Home Epigenetics HDAC inhibitor TMP269 For research use only.

TMP269

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

TMP269 Chemical Structure

CAS No. 1314890-29-3

Purity & Quality Control

TMP269 Related Products

Signaling Pathway

HDAC Signaling Pathways

HDAC Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
insect cells Function assay 60 mins Inhibition of human recombinant N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in insect cells using Boc-K(TFA)-AMC as substrate incubated for 60 mins by fluorescence assay, IC50 = 0.04085 μM. 27060764
insect cells Function assay 60 mins Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in baculovirus-infected insect cells after 60 mins by fluorimeter, Ki = 0.0463 μM. 29589441
insect cells Function assay 60 mins Inhibition of recombinant human C-terminal His-tagged HDAC5 (656 to 1122 residues) expressed in baculovirus-infected insect cells using Boc-Lys(TFA)-AMC as substrate after 60 mins by fluorimeter, Ki = 0.0869 μM. 29589441
insect cells Function assay Inhibition of recombinant human C-terminal GST-tagged HDAC4 expressed in baculovirus-infected insect cells using Boc-Lys(TFA)-AMC as substrate by fluorimeter, Ki = 0.0905 μM. 29589441
insect cells Function assay 60 mins Inhibition of human recombinant C-terminal His-tagged HDAC5 (657 to 1123 residues) expressed in insect cells using Boc-K(TFA)-AMC as substrate incubated for 60 mins by fluorescence assay, IC50 = 0.1084 μM. 27060764
insect cells Function assay 60 mins Inhibition of human recombinant N-terminal GST-tagged C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in insect cells using Boc-K(TFA)-AMC as substrate incubated for 60 mins by fluorescence assay, IC50 = 0.1344 μM. 27060764
insect cells Function assay 60 mins Inhibition of recombinant human C-terminal His-tagged HDAC8 (1 to 377 residues) expressed in baculovirus-infected insect cells using RHK(Ac)K(Ac)AMC as substrate after 60 mins by fluorimeter, Ki = 2.706 μM. 29589441
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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
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]
Kinase Assay 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 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.
In Vivo
In vivo

TMP269 is a selective class IIa HDAC inhibitor.

Chemical Information & Solubility

Molecular Weight 514.52 Formula

C25H21F3N4O3S
CAS No. 1314890-29-3 SDF Download TMP269 SDF
Smiles C1COCCC1(CNC(=O)C2=CC=CC(=C2)C3=NOC(=N3)C(F)(F)F)C4=NC(=CS4)C5=CC=CC=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (194.35 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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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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