VR23
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.
VR23是一种有效的蛋白酶抑制剂，抑制caspase样蛋白酶、胰蛋白酶样蛋白酶和胰凝乳酶样蛋白酶的活性的IC50值分别为3 μmol/L、1 nmol/L和50-100 μmol/L[ 1]。
泛素-蛋白酶体系统作为调节剂在细胞生长和细胞凋亡中发挥重要作用[2]。泛素-蛋白酶体系统在调节参与肿瘤生长和细胞周期调控的蛋白的降解中起到关键作用[3]。
VR23使癌细胞中心体扩增周期发生异常。这个周期是由泛素化细胞周期蛋白E的累积引起的，Bortezomib是临床批准的胰凝乳蛋白酶样蛋白酶体抑制剂。 VR23与bortezomib组合使用，在杀死多发性骨髓瘤细胞时产生协同效应。这种协同作用对具有bortezomib抗性的骨髓瘤细胞有效[1]。
在体内，VR23有效地控制转移性乳腺癌细胞和多发性骨髓瘤[1]。在移植的动物中，30 mg/kg剂量的VR23每周两次，连续三个星期，有效地抑制肿瘤的生长。通过20 mg/kg/week的紫杉醇预治疗24小时，VR23将紫杉醇的抗肿瘤活性提高70％。组织学数据表明，VR23较大幅度降低有丝分裂指数，抑制肿瘤浸润到周围组织，显著地减少了肿瘤细胞增殖和血管生成[4]。
参考文献：
[1]. Pundir S, Vu HY, Solomon VR, et al. VR23: A Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E-Mediated Centrosome Amplification. Cancer research, 2015, 75(19): 4164-4175.
[2]. Almond JB, Cohen GM. The proteasome: a novel target for cancer chemotherapy. Leukemia, 2002, 16(4): 433-443.
[3]. Adams J, Palombella VJ, Sausville EA, et al. Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer research, 1999, 59(11): 2615-2622.
[4]. Vu HYT, Pundir S, Solomon RV, et al. Anticancer effects and mechanism of VR23, a novel chloroquine derivative. Cancer Research, 2014, 74(19 Supplement): 4545-4545.
| Storage | Store at -20°C |
| M.Wt | 477.88 |
| Cas No. | 1624602-30-7 |
| Formula | C19H16ClN5O6S |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥45.55 mg/mL in DMSO |
| Chemical Name | 7-chloro-4-(4-((2,4-dinitrophenyl)sulfonyl)piperazin-1-yl)quinoline |
| SDF | Download SDF |
| Canonical SMILES | ClC1=CC2=C(C(N3CCN(S(C4=C([N+]([O-])=O)C=C([N+]([O-])=O)C=C4)(=O)=O)CC3)=CC=N2)C=C1 |
| 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
