中文名：TMP195
英文名：TMP195
纯度：≥98%
货号：T414032
Cas号：1314891-22-9
存储温度：-20°C储存
运输条件：超低温运输
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.
Targets
HDAC9 (Cell-free assay); HDAC7 (Cell-free assay); HDAC4 (Cell-free assay); HDAC5 (Cell-free assay) 15 nM(Ki); 26 nM(Ki); 59 nM(Ki); 60 nM(Ki)
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 Research(from reference)
Cell lines：Human monocytes
Concentrations：300 nM
Incubation Time：5 days
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关键字： TFMO 2Benzamide,N-?[2-?methyl-?2-?(2-?phenyl-?4-?oxazolyl)?propyl]?-?3-?[5-?(trifluoromethyl)?-?1,?2,?4-?oxadiazol-?3-?yl]?-
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