TPOP146

目录号: GC32880纯度: >99.50%

TPOP146是选择性的CBP/P300苯并西泮溴结构域抑制剂；对CBP和BRD4的Kd值分别为134nM和5.02μM。

Cas No.: 2018300-62-2

规格	价格	库存	数量
1mg	¥314.00	现货	1
5mg	¥945.00	现货	1
10mg	¥1,620.00	现货	1
50mg	¥4,320.00	现货	1
100mg	¥7,200.00	现货	1
10mM (in 1mL DMSO)	¥999.00	现货	1

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文献被引

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610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
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388(6745) (2025)
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产品描述 Description

TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.

Exposure to 1 μM TPOP146 results in a significant decrease of recovery half-life that is comparable to the construct that contained the bromodomain inactivating mutation N1168F, demonstrating that TPOP146 targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediated interactions of the CBP bromodomain in cellular environments[1].

[1]. Popp TA, et al. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. J Med Chem. 2016 Oct 13;59(19):8889-8912.

实验参考方法 Experimental Reference Method

Kinase experiment:

Proteins are buffered in 10 mM HEPES, pH 7.5, 500 mM NaCl and assayed in a 96-well plate at a final concentration of 2 μM in 20 μL volume. Compounds (TPOP146) are added at a final concentration of 10 μM. SYPRO Orange (Molecular Probes) is added as a fluorescence probe at a dilution of 1:1000. Excitation and emission filters for the SYPRO Orange dye are set to 465 and 590 nm, respectively. The temperature is raised with a step of 3°C per minute from 25 to 96°C, and fluorescence readings are taken at each interval[1].

References:

[1]. Popp TA, et al. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. J Med Chem. 2016 Oct 13;59(19):8889-8912.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号

2018300-62-2

SMILES

COC1=CC(OC)=CC(C2=CC(C(N[C@H]3CCCN(C)C3)=O)=C(OCCN(C(CC)=O)C4)C4=C2)=C1

分子式

C₂₇H₃₅N₃O₅

分子量

481.58 g/mol

溶解性

DMSO : ≥ 100 mg/mL (207.65 mM)

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。

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分子量 (MW)

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