| CAS NO: | 1624602-30-7 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Cas No. | 1624602-30-7 |
| 化学名 | 7-chloro-4-(4-((2,4-dinitrophenyl)sulfonyl)piperazin-1-yl)quinoline |
| 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 |
| 分子式 | C19H16ClN5O6S |
| 分子量 | 477.88 |
| 溶解度 | ≥ 45.55mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | VR23 is an effective proteasome inhibitor, with IC50 values of 3 μmol/L, 1 nmol/L, and 50-100 nmol/L to inhibit activities of caspase-like proteasomes, trypsin-like proteasomes, and chymotrypsin-like proteasomes, respectively [1]. As a regulator, the ubiquitin-proteasome system is important for cell growth and apoptosis [2]. The ubiquitin-proteasome pathway is critical in the regulated degradation of proteins involved in tumor growth and cell cycle control [3]. Treatment with VR23 made cancer cells undergo an abnormal centrosome amplification cycle. This cycle was caused by the accumulation of ubiquitinated cyclin E. Bortezomib is clinically approved as a chymotrypsin-like proteasome inhibitor. VR23 in combinations with bortezomib, caused a synergistic effect in killing multiple myeloma cells. This synergistic effect was also effective to myeloma cells resistant to bortezomib [1]. In vivo, VR23 was effective in controlling metastatic breast cancer cells and multiple myelomas [1]. In engrafted animals, the treatment with VR23 at 30 mg/kg twice per week for three weeks inhibited tumor growth effectively. Following 24 hours pre-treatment with paclitaxel at 20mg/kg/week, the administration of VR23 enhanced the anti-tumor activity of paclitaxel by 70%. Histological data showed that VR23 substantially decreased mitotic index, inhibited tumor infiltration into surrounding tissues and remarkably reduced tumor cell proliferation and angiogenesis [4]. References: |
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