TMP269

Alias: TMP269; TMP-269;TMP 269
Cat No.:V0269 Purity: ≥98%
TMP269 is a novel, potent, selective inhibitor of class IIa HDAC(4/5/7/9) with potential anticancer activity.
TMP269 Chemical Structure CAS No.: 1314890-29-3
Product category: HDAC
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

TMP269 is a novel, potent, selective inhibitor of class IIa HDAC(4/5/7/9) with potential anticancer activity. It blocks HDAC(4/5/7/9) with IC50 of 157 nM, 97 nM, 43 nM and 23 nM, respectively.

Biological Activity I Assay Protocols (From Reference)
Targets
HDAC9 ( IC50 = 23 nM ); HDAC7 ( IC50 = 43 nM ); HDAC5 ( IC50 = 97 nM ); HDAC4 ( IC50 = 157 nM ); HDAC8 ( IC50 = 42000 nM ); HDAC6 ( IC50 = 82000 nM )
ln Vitro

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

ln Vivo
N/A
Enzyme Assay
At Reaction Biology Corp., dose-response studies are carried out using ten concentrations in a triplicate dilution series, starting from a maximum final compound concentration of 100 μM in the reaction mixture. The same basic idea underlies all assays, including the HDAC9 assay previously mentioned: HDAC deacetylates acetylated or trifluoroacetylated lysine residues on fluorogenic peptide substrates. The substrate used by HDAC1, HDAC2, HDAC3, HDAC6, HDAC10, and HDAC11 was based on p53 residues 379–382 (Arg–His–Lys–Lys(Ac)). The diacetylated peptide substrate for HDAC8 is Arg-His-Lys(Ac)-Lys(Ac) and is based on residues 379–382 of p53. The class IIa HDAC-specific fluorogenic substrate, Boc-Lys(trifluoroacetyl)-AMC, was utilized in the HDAC4, HDAC5, HDAC7, and HDAC9 assays. 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 is used for all reactions. 50 μM HDAC substrate is used in these reactions, which are then incubated for two hours at 30 °C and developed using trichostatin A and trypsin.
Cell Assay
The RosetteSep Human CD4+ T cell enrichment kit's manufacturer's instructions are followed to isolate human CD4+ T cells from whole blood via negative selection. The cells are then 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 a 72-hour period. According to the manufacturer's instructions (Cell Proliferation Assay Kit I (MTT)), mitochondrial function or cell viability is determined and is expressed as a percentage of control (no inhibitor) wells.
Animal Protocol
N/A
N/A
References

[1]. Nat Chem Biol . 2013 May;9(5):319-25.

[2]. Am J Physiol Cell Physiol . 2014 May 15;306(10):C961-71.

[3]. Biochem Biophys Res Commun . 2018 Sep 5;503(2):1087-1091.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C25H21F3N4O3S
Molecular Weight
514.52
Exact Mass
514.13
Elemental Analysis
C, 58.36; H, 4.11; F, 11.08; N, 10.89; O, 9.33; S, 6.23
CAS #
1314890-29-3
Appearance
White to off-white solid powder
SMILES
C1COCCC1(CNC(=O)C2=CC=CC(=C2)C3=NOC(=N3)C(F)(F)F)C4=NC(=CS4)C5=CC=CC=C5
InChi Key
HORXBWNTEDOVKN-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H21F3N4O3S/c26-25(27,28)22-31-20(32-35-22)17-7-4-8-18(13-17)21(33)29-15-24(9-11-34-12-10-24)23-30-19(14-36-23)16-5-2-1-3-6-16/h1-8,13-14H,9-12,15H2,(H,29,33)
Chemical Name
N-[[4-(4-phenyl-1,3-thiazol-2-yl)oxan-4-yl]methyl]-3-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]benzamide
Synonyms
TMP269; TMP-269;TMP 269
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~100 mg/mL (~194.4 mM)
Water: <1 mg/mL
Ethanol: ~2 mg/mL (~3.9 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9436 mL 9.7178 mL 19.4356 mL
5 mM 0.3887 mL 1.9436 mL 3.8871 mL
10 mM 0.1944 mL 0.9718 mL 1.9436 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • TMP269
    Class IIa HDAC catalytic domain activity is necessary for mitogenic signaling induced by ANG II in intestinal epithelial cells.Am J Physiol Cell Physiol.2014 May 15;306(10):C961-71.
  • TMP269
    Class IIa HDAC inhibition by MC1568 or TMP269 does not prevent PKD1 activation, HDAC4 and HDAC5 phosphorylation, and HDAC5 nuclear extrusion in IEC-18 cells stimulated with ANG II.Am J Physiol Cell Physiol.2014 May 15;306(10):C961-71.
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