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TMP195

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Chemical Structure| 1314891-22-9 同义名 : TFMO 2
CAS号 : 1314891-22-9
货号 : A216033
分子式 : C23H19F3N4O3
纯度 : 99%+
分子量 : 456.417
MDL号 : MFCD26522024
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(230.05 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • HDAC4

    HDAC4, Ki:59 nM

  • HDAC9

    HDAC9, Ki:15 nM

  • HDAC7

    HDAC7, Ki:26 nM

  • HDAC5

    HDAC5, Ki:60 nM
描述 TMP195 effectively hinders the accumulation of CCL2 protein in the culture supernatants during the differentiation of monocyte-derived macrophages, while markedly enhancing the secretion of CCL1 protein by monocytes in comparison to the vehicle-treated group. This alteration in cytokine profile is confirmed by transcriptional profiling data from PHA-stimulated peripheral blood mononuclear cell (PBMC) experiments, where CCL2 is downregulated and CCL1 is upregulated following TMP195 treatment[1]. The mechanism of action of TMP195 involves its competition for the acetyllysine-binding site of class IIa HDACs, effectively preventing HDAC7 from binding to various side-chain modifications on a peptide backbone. Notably, this competitive inhibition does not affect the function of other acetyllysine reader proteins such as BRD4, where TMP195 shows no inhibitory activity at concentrations up to 50 μM[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.95mL

2.19mL

1.10mL

21.91mL

4.38mL

2.19mL
参考文献

[1]Lobera M, et al. Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group. Nat Chem Biol. 2013 May;9(5):319-25.

[2]Guerriero JL, et al. Class IIa HDAC inhibition reduces breast tumors and metastases through anti-tumor macrophages. Nature. 2017 Mar 16;543(7645):428-432.