Model of Alzheimers Disease. Front Pharmacol. 2018 Jan 30;9:48. [3]. Kita K， et al. Heat shock protein 70 inhibitors suppress androgen receptor expression in LNCaP95 prostate cancer cells. Cancer Sci. 2017 Sep;108(9):1820-1827. |
| 单位 | 瓶 |
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IV0710 VER-155008 细胞周期 索莱宝
￥222 - 4490
