2-Bromo-4'-hydroxyacetophenone

2-Bromo-4'-hydroxyacetophenone(PTP Inhibitor I) 是一种PTP1B 的有效抑制剂,其Ki=42 μM。

CAS号

2491-38-5

分子式

C8H7BrO2

主要靶点

Phosphatase

仅限科研使用

Cat No : CM01356

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Synonyms

PTP Inhibitor I|SHP-1 Inhibitor II|2-溴-4'-羟基苯乙酮|α-Bromo-4-hydroxyacetophenone|4-Hydroxyphenacyl bromide



产品信息

2-Bromo-4'-hydroxyacetophenone(PTP Inhibitor I) is a cell-permeable, protein tyrosine phosphatase (PTP) inhibitor that covalently blocks the catalytic domain of the Src homology region 2 domain-containing phosphatase (SHP-1(ΔSH2)) with a Ki value of 43 μM and PTP1B with a Ki value of 42 μM [1]. SHP-1 and PTP1B both have known roles in regulating insulin signaling as well as myeloid and lymphoid cell differentiation, making inhibitors of these phosphatases of interest in diabetes, cancer, allergy, and inflammation research [2].

CAS号 2491-38-5
分子式 C8H7BrO2
主要靶点 Phosphatase
主要通路 代谢
分子量 215.04
纯度 99.07%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 PTP Inhibitor I|SHP-1 Inhibitor II|2-溴-4'-羟基苯乙酮|α-Bromo-4-hydroxyacetophenone|4-Hydroxyphenacyl bromide

靶点活性

SHP-1:43 μM (Ki, cell free)|PTP1B:42 μM (Ki, cell free)

溶解度

Ethanol:20 mg/mL,H2O:Insoluble,DMSO:20 mg/mL

细胞实验

Cell lines: human B cells. Concentrations: 30, 100, 300, 1000 μM. Method: After incubation with varying concentrations of PTP Inhibitor I for 3 min, the cells are lysed, and the cellular proteins are separated on an SDS-PAGE gel, followed by western blot analysis.

参考文献

1.Arabaci, G., et al. αHaloacetophenone derivatives as photoreversible covalent inhibitors of protein tyrosine phosphatases. Journal of the American Chemical Society 121(21), 5085-5086 (1999).
2.Heneberg, P. Use of protein tyrosine phosphatase inhibitors as promising targeted therapeutic drugs. Current Medicinal Chemistry 16(6), 706-733 (2009).
3.Wu R, Wang C, Li Z, et al. SOX2 promotes resistance of melanoma with PD-L1 high expression to T-cell-mediated cytotoxicity that can be reversed by SAHA[J]. Journal for immunotherapy of cancer. 2020, 8(2).

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