CCT018159
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.
IC50: 3.2 and 6.6 μM for human Hsp90β and yeast Hsp90, respectively
CCT018159 is an inhibitor of Hsp90.
The molecular chaperone heat shock protein 90 (HSP90) regulates the activation, stability, and biological function of various oncogenic client proteins, such as steroid hormone receptors, kinases, and other proteins.
In vitro: CCT018159 was identified by high-throughput screening inhibiting human HSP90beta with comparable potency to 17-AAG and with similar ATP-competitive kinetics. X-ray crystallographic structures of the yeast Hsp90 complexed with CCT018159 showed binding properties similar to radicicol. The mean cellular GI50 of CCT018159 across a panel of human cancer cell lines, including melanoma, was 5.3 μM. Unlike 17-AAG, the in-vitro antitumor activity of CCT018159 was independent of NQO1/DT-diaphorase and P-glycoprotein expression. The signature of HSP90 inhibition, comprising increased expression of HSP72 protein and depletion of ERBB2, CDK4, C-RAF, and mutant B-RAF, was indicated in human cancer cell lines treated with CCT018159 [1].
In vivo: In human tumor xenografts including SKMEL 28 melanoma cells, CCT018159 was found to induce the expression of Hsp72 as well as ERBB2, Cdk4 and dc-Raf [1].
Clinical trial: Up to now, CCT018159 is still in the preclinical development stage.
Reference:
[1] S. Y. Sharp, K. Boxall, M. Rowlands, et al. In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors. Cancer Research 67(5), 2206-2216 (2007).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 352.4 |
Cas No. | 171009-07-7 |
Formula | C20H20N2O4 |
Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
Chemical Name | 4-[4-(2,3-dihydo-1,4-benzodioxin-6-yl)-5-methyl-1H-pyrazol-3-yl]-6-ethyl-1,3-benzenediol |
SDF | Download SDF |
Canonical SMILES | CCc1cc(c(O)cc1O)c1n[nH]c(C)c1c1ccc2OCCOc2c1 |
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。 |