NI-57
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- CAS号:
- 1883548-89-7
- 英文名:
- NI-57
- 英文别名:
- CS-2795;NI57;NI 57;BRPF inhibitor NI57;Inhibitor,inhibit,NI 57,NI-57,NI57,Epigenetic Reader Domain;Benzenesulfonamide, 4-cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)-2-methoxy-
- 中文名:
- NI-57
- 中文别名:
- 化合物NI-57
- CBNumber:
- CB03156586
- 分子式:
- C19H17N3O4S
- 分子量:
- 383.42
- MOL File:
- 1883548-89-7.mol
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NI-57化学性质
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沸点:
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580.1±60.0 °C(Predicted)
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密度:
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1.43±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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≤25mg/ml in DMSO;30mg/ml in dimethyl formamide
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形态:
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crystalline solid
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酸度系数(pKa):
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7.89±0.20(Predicted)
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颜色:
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White to off-white
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NI-57性质、用途与生产工艺
NI-57 为溴结构域和植物同源锌指结构域 (BRPF) 蛋白家族的抑制剂,对 BRPF1,BRPF2 (BRD1) 和 BRPF3 的 IC50 值分别为 3.1,46 和 140 nM。
IC50: 3.1 nM (BRPF1), 46 nM (BRPF2 (BRD1)), 140 nM (BRPF3)
NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF), with IC
50
s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively. NI-57 binds the BRD of BRPF1 with a K
d
of 31 ± 2 nM, BRD1 with a K
d
of 110 ± 13 nM, and BRPF3 with a K
d
of 410 ± 47 nM, whereas binding to BRD9 is weaker (K
d
1000 ± 130 nM) measured by isothermal titration calorimetry. NI-57 shows less active effect on BRD9 (IC
50
, 520 nM) and BRD4 (BD1) (IC
50
, 3700 nM), TRIM24 (IC
50
, 1600 nM). NI-57 also inhibits BRPF BRDs in the nucleus, but shows little effect on the proliferation of many cancer cell lines with GI
50
s 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%.
NI-57 has favorable oral bioavailability in mice.
NI-57
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更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2022/04/29 | S0554 | NI-57 NI-57 | 1883548-89-7 | 25mg | 11048.3元 |
1883548-89-7, NI-57 相关搜索:
- 化合物NI-57
- 1883548-89-7
- Inhibitor,inhibit,NI 57,NI-57,NI57,Epigenetic Reader Domain
- Benzenesulfonamide, 4-cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)-2-methoxy-
- NI57;NI 57
- CS-2795
- BRPF inhibitor NI57