2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. TMP269

TMP269 is a novel and selective class IIa histone deacetylase (HDAC) inhibitor with IC50s of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.

For research use only. We do not sell to patients.

TMP269 Chemical Structure

TMP269 Chemical Structure

CAS No. : 1314890-29-3

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solution
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Solid
5 mg USD 132 In-stock
10 mg USD 198 In-stock
25 mg USD 330 In-stock
50 mg USD 594 In-stock
100 mg USD 1122 In-stock
200 mg USD 1452 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

TMP269 Related Antibodies

Top Publications Citing Use of Products

View All HDAC Isoform Specific Products:

View All Isoforms
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

TMP269 is a novel and selective class IIa histone deacetylase (HDAC) inhibitor with IC50s of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.

IC50 & Target[1]

HDAC9

23 nM (IC50)

HDAC7

43 nM (IC50)

HDAC5

97 nM (IC50)

HDAC4

157 nM (IC50)

HDAC8

42000 nM (IC50)

HDAC6

82000 nM (IC50)

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]. As with HDAC4 knockdown, TMP269 significantly enhances cytotoxicity induced by CFZ in MM cell lines, upregulating ATF4 and CHOP and inducing apoptosis. TMP269 does not hyperacetylate histone H3K9 or α-tubulin in MM cell lines, confirming that it has no inhibitory effects on class I or IIb HDACs. In a dosedependent manner, TPM269-induced cytotoxicity is associated with cleavage of caspase-8, -9, -3 and PARP, consistent with apoptosis[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TMP269 Related Antibodies
In Vivo

In vivo angiogenesis assay, MDA-MB-231 cells are mixed with growth factor-reduced Matrigel and implanted subcutaneously into the flanks of nude mice. TMP269 (subcutaneous injection; 15 mg/kg; every other day; 10 days) shows an obvious antiangiogenic effect with 76% inhibition of angiogenesis in mice[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

514.52

Formula

C25H21F3N4O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC1(C2=NC(C3=CC=CC=C3)=CS2)CCOCC1)C4=CC=CC(C5=NOC(C(F)(F)F)=N5)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (194.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Kinase Assay
[1]

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. 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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9436 mL 9.7178 mL 19.4356 mL 48.5890 mL
5 mM 0.3887 mL 1.9436 mL 3.8871 mL 9.7178 mL
10 mM 0.1944 mL 0.9718 mL 1.9436 mL 4.8589 mL
15 mM 0.1296 mL 0.6479 mL 1.2957 mL 3.2393 mL
20 mM 0.0972 mL 0.4859 mL 0.9718 mL 2.4294 mL
25 mM 0.0777 mL 0.3887 mL 0.7774 mL 1.9436 mL
30 mM 0.0648 mL 0.3239 mL 0.6479 mL 1.6196 mL
40 mM 0.0486 mL 0.2429 mL 0.4859 mL 1.2147 mL
50 mM 0.0389 mL 0.1944 mL 0.3887 mL 0.9718 mL
60 mM 0.0324 mL 0.1620 mL 0.3239 mL 0.8098 mL
80 mM 0.0243 mL 0.1215 mL 0.2429 mL 0.6074 mL
100 mM 0.0194 mL 0.0972 mL 0.1944 mL 0.4859 mL
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TMP269 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TMP2691314890-29-3TMP 269TMP-269HDACHistone deacetylasesInhibitorinhibitorinhibit

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