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TMP195

HDAC Inhibitors
    级别和纯度:
  • 10mM in DMSO
  • CAS编号: 1314891-22-9
  • 分子式: C23H19F3N4O3
  • 分子量: 456.42
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
T408048-1ml
1ml 现货 Stock Image
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Compound libraries (12333)

基本描述

英文别名 TFMO 2 | Benzamide, N-​[2-​methyl-​2-​(2-​phenyl-​4-​oxazolyl)​propyl]​-​3-​[5-​(trifluoromethyl)​-​1,​2,​4-​oxadiazol-​3-​yl]​-
规格或纯度 10mM in DMSO
英文名称 TMP195
生化机理 TMP195 (TFMO 2) 是一种选择性很强的一流 IIa 类 HDAC 抑制剂,在基于细胞的 IIa 类 HDAC 检测中 IC50 为 300 nM。
储存温度 -80℃储存
运输条件 超低温冰袋运输
产品介绍


Information

TMP195 TMP195 (TFMO 2) is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays.
In vitro

TMP195 has low potency in recombinant class I and IIb HDAC assays, enabling full inhibition of class IIa HDAC activity without inhibition of other HDACs. TMP195 blocks the accumulation of CCL2 protein in the supernatants of monocyte-derived macrophage differentiation cultures and significantly increases the amount of CCL1 protein secreted by the monocytes compared to vehicle (DMSO)-treated M-CSF plus GM-CSF cultures. TMP195 influences human monocyte responses to the colony-stimulating factors CSF-1 and CSF-2 in vitro.

In vivo

In vivo TMP195 treatment alters the tumour microenvironment and reduces tumour burden and pulmonary metastases by modulating macrophage phenotypes. TMP195 induces the recruitment and differentiation of highly phagocytic and stimulatory macrophages within tumours. TMP195 treatment significantly decreases proliferating tumour cells, most notably at the leading edge of the tumour. The anti-tumour macrophage phenotype induced by TMP195 treatment thus enhances the efficacy and durability of both standard chemotherapeutic regimens and checkpoint blockade immunotherapy in this mouse model of breast cancer.
Cell Data

cell lines:

Concentrations:300 nM

Incubation Time:5 days

Powder Purity:≥98%

产品属性

ALogP 4.525
HBD Count 1
Rotatable Bond 7

关联靶点(人)

HDAC4 Tclin 组蛋白去乙酰化酶4(Histone deacetylase 4) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC7 Tclin 组蛋白去乙酰化酶7(Histone deacetylase 7) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC9 Tclin 组蛋白去乙酰化酶9(Histone deacetylase 9) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC5 Tclin 组蛋白去乙酰化酶5(Histone deacetylase 5) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

Isomeric SMILES CC(C)(CNC(=O)C1=CC=CC(=C1)C2=NOC(=N2)C(F)(F)F)C3=COC(=N3)C4=CC=CC=C4
PubChem CID 67324851
分子量 456.42

化学和物理性质

溶解性 Solubility (25°C) In vitro Water: 24 mg/mL (9.17 mM);    
DMSO(mg / mL) Max Solubility 91
DMSO(mM) Max Solubility 199.3777661
Water(mg / mL) Max Solubility <1

安全和危险性(GHS)

象形图 GHS07
信号词 Warning
危险声明

H302: 吞食有害

预防措施声明

P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器