中文名称: NI-57
英文名称: NI-57
CAS No: 1883548-89-7
分子式: C19H17N3O4S
分子量: 383.42
N10663 NI-57 ≥98% (psaitong)
包装规格:
50mg in glass bottle
溶解性:
溶于DMSO(100mg/mL 超声)
产品描述:

基本信息

产品编号:N10663

产品名称:NI-57

CAS:

1883548-89-7

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C19H17N3O4S

溶于液体

-80℃

六个月

分子量:

383.42

-20℃

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

'mg/mL

Ethanol

 

Water

 

体内(现配现用)

 

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.6081mL

13.0405mL

26.0811mL

5mM

0.5216mL

2.6081mL

5.2162mL

10mM

0.2608mL

1.3041mL

2.6081mL

 

生物活性

产品描述

一种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 140nM。

靶点/IC50

3.1nM (BRPF1),46nM (BRPF2 (BRD1)),140nM (BRPF3)

 

体外研究

NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF), with IC50s of 3.1, 46 and 140nM for BRPF1, BRPF2 (BRD1) and BRPF3,respectively. NI-57 binds the BRD of BRPF1 with a Kd of 31 ± 2nM, BRD1 with a Kd of 110±13nM, and BRPF3 with a Kd of 410±47nM, whereas binding to BRD9 is weaker (Kd 1000±130nM) measured by isothermal titration calorimetry.NI-57 shows less active effect on BRD9 (IC50, 520nM) and BRD4 (BD1 (IC50,3700nM), TRIM24 (IC50,1600nM). NI-57 also inhibits BRPF BRDs in the nucleus, but shows little effect on the proliferation of many cancer cell lines with GI50s of 10.4μM (NCI-H1703 cells),14.7μM (DMS114), 15.6μM (HRA-19), and 16.6μM (RERF-LC-Sq1). Furthermore,Inhibition on BRPF1 of NI-57 (10μM) reduces the gene expression of CCL-22 by 27.7 ± 9.4%.

体内研究

NI-57 has favorable oral bioavailability in mice.

 

推荐实验方法(仅供参考)

激酶实验:

All reagents are diluted in the recommended buffer (50mMHEPES, 100mM NaCl, 0.1% BSA;pH=7.4) supplemented with 0.05% CHAPS and allowed to equilibrate to room temperature prior to addition to plates. 4mL of HIS-tagged protein is added to low-volume 384-well plates,followed by 4mL of either buffer, non-biotinylated peptide, solvent or compounds (NI-57,etc.). Plates are sealed and incubated at room temperature for 30 minutes, before the addition of 4mL biotinylated peptide, resealing and incubation for a further 30 minutes. 4mL of streptavidin-coated donor beads (25µg/mL) and 4 µL of nickel chelate acceptor beads (25µg/mL) are then added under low light conditions. Plates are foil sealed to protect from light, incubated at room temperature for 60 minutes and read on a PHERAstar FS plate reader using an AlphaScreenTM 680 excitation/570 emission filter set. IC50s are calculated in GraphPad Prism 5.Results for compounds (NI-57, etc.) dissolved in DMSO are normalised against corresponding DMSO controls prior to IC50 determination, which are given as the final concentration of compound in the 20µL reaction volume.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

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    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):