A1874 |
| رقم الكتالوجGC33280 |
A1874 عبارة عن يجند قائم على الجوز (MDM2) و PROTAC مهين لـ BRD4 مع DC50 من 32 نانومتر (تحفيز تدهور BRD4 في الخلايا)فعال في منع تكاثر خطوط الخلايا السرطانية
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2064292-12-0
Sample solution is provided at 25 µL, 10mM.
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A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation[1].
Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) induces a dose-dependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nmol/L and a maximum degradation (Dmax) of BRD4 of 98% of the levels in control (0.1% DMSO-treated) cells[1].
Treatment of HCT116 cells of A1874 (0-10 μM, 24 hours) increases p53 levels in the HCT116 cells and showed dose-dependent p53 stabilization[1].
Reference:
[1]. Hines J, et al. MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53. Cancer Res. 2019 Jan 1;79(1):251-262.
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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