N-[2-Methyl-2-(2-phenyloxazol-4-yl)propyl]-3-[5-(trifluoroMethyl)-1,2,4-oxadiazol-3-yl]benzaMide
N-[2-Methyl-2-(2-phenyloxazol-4-yl)propyl]-3-[5-(trifluoroMethyl)-1,2,4-oxadiazol-3-yl]benzaMide Basic information
- Product Name:
- N-[2-Methyl-2-(2-phenyloxazol-4-yl)propyl]-3-[5-(trifluoroMethyl)-1,2,4-oxadiazol-3-yl]benzaMide
- Synonyms:
-
- TMP-195;TMP195;TMP 195
- CS-2651
- TFMO 2
- N-[2-Methyl-2-(2-phenyloxazol-4-yl)propyl]-3-[5-(trifluoroMethyl)-1,2,4-oxadiazol-3-yl]benzaMide
- TMP 195
- TMP 195 - TFMO 2
- TMP195; TMP-195
- Inhibitor,TMP195,TMP-195,HDAC,Histone deacetylases,inhibit
- CAS:
- 1314891-22-9
- MF:
- C23H19F3N4O3
- MW:
- 456.42
- Product Categories:
-
- API
- Mol File:
- 1314891-22-9.mol
N-[2-Methyl-2-(2-phenyloxazol-4-yl)propyl]-3-[5-(trifluoroMethyl)-1,2,4-oxadiazol-3-yl]benzaMide Chemical Properties
- Density
- 1.303±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF: 10 mg/ml; DMSO: 10 mg/ml; Ethanol: 10 mg/ml; PBS (pH 7.2): 0.2 mg/ml
- form
- A crystalline solid
- pka
- 13.05±0.46(Predicted)
- color
- White to off-white
N-[2-Methyl-2-(2-phenyloxazol-4-yl)propyl]-3-[5-(trifluoroMethyl)-1,2,4-oxadiazol-3-yl]benzaMide Usage And Synthesis
Uses
TMP195 is a selective class IIa histone deacetylase (HDAC) inhibitor with Kis of 59, 60, 26, 15 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
Biological Activity
TMP195 (TFMO 2) is a selective class IIa HDAC inhibitor with IC50 of 300 nM in cell-based assays.
in vitro
TMP195 has low potency in recombinant class I and class IIb HDAC assays, and is able to completely inhibit class IIa HDAC activity without inhibiting other HDACs. In the supernatant of monocyte-derived macrophage differentiation medium, it prevented the accumulation of CCL2 protein; compared with the control group, it could significantly increase the level of CCL1 protein secreted by monocytes.
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 tumors. Combining TMP195 with chemotherapy regimens or T-cell checkpoint blockade in this model significantly enhances the durability of tumour reduction[2].
target
| 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) |
IC 50
HDAC9: 9 nM (IC50); HDAC7: 46 nM (IC50); HDAC5: 106 nM (IC50); HDAC4: 111 nM (IC50); HDAC8: 11700 nM (IC50); HDAC6: 47800 nM (IC50)
References
[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. DOI:10.1038/nchembio.1223
[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. DOI:10.1038/nature21409
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