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| Product Name: | TMP269 | | Synonyms: | N-[[Tetrahydro-4-(4-phenyl-2-thiazolyl)-2H-pyran-4-yl]methyl]-3-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]benzamide TMP269;TMP269 N-[[Tetrahydro-4-(4-phenyl-2-thiazolyl)-2H-pyran-4-yl]methyl]-3-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]benzamide;BenzaMide, N-[[tetrahydro-4-(4-phenyl-2-thiazolyl)-2H-pyran-4-yl]Methyl]-3-[5-(trifluoroMethyl)-1,2,4-oxadiazol-3-yl]-;TMP269;N-((4-(4-phenylthiazol-2-yl)tetrahydro-2H-pyran-4-yl)Methyl)-3-(5-(trifluoroMethyl)-1,2,4-oxadiazol-3-yl)benzaMide;N-[[Tetrahydro-4-(4-phenyl-2-thiazolyl)-2H-pyran-4-yl]methyl]-3-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]benzamide;TMP269, >=98%;N-((4-(4-Phenylthiazol-2-yl)tetrahydro-2H-pyran-4-yl)methyl)-3-(5-(trifluoromethyl)-1,2,4-oxad | | CAS: | 1314890-29-3 | | MF: | C25H21F3N4O3S | | MW: | 514.52 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1314890-29-3.mol |  |
| | TMP269 Chemical Properties |
| density | 1.347±0.06 g/cm3(Predicted) | | storage temp. | Amber Vial, -20°C Freezer, Under inert atmosphere | | solubility | ≥23 mg/mL in DMSO; insoluble in H2O; ≥21 mg/mL in EtOH with ultrasonic | | form | solid | | pka | 13.66±0.46(Predicted) |
| | TMP269 Usage And Synthesis |
| Uses | TMP269 is a selective class IIa histone deacetylase (HDAC) inhibitor via a non chelating zinc-binding group. | | Biological Activity | tmp269 is a novel and selective inhibitor of class iia histone deacetylase with ic50 values of 126, 80, 36, 9 nm for hdac 4, 5, 7, 9, respectively [1].histone deacetylases (hadc) are a series of enzymes that remove acetyl groups from an ε-n-acetyl lysine amino acid on a histone and make the histones to wrap the dna more tightly, which prevent transcription.tmp269 is a novel and selective class iia hdac inhibitor. in mm cell lines, tmp269 induced modest cytotoxicity with ic50 values ranging from 22 to 38 μm in a dose-dependent way, which was associated with cleavage of caspase-3, -8, -9 and parp. also, tmp269 enhanced cfz-induced apoptosis and increased the expression of activating transcription factor 4 (atf4) and proapoptotic transcription factor c/ebp homologous protein (chop). in the presence of bmscs or il-6, tmp269 and cfz also showed significant cytotoxicity [2]. in iec-18 intestinal epithelial cells, tmp269 inhibited cell proliferation, cell cycle progression and dna synthesis in response to g protein-coupled receptor/protein kinase d1 (pkd1) activation [3]. | | target | HDAC9 | | references | [1]. lobera m, madauss kp, pohlhaus dt, et al. selective class iia histone deacetylase inhibition via a nonchelating zinc-binding group. nat chem biol, 2013, 9(5): 319-325.
[2]. kikuchi s, suzuki r, ohguchi h, et al. class iia hdac inhibition enhances er stress-mediated cell death in multiple myeloma. leukemia, 2015.
[3]. sinnett-smith j, ni y, wang j, et al. protein kinase d1 mediates class iia histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling. am j physiol cell physiol, 2014, 306(10): c961-71. |
| | TMP269 Preparation Products And Raw materials |
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