HSP990 (NVP-HSP990)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
HSP990（NVP-HSP990）是一种有效的和选择性的HSP90抑制剂，作用于Hsp90α、Hsp90β和Grp94，IC50值分别为0.6、0.8和8.5 nM[1]。
热休克蛋白90（HSP90）是一种伴侣蛋白，稳定蛋白抵抗热应力，协助蛋白正确折叠，帮助蛋白降解。此外，HSP90稳定肿瘤生长所需的蛋白。
HSP990（NVP-HSP990）是一种有效的和选择性的HSP90抑制剂，与Hsp90 N端的ATP结合域相结合。NVP-HSP990抑制90%的TRAP1 ATPase活性，IC50值为320 nM。在GTL-16细胞中，NVP-HSP990以浓度和时间依赖的方式对Hsp90-p23复合体进行去稳定化。NVP-HSP990也减少c-Met和诱导Hsp70，EC50值分别为37 nM和20 nM。NVP-HSP990抑制ERK和AKT的磷酸化，EC50值分别为11和6 nM，从而抑制ERK和AKT的激活。在5个人肿瘤细胞系中，NVP-HSP990抑制细胞生长，GI50值介于4-40 nM之间[1]。在胶质瘤起始细胞中，NVP-HSP990以剂量依赖的方式抑制细胞生长，IC50值介于10-500 nM之间，减少CDK2和CDK4，从而扰乱细胞周期控制[2]。
在GTL-16胃癌小鼠模型中，NVP-HSP990具有抗肿瘤效应[1]。
参考文献：
[1]. Menezes DL, Taverna P, Jensen MR, et al. The novel oral Hsp90 inhibitor NVP-HSP990 exhibits potent and broad-spectrum antitumor activities in vitro and in vivo. Mol Cancer Ther, 2012, 11(3): 730-739.
[2]. Fu J, Koul D, Yao J, et al. Novel HSP90 inhibitor NVP-HSP990 targets cell-cycle regulators to ablate Olig2-positive glioma tumor-initiating cells. Cancer Res, 2013, 73(10): 3062-3074.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 379.39 |
| Cas No. | 934343-74-5 |
| Formula | C20H18FN5O2 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥12.3 mg/mL in DMSO |
| Chemical Name | (7R)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one |
| SDF | Download SDF |
| Canonical SMILES | CC1=NC(=NC2=C1C(=O)NC(C2)C3=C(C=C(C=C3)F)C4=NC(=CC=C4)OC)N |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
