Oprozomib
作者：齐岳
发布时间：2023-09-08
09:03:28
点击数：
产品名称：Oprozomib
产品描述：
| 产品描述 | Oprozomib (ONX 0912) , an inhibitor for CT-L activity of 20S proteasome β5（IC50=36 nM）/LMP7（IC50=82 nM）, is orally bioavailable. Oprozomib also has potential antineoplastic activity. |
| 靶点活性 | 20S proteasome LMP7:82 nM, 20S proteasome β5:36 nM |
| 体外活性 | 在多种人类肿瘤移植瘤和小鼠同系模型中,Oprozomib能够抑制>80％蛋白酶,诱导抗肿瘤反应.Oprozomib经过重复口服后,在动物的大多数组织具有良好的安全性与耐受性. |
| 体内活性 | Oprozomib具有抗MM活性,可以抑制MM细胞的迁移和血管生成。Oprozomib也能抑制caspase-8,caspase-9,caspase-3和PARP的激活。 |
| 激酶实验 | ELISA-based active site binding assay: Samples (lysed cells or tissue homogenates) are treated for 1 h at room temperature with the biotinylated active site probe PR-584 (5-15 μM). Samples are denatured by addition of SDS (0.9% final) and heating to 100 °C for 5 min. The denatured samples are transferred to a 96-well or 384-well filter plat, mixed with streptavidin-sepharose beads (2.5-5 μL packed beads/well), and incubated for 1 h at room temperature on a plate shaker. The beads are washed 5 times with 100-200 μL /well of ELISA buffer (PBS, 1% bovine serum albumin, 0.1% Tween-20) by vacuum filtration. The beads are incubated overnight at 4 °C on a plate shaker with the following antibodies recognizing the six catalytic subunits diluted into ELISA buffer: β5, β1, and β2 diluted 1:3000, LMP7 and LMP2 diluted 1:5000, and MECL-1 diluted 1:1000. The beads are washed 5 times with 100-200 μL /well of ELISA buffer and incubated with HRP-conjugated secondary antibody diluted 1:5000 in ELISA buffer and incubated 2 h at room temperature on a plate shaker. The beads are washed 5 times with 100-200 μL /well of ELISA buffer and developed for chemiluminsecence signal using the supersignal ELISA pico substrate following the manufacturer's instructions. Luminescence is measured on a plate reader and converted to ng of proteasome or μg/ml of lysate by comparison with 20S proteasome or untreated cell lysate standard curves. For proteasome inhibitor studies, active site probe binding values are expressed as the percent of binding relative to DMSO treated cells. |
| 细胞实验 | MTT assay(Only for Reference) |
| 别名 | ONX 0912, 奥泼佐米, PR-047 |
| 分子量 | 532.61 |
| 分子式 | C25H32N4O7S |
| CAS No. | 935888-69-0 |
存储
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
DMSO: 93 mg/mL (174.6 mM)
Ethanol: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
联系我们：
邮箱：2519696869@qq.com
QQ: 2519696869
电话：18066853083
微信：18066853083
公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
主营产品：COF、MOF单体系列：三蝶烯衍生物、金刚烷衍生物、四苯甲烷衍生物、peg、上转换、石墨烯、光电材料、点击化学、凝集素、载玻片、蛋白质交联剂、脂质体、蛋白、多肽、氨基酸、糖化学等。
