AUY922 (NVP-AUY922)
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.
AUY922（NVP-AUY922）是一种有效的、新合成的间苯二酚异恶唑酰胺（resorcinylic isoxazole amide）类热休克蛋白90（HSP90，heat shock protein 90）的小分子抑制剂，分子式为C26H31N3O5，分子量为465.5，对Hsp90有高亲和性，可以与Hsp90 N端结构域的ATP结合位点相结合[1][2]。HSP90是一种分子伴侣，对调节细胞生长和存活的关键蛋白的稳定性是至关重要的。NVP-AUY922可以有效抑制胃癌细胞的增殖，GI50值约为2-40 nmol/L，也可以显著诱导生长因子受体和其它目标蛋白的降解[3]。
参考文献：
[1] Suzanne A. E, Andy M, Florence I. R, et al. NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis. Cancer Res. 2008, 68. 2850-2860.
[2] Tsuyoshi U, Kazunori T, Shinichi T, Midori A, Munenori T, et al. Strong anti-tumor effect of NVP-AUY922, a novel Hsp90 inhibitor, on non-small cell lung cancer. Lung Cancer. 2012, 76. 26-31.
[3] Kyung-Hun L, Ju-Hee L, Sae-Won H, Seock-Ah I, et al. Antitumor activity of NVP-AUY922, a novel heat shock protein 90 inhibitor, in human gastric cancer cells is mediated through proteasomal degradation of client proteins. Cancer Sci. 2011, 102. 1388–1395.
- 1. Ying Zhang, Garrett C. VanHecke, et al. "Sulfoxythiocarbamate S-4 inhibits HSP90 in human cutaneous squamous cell carcinoma cells." Eur J Pharmacol. 2020 Oct 6;889:173609. PMID:33031796
- 2. Jason E. Gestwicki, Co-Chair, et al. "Strategies and functional consequences of inhibiting protein-protein interactions." University of Michigan. 2016.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 465.5 |
| Cas No. | 747412-49-3 |
| Formula | C26H31N3O5 |
| Synonyms | VER-52296, AUY-922, AUY 922 |
| Solubility | ≥23.27 mg/mL in DMSO; insoluble in H2O; ≥100.6 mg/mL in EtOH with ultrasonic |
| Chemical Name | (5Z)-N-ethyl-5-(4-hydroxy-6-oxo-3-propan-2-ylcyclohexa-2,4-dien-1-ylidene)-4-[4-(morpholin-4-ylmethyl)phenyl]-2H-1,2-oxazole-3-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CCNC(=O)C1=C(C(=C2C=C(C(=CC2=O)O)C(C)C)ON1)C3=CC=C(C=C3)CN4CCOCC4 |
| 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。 |
| 细胞实验[1]： | |
|
细胞系 |
NCI-N87、SNU-216和SNU-484细胞 |
|
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
200 nM；24 h |
|
应用 |
AUY922减少客户蛋白的表达，减少受体酪氨酸激酶的表达，比如VEGFR1、2、3和PDGFR-α，以剂量依赖的方式减少Akt和磷酸化Akt。除此之外，在NCI-N87细胞中，AUY922减少HER-2的表达。 |
| 动物实验[2]： | |
|
动物模型 |
BT-474乳腺癌异种移植无胸腺Nude-nu裸鼠 |
|
剂量 |
30 mg/kg；静脉给药 |
|
应用 |
在2和6小时的时间点观察到AUY922对HSP90-p23复合体解离的显著效应。在BT-474异种移植模型中，AUY922处理后的16和24小时观察到HSP90-p23复合体的重新装配，AUY922也诱导磷酸化AKT水平的下降。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Lee K H, Lee J H, Han S W, et al. Antitumor activity of NVP‐AUY922, a novel heat shock protein 90 inhibitor, in human gastric cancer cells is mediated through proteasomal degradation of client proteins. Cancer science, 2011, 102(7): 1388-1395. [2] Jensen M R, Schoepfer J, Radimerski T, et al. NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models. Breast Cancer Res, 2008, 10(2): R33. |
|
| 描述 | AUY922 (NVP-AUY922)是一种高效的HSP90抑制剂，作用于HSP90α/β，IC50值为13 nM /21 nM。 | |||||
| 靶点 | HSP90α | HSP90β | ||||
| IC50 | 13 nM | 21 nM | ||||
质量控制和MSDS
- 批次:
化学结构
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