GlpBio

I-BET-762

目录号: GC17073纯度: >99.00%同义词: (4S)-6-(4-氯苯基)-N-乙基-8-甲氧基-1-甲基-4H-[1,2,4]三唑并[4,3-A][1,4]苯并二氮杂卓-4-乙酰胺,I-BET762; GSK525762; GSK525762A
Inhibitor of BET proteins
I-BET-762
Cas No.: 1260907-17-2
规格价格库存数量操作
5mg¥672.00现货
1
10mg¥1,050.00现货
1
50mg¥3,444.00现货
1
10mM (in 1mL DMSO)¥662.00现货
1
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产品描述 Description

I-BET-762 is a highly potent inhibitor of BET with IC50 values of 32.5–42.5 nM [1].

I-BET-762 is found to have high affinity with BET (Kd of 50.5–61.3 nM). It binds to the acetyl-lysine (AcK)-binding pocket of BET and competes with AcK. The structure of I-BET-762 allows it to bind with BET in ratio of 2:1 results in the high affinity of it. I-BET-762 also has high selectivity, it has no interaction with other bromodomain-containing proteins. I-BET-762 is reported to downregulate the expression of the genes which are induced by LPS, thus causing the decreased expression of LPS-inducible cytokines and chemokines. In vivo assay shows that I-BET-762 has the anti-inflammatory potential. Treatment of I-BET-762 can cure the mice which have started to develop symptoms of inflammatory disease [1].

References:
[1] Nicodeme E, Jeffrey KL, Schaefer U, Beinke S, Dewell S, Chung CW, Chandwani R, Marazzi I, Wilson P, Coste H, White J, Kirilovsky J, Rice CM, Lora JM, Prinjha RK, Lee K, Tarakhovsky A. Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468 (7327):1119-23.

实验参考方法 Experimental Reference Method

Kinase experiment [1]:

Fluorescence resonance energy transfer (FRET) titrations

I-BET is titrated against BRD2 (200 nM), BRD3 (100 nM) and BRD4 (50 nM) in 50 mM HEPES pH7.5, 50 mM NaCl, 0.5 mM CHAPS in the presence of tetra-acetylated Histone H4 peptide (200 nM). After equilibrating for 1 hour, the bromodomain protein : peptide interaction is detected using FRET following the addition of 2nM Europium cryptate labelled streptavidin and 10 nM XL-665-labelled anti-6His antibody in assay buffer c

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
1260907-17-2
同义词
(4S)-6-(4-氯苯基)-N-乙基-8-甲氧基-1-甲基-4H-[1,2,4]三唑并[4,3-A][1,4]苯并二氮杂卓-4-乙酰胺,I-BET762; GSK525762; GSK525762A
化学名
2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide
SMILES
CCNC(=O)CC1C2=NN=C(N2C3=C(C=C(C=C3)OC)C(=N1)C4=CC=C(C=C4)Cl)C
分子式
C22H22ClN5O2
分子量
423.9 g/mol
溶解性
≥ 21.195mg/mL in DMSO
保存条件
Store at -20°C
General tips
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。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol