TMP269

Catalog No.S7324

For research use only.

TMP269 is a potent, selective class IIa HDAC inhibitor with IC50 of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.

TMP269 Chemical Structure

CAS No. 1314890-29-3

Selleck's TMP269 has been cited by 24 publications

Purity & Quality Control

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Biological Activity

Description TMP269 is a potent, selective class IIa HDAC inhibitor with IC50 of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
Targets
HDAC9 [1]
(Cell-free assay)
HDAC7 [1]
(Cell-free assay)
HDAC5 [1]
(Cell-free assay)
HDAC4 [1]
(Cell-free assay)
23 nM 43 nM 97 nM 157 nM
In vitro

TMP269 has no impact on the mitochondrial activity and/or the viability of human CD4+ T cells at 10 μM, and may be used as tools to identify the endogenous substrates of the class IIa HDAC enzymes. [1] In IEC-18 intestinal epithelial cells, TMP269 prevents cell cycle progression, DNA synthesis, and proliferation induced in response to G protein-coupled receptor/PKD1 activation. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
insect cells MXfGeY5kfGmxbjDhd5NigQ>? MoXmOlAhdWmwcx?= MYjJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KE5vdHXycYlv[WxiR2PUMZRi\2enZDDISGFEPyBqNUG4JJRwKDl7MTDy[ZNq\HWnczmg[ZhxemW|c3XkJIlvKGmwc3XjeEBk\WyuczD1d4lv\yCEb3OtT{hVTkFrLVHNR{BieyC|dXLzeJJifGViaX7jeYJifGWmIH\vdkA3OCCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDhd5NigSxiSVO1NEA:KDBwMESwPFUh|ryPLh?= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB4MEe2OEc,OjdyNkC3OlQ9N2F-
insect cells M3PrT2Z2dmO2aX;uJIF{e2G7 M2S0b|YxKG2rboO= NHPKPXhKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIF6teIVzdWmwYXygS3NVNXSjZ3fl[EBJTEGFNzCoOVE5KHSxIEm5NUBz\XOrZIXld{kh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzMYlv\mWldHXkJIlve2WldDDj[YxteyCjZoTldkA3OCCvaX7zJIJ6KG[udX;ybY1mfGW{LDDLbUA:KDBwMES2N{DPxE1w MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV6OUS0NUc,Ojl3OEm0OFE9N2F-
insect cells NEX3WlFHfW6ldHnvckBie3OjeR?= M{HBW|YxKG2rboO= NW\FSoJlUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDDMZRmem2rbnHsJGhqey22YXfn[YQhUESDQ{WgLFY2PiC2bzCxNVIzKHKnc3nkeYV{MSCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMucW6oZXP0[YQhcW6|ZXP0JINmdGy|IIXzbY5oKEKxYz3MfZMpXE[DKT3BUWMh[XNic4Xid5Rz[XSnIHHmeIVzKDZyIH3pcpMh[nliZnz1c5JqdWW2ZYKsJGtqKD1iMD6wPFY6KM7:TT6= M4Ljb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUi5OFQyLz5{OUW4PVQ1OTxxYU6=
insect cells NIewNVNHfW6ldHnvckBie3OjeR?= NW\C[ZNxUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDDMZRmem2rbnHsJGdUXC22YXfn[YQhUESDQ{Sg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|LXnu[oVkfGWmIHnud4VkfCClZXzsd{B2e2mwZzDCc4MuVHm|KGTGRUkuSU2FIHHzJJN2[nO2cnH0[UBjgSCobIXvdolu\XSncjygT4khRSByLkC5NFUh|ryPLh?= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV6OUS0NUc,Ojl3OEm0OFE9N2F-
insect cells M4HhRWZ2dmO2aX;uJIF{e2G7 M3y5[|YxKG2rboO= M1LJ[mlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiQz30[ZJucW6jbDDIbZMufGGpZ3XkJGhFSUN3IDi2OVchfG9iMUGyN{Bz\XOrZIXld{kh\XiycnXzd4VlKGmwIHnud4VkfCClZXzsd{B2e2mwZzDCc4MuUyiWRlGpMWFOSyCjczDzeYJ{fHKjdHWgbY5kfWKjdHXkJIZweiB4MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBie3OjeTygTWM2OCB;IECuNVA5PCEQvF2u NG\nVYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C2NFc3PCd-MkewOlA4PjR:L3G+
insect cells NWLOe2hHTnWwY4Tpc44h[XO|YYm= MlrwOlAhdWmwcx?= NEW1XlFKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IF6teIVzdWmwYXygS3NVNXSjZ3fl[EBENXSncn3pcoFtKEircz30ZYdo\WRiSFTBR|QhMDZ{NzD0c{AyODh2IILld4llfWW|KTDlfJBz\XO|ZXSgbY4hcW6|ZXP0JINmdGy|IIXzbY5oKEKxYz3LLHRHSSlvQV3DJIF{KHO3YoP0doF1\SCrbnP1ZoF1\WRiZn;yJFYxKG2rboOgZpkh\my3b4Lld4NmdmOnIHHzd4F6NCCLQ{WwJF0hOC5zM{S0JO69VS5? MmLwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyNkC3OlQoRjJ5ME[wO|Y1RC:jPh?=
insect cells MnjBSpVv[3Srb36gZZN{[Xl? NGrpXVY3OCCvaX7z M4nkXGlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iQz30[ZJucW6jbDDIbZMufGGpZ3XkJGhFSUN6IDixJJRwKDN5NzDy[ZNq\HWnczmg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|LXnu[oVkfGWmIHnud4VkfCClZXzsd{B2e2mwZzDSTGspSWNrSzjBZ{lCVUNiYYOgd5Vje3S{YYTlJIFnfGW{IE[wJI1qdnNiYomg[ox2d3KrbXX0[ZItKEurIE2gNk44ODZizszNMi=> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV6OUS0NUc,Ojl3OEm0OFE9N2F-

Protocol (from reference)

Kinase Assay:[1]
  • HDAC selectivity assays:

    Dose-response studies are done with ten concentrations in a threefold dilution series from a maximum final compound concentration of 100 μM in the reaction mixture and are conducted at Reaction Biology Corp. All assays are based on the same principle as the HDAC9 assay described above: the deacetylation of acetylated or trifluoroacetylated lysine residues on fluorogenic peptide substrates by HDAC. HDAC1, HDAC2, HDAC3, HDAC6, HDAC10 and HDAC11 used a substrate based on residues 379-382 of p53 (Arg-His-Lys-Lys(Ac)). For HDAC8, the diacetylated peptide substrate, based on residues 379–382 of p53 (Arg-His-Lys(Ac)-Lys(Ac)), is used. HDAC4, HDAC5, HDAC7 and HDAC9 assays used the class IIa HDAC–specific fluorogenic substrate (Boc-Lys(trifluoroacetyl)-AMC). All reactions are done with 50 μM HDAC substrate in assay buffer (50 mM Tris-HCl, pH 8.0, 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1 mg/mL BSA) containing 1% DMSO final concentration; incubated for 2 h at 30 °C; and developed with trichostatin A and trypsin.

Cell Research:[1]
  • Cell lines: Human CD4+ T cells
  • Concentrations: 10 μM
  • Incubation Time: 72 hours
  • Method: Human CD4+ T cells are isolated from whole blood via negative selection according to manufacturer's instructions (RosetteSep Human CD4+ T cell enrichment kit), re-suspended in T-cell culture medium (10% FBS, 2 mM L-glutamine, 1 mM pyruvate, 10 mM HEPES, 10 U/10 mg penicillin/streptomycin, 0.5% DMSO in RPMI) and plated at 50,000 cells/well with IL-2 (10 BRMP units/mL) and 100,000 human T-expander Dynabeads for 72 h. Determination of mitochondrial function or cell viability is done according to manufacturer’s instructions (Cell Proliferation Assay Kit I (MTT)) and is represented as a percent of control (no inhibitor) wells.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 514.52
Formula

C25H21F3N4O3S

CAS No. 1314890-29-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1COCCC1(CNC(=O)C2=CC=CC(=C2)C3=NOC(=N3)C(F)(F)F)C4=NC(=CS4)C5=CC=CC=C5

In vivo Formulation Calculator (Clear solution)

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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