TMP269

For research use only.

Catalog No.S7324

22 publications

TMP269 Chemical Structure

CAS No. 1314890-29-3

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.

Selleck's TMP269 has been cited by 22 publications

Purity & Quality Control

Choose Selective HDAC Inhibitors

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 Mnq2SpVv[3Srb36gZZN{[Xl? NWrVW|g5PjBibXnudy=> MnToTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCQLYTldo1qdmGuIFfTWE11[WepZXSgTGRCSzdiKEWxPEB1dyB7OUGgdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCrboPlZ5Qh[2WubIOgeZNqdmdiQn;jMWspXE[DKT3BUWMh[XNic4Xid5Rz[XSnIHnuZ5Vj[XSnZDDmc5IhPjBibXnud{BjgSCobIXvdoV{[2WwY3WgZZN{[XluIFnDOVAhRSByLkC0NFg2KM7:TT6= NGe4dZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C2NFc3PCd-MkewOlA4PjR:L3G+
insect cells MnO0SpVv[3Srb36gZZN{[Xl? MYq2NEBucW6| NUfLdmJKUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDOMZRmem2rbnHsJGdUXC22YXfn[YQhUESDQ{egLFUyQCC2bzC5PVEhemW|aXT1[ZMqKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{1qdm[nY4Tl[EBqdnOnY4SgZ4VtdHNiYX\0[ZIhPjBibXnud{BjgSCobIXvdolu\XSncjygT4khRSByLkC0OlMh|ryPLh?= NWfkVlRORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1PFk1PDFpPkK5OVg6PDRzPD;hQi=>
insect cells MYDGeY5kfGmxbjDhd5NigQ>? MVq2NEBucW6| MYLJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKENvdHXycYlv[WxiSHnzMZRi\2enZDDISGFEPSBqNkW2JJRwKDFzMkKgdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3cz3pcoZm[3SnZDDpcpNm[3RiY3XscJMhfXOrbnegRo9kNUy7czjUSmEqNUGPQzDhd{B{fWK|dILheIUh[W[2ZYKgOlAhdWmwczDifUBndHWxcnnt[ZRmeixiS3mgQUAxNjB6Nkmg{txONg>? M4S1PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUi5OFQyLz5{OUW4PVQ1OTxxYU6=
insect cells MVzGeY5kfGmxbjDhd5NigQ>? M1nlV2lvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iQz30[ZJucW6jbDDHV3QufGGpZ3XkJGhFSUN2IHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2ey2rbn\lZ5Rm\CCrboPlZ5Qh[2WubIOgeZNqdmdiQn;jMWx6eyiWRlGpMWFOSyCjczDzeYJ{fHKjdHWgZpkh\my3b4LpcYV1\XJuIFvpJF0hOC5yOUC1JO69VS5? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV6OUS0NUc,Ojl3OEm0OFE9N2F-
insect cells M3zwUWZ2dmO2aX;uJIF{e2G7 NELyUII3OCCvaX7z NXP1eHE1UW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDDMZRmem2rbnHsJGhqey22YXfn[YQhUESDQ{WgLFY2PyC2bzCxNVI{KHKnc3nkeYV{MSCneIDy[ZN{\WRiaX6gbY5{\WO2IHPlcIx{KHW|aX7nJGJw[y2NKGTGRUkuSU2FIHHzJJN2[nO2cnH0[UBqdmO3YnH0[YQh\m:{IE[wJI1qdnNiYomg[ox2d3Knc3PlcoNmKGG|c3H5MEBKSzVyIE2gNE4yODh2IN88UU4> Ml;3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyNkC3OlQoRjJ5ME[wO|Y1RC:jPh?=
insect cells M{\ERmZ2dmO2aX;uJIF{e2G7 MmTNOlAhdWmwcx?= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KE5vdHXycYlv[WxiR2PUMZRi\2enZDDDMZRmem2rbnHsJGhqey22YXfn[YQhUESDQ{SgLFYzPyC2bzCxNFg1KHKnc3nkeYV{MSCneIDy[ZN{\WRiaX6gbY5{\WO2IHPlcIx{KHW|aX7nJGJw[y2NKGTGRUkuSU2FIHHzJJN2[nO2cnH0[UBqdmO3YnH0[YQh\m:{IE[wJI1qdnNiYomg[ox2d3Knc3PlcoNmKGG|c3H5MEBKSzVyIE2gNE4yOzR2IN88UU4> M2T1b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5ME[wO|Y1Lz5{N{C2NFc3PDxxYU6=
insect cells M4HobmZ2dmO2aX;uJIF{e2G7 NUHBd3Y4PjBibXnudy=> MlOyTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDoeY1idiCFLYTldo1qdmGuIFjpd{11[WepZXSgTGRCSzhiKEGgeI8hOzd5IILld4llfWW|KTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNvaX7m[YN1\WRiaX7z[YN1KGOnbHzzJJV{cW6pIGLIT{hC[ymNKFHjLWFOSyCjczDzeYJ{fHKjdHWgZYZ1\XJiNkCgcYlveyCkeTDmcJVwemmvZYTldkwhU2liPTCyMlcxPiEQvF2u MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV6OUS0NUc,Ojl3OEm0OFE9N2F-

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:[1]
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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]
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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (194.35 mM)
Ethanol 2 mg/mL warmed (3.88 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 514.52
Formula

C25H21F3N4O3S

CAS No. 1314890-29-3
Storage powder
in solvent
Synonyms N/A
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

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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Molecular Weight Calculator

Molecular Weight Calculator

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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

Tel: +1-832-582-8158 Ext:3

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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID