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CAS No.: 1624602-30-7

VR23 Catalog No. CSN17237

Synonyms: VR23

VR23 is a small molecule inhibitor which targets β2 of the 20S proteasome with IC50 of 1 nM and can induce apoptosis of cancer cells via cyclin E–mediated centrosome amplification.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Trypsin-like Proteasomes

IC50:1nM Cannabinoid Receptor 1

IC50:3μM Chymotrypsin-like Proteasomes

IC50:50-100nM
描述Proteasomes play a critical role in regulating the level of cellular proteins and recycling damaged and misfolded proteins, as well as regulating the proliferation and survival of cancer cells. VR23 is a small molecule inhibitor of trypsin-like proteasomes, chymotrypsin-like proteasomes, and caspase-like proteasomes with IC50 values of 1nM, 50-100nM, and 3μM, respectively^[2]. In vitro, VR23 inhibited proliferation of the multiple myeloma cell lines RPMI 8226 and KAS6/1 with IC50 values of 2.94μM and 1.46μM, respectively. VR23 also inhibited proliferation of the noncancer cell lines 184B5 and MCF10A with IC50 values of 9.00μM and 12.30μM, respectively. A clonogenic assay showed that very few MCF7 cells survived for 2 weeks at 1.5μM of VR23. Treatment of MCF7 cells with 2.7μM or 8.0μM of VR23 resulted in 23.7% or 38.2% sub-G1 DNA content within 48 hours after treatment, respectively. These data demonstrated that the noncancer MCF10A was more resistant to VR23 compared to MCF7 cells. In vivo, intraperitoneal administration of VR23 at 30mg/kg twice per week for 3 weeks reduced tumor size in ATH490 athymic mice engrafted with MDA-MB-231 metastatic breast cancer cells. VR23 also reduced tumor size in ATH490 athymic mice engrafted with RPMI8226 multiple myeloma cells, suggesting the antitumor activity of VR23 is not limited to metastatic breast cancer^[2].
作用机制VR23 binds β2 of the 20S proteasome subunit^[2].
参考文献

[1] Pundir S, Vu HY, et ak. VR23: A Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E-Mediated Centrosome Amplification. Cancer Res. 2015 Oct 1;75(19):4164-75.
[2] Pundir S, Vu H, Solomon V R, 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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0926 mL
- 10.4629 mL
- 20.9258 mL
- 5 mM
- 0.4185 mL
- 2.0926 mL
- 4.1852 mL
- 10 mM
- 0.2093 mL
- 1.0463 mL
- 2.0926 mL

技术信息

CAS号

1624602-30-7

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H16ClN5O6S

运输

蓝冰

分子量

477.88

别名

VR23

溶解度

DMSO	30.0 mg/mL (62.8 mM) warming
Water	5.0 mg/mL (10.5 mM) warming
Ethanol	Insoluble

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靶点	Description	IC50
Trypsin-like Proteasomes		IC50:1nM
Cannabinoid Receptor 1		IC50:3μM
Chymotrypsin-like Proteasomes		IC50:50-100nM

VR23 Catalog No. CSN17237

靶点选择性

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