- ￥1838 - 5933
- 爱必信(absin)
- 上海
- abs814330
- 2025年07月08日
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- 详细信息
- 技术资料
- 保存条件：
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
- 库存：
99
- 供应商：
爱必信(上海)生物科技有限公司
- CAS号：
1883548-89-7
- 规格：
50mg/10mg
| 规格： | 50mg | 产品价格： | ￥5933.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥1838.0 |
| 公告提醒：爱必信所有产品和服务仅用于科学研究，不用于临床应用及其他用途提供产品和服务（也不为任何个人提供产品和服务）!
抑制剂描述： 产品名称：NI-57 产品别名：见爱必信官网 英文别名：NI-57 靶点：Others CAS：1883548-89-7 纯度：>98% 外观：见爱必信官网 保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. 描述：NI-57 is a potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively, as determined by isothermal titration calorimetry. 溶解性：DMSO : ≥ 83.3 mg/mL (217.26 mM) 体外研究： NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF), with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively. NI-57 binds the BRD of BRPF1 with a Kd of 31 ± 2 nM, BRD1 with a Kd of 110 ± 13 nM, and BRPF3 with a Kd of 410 ± 47 nM, whereas binding to BRD9 is weaker (Kd 1000 ± 130 nM) measured by isothermal titration calorimetry. NI-57 shows less active effect on BRD9 (IC50, 520 nM) and BRD4 (BD1) (IC50, 3700 nM), TRIM24 (IC50, 1600 nM). NI-57 also inhibits BRPF BRDs in the nucleus, but shows little effect on the proliferation of many cancer cell lines with GI50s of 10.4 μM (NCI-H1703 cells), 14.7 μM (DMS114), 15.6 μM (HRA-19), and 16.6 μM (RERF-LC-Sq1). Furthermore, Inhibition on BRPF1 of NI-57 (10 μM) reduces the gene expression of CCL-22 by 27.7 ± 9.4%. 体内研究：NI-57 has favorable oral bioavailability in mice.
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