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- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
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货期：1-2天
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MedChemExpress LLC
- 规格：
10 mM * 1 mL/1 mg/5 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥ |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥2200.0 |
| 规格： | 5 mg | 产品价格： | ￥5500.0 |
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PR-924
CAS No. : 1416709-79-9
MCE 国际站：PR-924
产品活性：PR-924 是一种选择性三肽环氧酮免疫蛋白酶亚单位 LMP-7 的抑制剂，IC50 为 22 nM。PR-924 共价修饰蛋白酶体的 N 端苏氨酸活性位点。PR-924 在多发性骨髓瘤细胞中抑制细胞生长并触发凋亡 (apoptosis)，并具有抗肿瘤活性。
研究领域：Metabolic Enzyme/Protease | Apoptosis
作用靶点：Proteasome | Apoptosis
In Vitro: PR-924 (1-20 μM; 24-72 hours; MM.1S, MM.1R, RPMI-8226, KMS12, LR-5, DOX40, INA-6, OPM1 and OPM2 cells) treatment significantly decreases the viability of all the MM cell lines in a time-and dose-dependent manner (IC 50 range for cell lines: 3-7 μM for 48 h).
PR-924 (3 μM; 48 hours; MM.1S and MM.1R cells) treatment triggers apoptosis in MM cells.
PR-924 (3 μM; 48 hours; MM.1S and MM.1R cells) treatment triggers activation of caspase-3, caspase-8 and caspase-9, and significantly down-regulated the expression of Bcl-2 protein, without altering Bax or MCL-1 protein levels.
PR-924 induces BID cleavage and its translocation to mitochondria, as well as cyto-c release BID, a proapoptotic BH-3 family protein, is linked to mitochondria-mediated apoptotic signaling pathways via cyto-c release.
In Vivo: PR-924 (6 mg/kg; intravenous injection; twice a week; for 21 days; CB-17 SCID-mice) treatment significantly inhibits tumour growth in human plasmacytoma xenografts.
PR-924 treatment significant reduces the shIL-6R levels in SCID-hu model. Treatment of tumour-bearing mice with PR-924, prolongs survival.
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文献和实验身高组段（1） 频数（2） 累计频数*（3） 累计频率（%）（4） 概率单位（5） 162～ 1 1 0.9 2.63 164～ 4 5 4.5 3.30 166～ 9 14 12.7 3.86 168～ 13 27 24.5 4.31 170～ 19 46 41.8 4.79 172～ 27 73 66.4 5.42 174～ 16 89 80.9 5.87 176～ 8 97 88.2 6.19 178～ 8 105 95.5 6.70 180～ 3 108 98.2
7.91g 15.82g 39.55g H2 O mQ 85.394 46.245ml 92.49ml 231.23ml 1000ml/ 158.2g/M 1M 1.5M (AcO)2 Ca [g] 158.2 237.3 H2 O [ml] 924.9 884.1 %(w/w) 14.606 21.161 H2 O
硼（boron） B 5 10.81 溴（bromine） Br 35 79.90 镉（cadmium） Cd 48 112.41
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