UC2288是一种新型的、具有细胞通透性和口服活性的 p21 衰减试剂 (对 p21 具有相对选择性活性),基于索拉非尼的结构合成。UC2288 在不依赖 p53 的情况下下调 p21 mRNA 的表达,降低 p21 蛋白水平,对 p21 蛋白的稳定性影响很小。


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| Concentration | Treated Time | Description | References | |
| SH-SY5Y cells | 10 µM | 2 hours, 4 hours and 6 hours | Investigate the effect of UC2288 on p21 mRNA and protein levels. Results showed an increase in p21 mRNA levels at 4 hours but no change in the fraction of p21 or p-p21 positive cells. | Front Oncol. 2022 Sep 6;12:906194 |
| Kelly cells | 10 µM | 2 hours, 4 hours and 6 hours | Investigate the effect of UC2288 on p21 mRNA and protein levels. Results showed a decrease in p21 mRNA levels after 2 hours followed by an increase at 4 and 6 hours. Western blot showed reduced p-p21 expression at all time points. | Front Oncol. 2022 Sep 6;12:906194 |
| BCBL1 cells | 5 µM | 24 and 48 hours | To evaluate the effect of UC2288 on PEL cell survival, results showed that UC2288 alone induced cytotoxic effects and further reduced cell survival when combined with Lovastatin. | IUBMB Life. 2021 Jul;73(7):968-977 |
| BC3 cells | 5 µM | 24 and 48 hours | To evaluate the effect of UC2288 on PEL cell survival, results showed that UC2288 alone induced cytotoxic effects and further reduced cell survival when combined with Lovastatin. | IUBMB Life. 2021 Jul;73(7):968-977 |
| MIN6 cells | 2.5 µM | 24 hours | To investigate the effect of UC2288 on apoptosis in MIN6 cells under DNA damage conditions. Results showed that UC2288 inhibited p21 function and significantly increased the frequency of apoptosis in MIN6 cells under DNA damage conditions. | Sci Rep. 2019 Dec 18;9(1):19341 |
| BE(2)-C cells | 10 µM | 24 hours | Investigate the effect of UC2288 on p21 and p-p21 expression. Western blot showed increased p21 expression and decreased p-p21 expression. | Front Oncol. 2022 Sep 6;12:906194 |
| Normal kidney proximal tubule epithelial cell line HK2 | 10 µM | 24 hours | UC2288 markedly decreased p21 protein levels. | Cancer Biol Ther. 2013 Mar;14(3):278-85 |
| Ovarian cancer cell line Hey | 10 µM | 24 hours | UC2288 markedly decreased p21 protein levels. | Cancer Biol Ther. 2013 Mar;14(3):278-85 |
| Renal cell carcinoma cell line ACHN | 10 µM | 24 hours | UC2288 markedly decreased p21 protein levels. | Cancer Biol Ther. 2013 Mar;14(3):278-85 |
| Renal cell carcinoma cell line Caki-1 | 10 µM | 24 hours | UC2288 markedly decreased p21 protein levels. | Cancer Biol Ther. 2013 Mar;14(3):278-85 |
| Renal cell carcinoma cell line 786-O | 10 µM | 24 hours | UC2288 decreased p21 protein levels independently of p53 activity, via transcriptional or post-transcriptional regulation. | Cancer Biol Ther. 2013 Mar;14(3):278-85 |
| 5-8F | 4 µM, 6 µM, 8 µM, 12 µM | 24 hours, 48 hours | To evaluate the inhibitory effect of UC2288 on the proliferation of 5-8F cells, the results showed that UC2288 significantly inhibited cell proliferation in a dose- and time-dependent manner, and the effect was better than that of cisplatin. | J Cancer. 2021 Jan 1;12(4):988-995 |
| CNE-2 | 4 µM, 6 µM, 8 µM, 12 µM | 24 hours, 48 hours | To evaluate the inhibitory effect of UC2288 on the proliferation of CNE-2 cells, the results showed that UC2288 significantly inhibited cell proliferation in a dose- and time-dependent manner. | J Cancer. 2021 Jan 1;12(4):988-995 |
| Amnion Epithelial Cells (AECs) | 20 µM | 48 hours | UC2288, as a p21 inhibitor, was used to block Dex-induced senescence in amnion epithelial cells. Results showed that UC2288 significantly reduced Dex-induced cellular senescence. | Biol Reprod. 2019 Jun 1;100(6):1605-1616 |
| Human erythroid progenitors | 1 µM | 6 days | Partially rescued DNMT1 deficiency-induced cell cycle arrest by inhibiting p21 expression. | Cell Death Differ. 2024 Aug;31(8):999-1012 |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Db/db mice | In vitro treatment | 2.5 µM | 24 hours | To investigate the effect of UC2288 on apoptosis in β-cells of db/db mice under DNA damage conditions. Results showed that UC2288 inhibited p21 function and significantly increased the frequency of apoptosis in β-cells under DNA damage conditions. | Sci Rep. 2019 Dec 18;9(1):19341 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.08mL 0.42mL 0.21mL |
10.38mL 2.08mL 1.04mL |
20.75mL 4.15mL 2.08mL |
|
| CAS号 | 1394011-91-6 |
| 分子式 | C20H18ClF6N3O2 |
| 分子量 | 481.82 |
| SMILES Code | O=C(N[C@H]1CC[C@H](OC2=NC=C(C(F)(F)F)C=C2)CC1)NC3=CC=C(Cl)C(C(F)(F)F)=C3 |
| MDL No. | MFCD28139634 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | ISPSOOYSNVVMMB-UHFFFAOYSA-N |
| Pubchem ID | 60196635 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C |
| 溶解方案 |
DMSO: 50 mg/mL(103.77 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 无水乙醇: 12.5 mg/mL(25.94 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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