TP-238

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TP-238 

TP-238 是一种有效的选择性 CECR2/BPTF 双探针,IC50 值分别为 30 nM 和 350 nM。TP-238 还抑制 BRD9pIC50 为 5.9,对其他 338 激酶的活性较低。

TP-238

TP-238 Chemical Structure

CAS No. : 2415263-04-4

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生物活性

TP-238 is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases[1][2].

IC50 & Target

CECR2

7.5 (pIC50)

BRD9

5.9 (pIC50)

CECR2

30 nM (IC50)

CECR2

10 nM (Kd)

BPTF

6.5 (pIC50)

BPTF

350 nM (IC50)

BPTF

120 nM (Kd)

体外研究
(In Vitro)

TP-238 has on target biochemical activity of 10-30 nM with CECR2 and 100-350 nM with BPTF. TP-238 displays potency for both CECR2 (pIC50 of 7.5) and BPTF (pIC50 of 6.5) in an Alpha screen assay. Isothermal titration calorimetry (ITC) shows TP-238 with a Kd of 10 nM for CECR2 and 120 nM for BPTF[1][2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

458.58

Formula

C22H30N6O3S

CAS 号

2415263-04-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Michael A Clegg, et al. Advancements in the Development of non-BET Bromodomain Chemical Probes. ChemMedChem. 2019 Feb 19;14(4):362-385.

    [2]. Peter D Ycas, et al. New Inhibitors for the BPTF Bromodomain Enabled by Structural Biology and Biophysical Assay Development. Org Biomol Chem. 2020 Jun 26.

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