Cereblon modulator 1 MCE | PROTAC
- 公司名稱 MedChemExpress LLC
- 品牌 MedChemExpress (MCE)
- 型號 Cereblon modulator 1
- 產(chǎn)地 美國
- 廠商性質 生產(chǎn)廠家
- 更新時間 2021/7/26 10:32:06
- 訪問次數(shù) 532
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CAS | 1860875-51-9 | 純度 | 99.51% |
---|---|---|---|
分子量 | 461.85 | 分子式 | C??H??ClF?N?O? |
供貨周期 | 現(xiàn)貨 | 規(guī)格 | 電詢 |
貨號 | HY-130800 | 應用領域 | 生物產(chǎn)業(yè) |
主要用途 | 科研 |
MCE 的所有產(chǎn)品僅用作科學研究或藥證申報,,我們不為任何個人用途提供產(chǎn)品和服務。
Cereblon modulator 1
產(chǎn)品活性:Cereblon modulator 1 (compound F) 是一種 cereblon (CRBN) E3 連接酶調節(jié)劑。Cereblon modulator 1 與 CRBN 特異性結合,,從而影響泛素 E3 連接酶復合物的活性,。 這導致某些底物蛋白的泛素化并誘導蛋白酶體介導的某些轉錄因子的降解,包括 Ikaros (IKZF1) 和 Aiolos (IKZF3),。
研究領域:PROTAC | Apoptosis
作用靶點:Ligand for E3 Ligase | Apoptosis
In Vitro: A different CRBN-binding compound, Cereblon modulator 1 (compound F), that demonstrates anti-proliferative activity in non-AML hematological cancer cell lines (such as multiple myeloma) does not inhibit cell growth in any of the 11 AML cell lines tested, including the ten cell lines that are sensitive to the growth inhibitory activity of Compound D. However, when excess Cereblon modulator 1 is added to KG-1 AML cell cultures in the presence of Compound D, the anti-proliferative activity of Compound D is reduced, presumably due to competition for binding of Compound D to CRBN. The relative impact of Cereblon modulator 1 on the anti-proliferative effect of Compound D progressively increased with increasing concentrations of Cereblon modulator 1. In the presence of 100 µΜ Cereblon modulator 1, the potency of Compound D in inhibiting cell growth reduced by approximately 60-fold, and the potency of Compound D in inducing apoptosis reduced by approximately 40-fold.
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