Kobe0065
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.
Kobe0065是Ras的小分子抑制剂,对H-Ras.GTP 结合c-Raf-1的Ki值为46 μM [1].
Kobe0065是通过硅片筛选方法筛选出的一种化合物,作为Ras-Raf相互作用的高效抑制剂.其能有效抑制M-Ras.GTP和H-Ras.GTP结合c-Raf-1的Ras结合域.在NIH 3T3细胞中,Kobe0065也能剂量依赖性抑制H-RasG12V结合c-Raf-1,IC50值约为10 μM.此外,20 μM Kobe0065有效抑制Raf下游激酶的磷酸化,包括MEK和ERK.在转染H-rasG12V 的NIH 3T3细胞中,Kobe0065抑制集落形成,IC50值为0.5 μM.Kobe0065对其它具有活化的Ras原癌基因的癌细胞也具有效应,如PANC-1(K-rasG12V)\HT1080 (N-rasQ61L)和HCT116 (H-rasG13D).而且,在SW480异种移植小鼠中,按80 mg/kg的剂量给予Kobe0065能够抑制40-50%的肿瘤生长.此效应在剂量高达160 mg/kg时变得更加明显[1].
参考文献：
[1] Shima F, Yoshikawa Y, Ye M, et al. In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras–effector interaction. Proceedings of the National Academy of Sciences, 2013, 110(20): 8182-8187.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 449.79 |
| Cas No. | 436133-68-5 |
| Formula | C15H11ClF3N5O4S |
| Solubility | ≥23.85 mg/mL in DMSO; insoluble in H2O; ≥3.24 mg/mL in EtOH with ultrasonic |
| Chemical Name | N-(3-chloro-4-methylphenyl)-2-(2,6-dinitro-4-(trifluoromethyl)phenyl)hydrazinecarbothioamide |
| SDF | Download SDF |
| Canonical SMILES | ClC1=CC(NC(NNC2=C([N+]([O-])=O)C=C(C(F)(F)F)C=C2[N+]([O-])=O)=S)=CC=C1C |
| 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
