VER-50589
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.
VER-50589是HSP90的高效抑制剂,对HSP90β的IC50值为21 nM [1].
热休克蛋白90(HSP90)是一种伴侣蛋白,能够稳定蛋白抵抗热激,协助蛋白正确折叠和辅助蛋白降解.HSP90也能稳定肿瘤生长所需的蛋白质
VER-50589是HSP90的高效抑制剂.VER-50589抑制重组酵母Hsp90 ATP酶活性,在400 μM ATP时的IC50值为143 nM,在激活剂AHA1存在时抑制重组人HSP90β,IC50值为821 nM.VER-50589也能结合重组人HSP90β,Kd值为4.5 nM.在人癌细胞中,VER-50589表现出抗增殖活性,平均GI50值为78 nM.在CH1人卵巢癌细胞中,VER-50589抑制细胞生长,GI50值为32.7 nM.在HT29细胞中,VER-50589表现出广泛的葡萄糖醛酸化作用,并能将葡萄糖醛酸水平提高50倍,从而引起抗性.在doxorubicin耐受性CH1doxR细胞中,VER-50589表现出与CH1细胞类似的GI50值.在HCT116结肠癌细胞中,VER-50589引起G1和G2/M期停滞.VER-50589也能诱导白细胞郁滞和细胞凋亡[1].
在OVCAR3人卵巢腹水瘤的无胸腺小鼠中,VER-50589完全抑制HSP90.在HCT116结肠癌异种移植小鼠中,VER-50589 (100 mg/kg)能将肿瘤体积降低30%,将肿瘤重量降低26%.VER-50589也能降低ERBB2和C-RAF的表达[1].
参考文献：
[1]. Sharp SY, Prodromou C, Boxall K, et al. Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues. Mol Cancer Ther, 2007, 6(4): 1198-1211.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 388.8 |
| Cas No. | 747413-08-7 |
| Formula | C19H17ClN2O5 |
| Solubility | ≥38.9 mg/mL in DMSO; insoluble in H2O; ≥57.2 mg/mL in EtOH |
| Chemical Name | 5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)isoxazole-3-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CCNC(C1=NOC(C2=CC(Cl)=C(O)C=C2O)=C1C3=CC=C(OC)C=C3)=O |
| 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。 |
| Description | VER-50589是HSP90的高效抑制剂,对HSP90β的IC50值为21 nM. | |||||
| 靶点 | HSP90β | |||||
| IC50 | 21 nM | |||||
质量控制和MSDS
- 批次:
化学结构
