Name | TMP195 |
Synonyms | TMP195 TFMO 2 TMP 195 CS-2651 TMP-195 TMP-195 TMP 195 - TFMO 2 N-[2-Methyl-2-(2-phenyloxazol-4-yl)propyl]-3-[5-(trifluoroMethyl)-1,2,4-oxadiazol-3-yl]benzaMide |
CAS | 1314891-22-9 |
Molecular Formula | C23H19F3N4O3 |
Molar Mass | 456.42 |
Solubility | 10 mM in DMSO |
Storage Condition | -20℃ |
In vitro study | TMP195 has low potency in recombinant class I and Class II B HDAC assays and is able to completely inhibit Class II a HDAC activity without inhibiting other HDACs. In the supernatant of monocyte-derived macrophage differentiation medium, TMP195 prevented the accumulation of CCL2 protein; Compared with the control group, TMP195 significantly increased the level of CCL1 protein secreted by monocytes. TMP195 is able to influence the response of human monocytes to colony stimulating factors CSF-1 and CSF-2. |
In vivo study | TMP195 alters tumor microenvironment, reduces tumor burden and lung metastasis in vivo by modulating macrophage phenotype. TMP195 induces recruitment and differentiation of highly phagocytic and stimulatory macrophages within tumors. TMP195 can significantly reduce the proliferation of tumor cells, especially in the front region of the tumor. In a mouse breast cancer model, anti-tumor macrophages induced by TMP195 have been shown to enhance the efficacy and durability of standard chemotherapy regimens and checkpoint blockade immunotherapy. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.191 ml | 10.955 ml | 21.91 ml |
5 mM | 0.438 ml | 2.191 ml | 4.382 ml |
10 mM | 0.219 ml | 1.095 ml | 2.191 ml |
5 mM | 0.044 ml | 0.219 ml | 0.438 ml |
Biological activity | TMP195 (TFMO 2) is a selective class IIa HDAC inhibitor. In cell-based experiments, IC50 is 300 nM. |
target | TargetValue HDAC9 (cell-free say) 15 nM (ki) HDAC7 (cell-free say) 26 nM (ki) HDAC4 (cell-free say) 59 nM (ki) HDAC5 (cell-free say) 60 nM (ki) |
Target | Value |
HDAC9 (Cell-free assay) | 15 nM(Ki) |
HDAC7 (Cell-free assay) | 26 nM(Ki) |
HDAC4 (Cell-free assay) | 59 nM(Ki) |
HDAC5 (Cell-free assay) | 60 nM(Ki) |
in vitro study | TMP195 has low efficacy in recombinant class I and class Ⅱb HDAC tests, and can completely inhibit class Ⅱa HDAC activity without inhibiting other HDACs. In the supernatant of monocyte-derived macrophage differentiation medium, TMP195 prevents the accumulation of CCL2 protein. Compared with the control group, TMP195 can significantly increase the level of CCL1 protein secreted by monocytes. TMP195 can affect the response of human monocytes to colony-stimulating factor CSF-1 and CSF-2. |
in vivo study | TMP195 changes tumor microenvironment, reduces tumor burden and lung metastasis by regulating macrophage phenotype in vivo. TMP195 induces recruitment and differentiation of highly phagocytic and irritating macrophages within tumors. TMP195 can significantly reduce the proliferation of tumor cells, especially in the front area of the tumor. In a mouse breast cancer model, anti-tumor macrophages induced by TMP195 have been shown to enhance the efficacy and persistence of standard chemotherapy regimens and checkpoint blockade immunotherapy. |