1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. Tacedinaline

Tacedinaline  (Synonyms: N-acetyldinaline; CI-994; Goe-5549)

Cat. No.: HY-50934 Purity: 99.32%
SDS COA Handling Instructions

Tacedinaline (N-acetyldinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively.

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

Tacedinaline Chemical Structure

Tacedinaline Chemical Structure

CAS No. : 112522-64-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 35 In-stock
10 mg USD 55 In-stock
50 mg USD 83 In-stock
100 mg USD 121 In-stock
200 mg USD 211 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Tacedinaline (N-acetyldinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively.

IC50 & Target[1]

HD1

0.9 μM (IC50)

HD2

0.9 μM (IC50)

HD3

1.2 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
A-375 IC50
11.29 μM
Compound: CI994
Antiproliferative activity against human A375 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A375 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31003060]
A-375 IC50
11.29 μM
Compound: CI994
Antiproliferative activity against human A375 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human A375 cells after 72 hrs by CCK-8 assay
[PMID: 29202397]
A-375 IC50
11.3 μM
Compound: Tacedinaline
Antiproliferative activity against human A375 cells after 72 hrs CCK8 assay
Antiproliferative activity against human A375 cells after 72 hrs CCK8 assay
[PMID: 30108928]
A-375 IC50
9.64 μM
Compound: 5; CI994
Antiproliferative activity against human A375 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human A375 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
[PMID: 31103900]
A549 IC50
10.17 μM
Compound: 2
Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay
[PMID: 30045621]
A549 IC50
15.96 μM
Compound: CI-994
Cytotoxicity against human A549 cells assessed as decrease in cell viability measured after 72 hrs by CellTiter-Glo Luminescent assay
Cytotoxicity against human A549 cells assessed as decrease in cell viability measured after 72 hrs by CellTiter-Glo Luminescent assay
[PMID: 31223439]
A549 IC50
16.45 μM
Compound: 5; CI994
Antiproliferative activity against human A549 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
[PMID: 31103900]
A549 IC50
20.1 μM
Compound: CI994
Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31003060]
A549 IC50
20.1 μM
Compound: 6; CI994
Antiproliferative activity against human A549 cells after 72 hrs by CCK-8 reagent based assay
Antiproliferative activity against human A549 cells after 72 hrs by CCK-8 reagent based assay
[PMID: 28391133]
A549 IC50
20.1 μM
Compound: Tacedinaline
Antiproliferative activity against human A549 cells after 72 hrs CCK8 assay
Antiproliferative activity against human A549 cells after 72 hrs CCK8 assay
[PMID: 30108928]
Epithelial cell IC50
> 50 μM
Compound: 18, pfizer,CI-994
Cytotoxicity against human mammary epithelial cells by MTT assay
Cytotoxicity against human mammary epithelial cells by MTT assay
[PMID: 17941625]
HCT-116 IC50
10 μM
Compound: 5; CI-994
Cytotoxicity in human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity in human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 28885834]
HCT-116 IC50
4 μM
Compound: 18, pfizer,CI-994
Cytotoxicity against human HCT116 cells by MTT assay
Cytotoxicity against human HCT116 cells by MTT assay
[PMID: 17941625]
HCT-116 IC50
6.39 μM
Compound: 5; CI994
Antiproliferative activity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
[PMID: 31103900]
HCT-116 IC50
7.71 μM
Compound: CI994
Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31003060]
HCT-116 IC50
7.71 μM
Compound: CI994
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay
[PMID: 29202397]
HCT-116 IC50
7.71 μM
Compound: 6; CI994
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 reagent based assay
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 reagent based assay
[PMID: 28391133]
HCT-116 EC50
8.4 μM
Compound: Cl-994
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 48 hrs by cell-titer glo assay
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 48 hrs by cell-titer glo assay
[PMID: 35293758]
HCT-116 IC50
9.83 μM
Compound: 2
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay
[PMID: 30045621]
HeLa IC50
1.81 μM
Compound: 5; CI994
Inhibition of HDAC in human HeLa cell nuclear extract assessed as decrease in deacetylation of FLUOR DE LYS Green substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence based assay
Inhibition of HDAC in human HeLa cell nuclear extract assessed as decrease in deacetylation of FLUOR DE LYS Green substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence based assay
[PMID: 31103900]
HeLa IC50
1.81 μM
Compound: CI994
Inhibition of HDAC in human HeLa cell nuclear extract using fluor-de-lys-green as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay
Inhibition of HDAC in human HeLa cell nuclear extract using fluor-de-lys-green as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay
[PMID: 31003060]
HeLa IC50
13.43 μM
Compound: 5; CI994
Antiproliferative activity against human HeLa cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
[PMID: 31103900]
HeLa IC50
18.02 μM
Compound: CI994
Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 assay
[PMID: 29202397]
HeLa IC50
18.78 μM
Compound: CI994
Antiproliferative activity against human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31003060]
HepG2 IC50
10 μM
Compound: 5; CI-994
Cytotoxicity in human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity in human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 28885834]
HepG2 IC50
18.5 μM
Compound: Tacedinaline
Antiproliferative activity against human HepG2 cells after 72 hrs CCK8 assay
Antiproliferative activity against human HepG2 cells after 72 hrs CCK8 assay
[PMID: 30108928]
HepG2 IC50
18.51 μM
Compound: 6; CI994
Antiproliferative activity against human HepG2 cells after 72 hrs by CCK-8 reagent based assay
Antiproliferative activity against human HepG2 cells after 72 hrs by CCK-8 reagent based assay
[PMID: 28391133]
LNCaP IC50
7.4 μM
Compound: 3, CI-994
Antiproliferative activity against human LNCap by MTT assay
Antiproliferative activity against human LNCap by MTT assay
[PMID: 18166465]
MCF7 IC50
13.16 μM
Compound: 2
Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay
[PMID: 30045621]
MDA-MB-231 GI50
0.17 μM
Compound: 1
Growth inhibition of human MDA-MB-231 cells after 5 days by MTT assay
Growth inhibition of human MDA-MB-231 cells after 5 days by MTT assay
[PMID: 18543902]
MGC-803 IC50
11.6 μM
Compound: CI994
Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 assay
[PMID: 29202397]
MGC-803 IC50
11.6 μM
Compound: 6; CI994
Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 reagent based assay
Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 reagent based assay
[PMID: 28391133]
NCI-H1299 IC50
33.79 μM
Compound: CI994
Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK-8 assay
[PMID: 29202397]
NCI-H1299 IC50
33.8 μM
Compound: Tacedinaline
Antiproliferative activity against human H1299 cells after 72 hrs CCK8 assay
Antiproliferative activity against human H1299 cells after 72 hrs CCK8 assay
[PMID: 30108928]
NCI-H1299 IC50
6.79 μM
Compound: 2
Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay
[PMID: 30045621]
NCI-H460 IC50
9.7 μM
Compound: Tacedinaline
Antiproliferative activity against human H460 cells after 72 hrs CCK8 assay
Antiproliferative activity against human H460 cells after 72 hrs CCK8 assay
[PMID: 30108928]
NCI-H661 IC50
20 μM
Compound: CI-994
Antiproliferative activity against human NCI-H661 cells after 48 hrs
Antiproliferative activity against human NCI-H661 cells after 48 hrs
[PMID: 18692397]
NIH3T3 IC50
9.05 μM
Compound: CI994
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
[PMID: 31003060]
NIH3T3 IC50
9.05 μM
Compound: 5; CI994
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay
[PMID: 31103900]
PC-3 GI50
0.29 μM
Compound: 1
Growth inhibition of human PC3 cells after 5 days by MTT assay
Growth inhibition of human PC3 cells after 5 days by MTT assay
[PMID: 18543902]
Sf9 IC50
147 nM
Compound: 27; CI-994
Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC2 expressed in Sf9 insect cells using FAM-labeled acetylated peptide A as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence ass
Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC2 expressed in Sf9 insect cells using FAM-labeled acetylated peptide A as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence ass
[PMID: 30735902]
Sf9 IC50
41 nM
Compound: 27; CI-994
Inhibition of recombinant human full length C-terminal His/FALG-tagged HDAC1 expressed in Sf9 insect cells using FAM-labeled acetylated peptide A as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence
Inhibition of recombinant human full length C-terminal His/FALG-tagged HDAC1 expressed in Sf9 insect cells using FAM-labeled acetylated peptide A as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence
[PMID: 30735902]
SMMC-7721 IC50
> 32 μM
Compound: CI994
Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31003060]
SMMC-7721 IC50
14.06 μM
Compound: 5; CI994
Antiproliferative activity against human SMMC7721 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human SMMC7721 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
[PMID: 31103900]
SMMC-7721 IC50
16.9 μM
Compound: Tacedinaline
Antiproliferative activity against human SMMC7721 cells after 72 hrs CCK8 assay
Antiproliferative activity against human SMMC7721 cells after 72 hrs CCK8 assay
[PMID: 30108928]
In Vitro

Tacedinaline (N-acetyldinaline) is a novel oral compound with a wide spectrum of antitumor activity in preclinical models. The mechanism of action may involve inhibition of histone deacetylation and cell cycle arrest. Tacedinaline (N-acetyldinaline) is combined with antineoplastic agents commonly used in non-small cell lung cancer cell line management, a marked synergism of action (R=1.8, R=1.5) is observed between Tacedinaline (N-acetyldinaline) (40 μM) and gemcitabine (0.01 μM) at 48 and 72 h of treatment[2].
Tacedinaline (N-acetyldinaline) inhibits mitogen-stimulated blood lymphocyte proliferation with an IC50 value of 3 μM[4].

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

In Vivo

Tacedinaline (CI-994) can effect lymphoid tissue in rats within 1 day of a single oral dose, that effects are generally reversible within 7 days[4].

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

Clinical Trial
Molecular Weight

269.30

Formula

C15H15N3O2

CAS No.
Appearance

Solid

Color

White to gray

SMILES

O=C(NC1=C(N)C=CC=C1)C2=CC=C(NC(C)=O)C=C2

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 : ≥ 50 mg/mL (185.67 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7133 mL 18.5667 mL 37.1333 mL
5 mM 0.7427 mL 3.7133 mL 7.4267 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
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (9.28 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

Purity: 99.32%

References
Animal Administration
[4]

Rats: To characterize the effects of Tacedinaline (CI-994) on lymphoid tissue, male rats are administered single oral doses at 0 (vehicle control), 10, 23, and 45 mg/kg and killed up to 7 days after dosing for evaluation of white blood cell differentials, bone marrow differentials, lymphoid tissue weights, and selected histopathology of lymphoid tissue[4].

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 3.7133 mL 18.5667 mL 37.1333 mL 92.8333 mL
5 mM 0.7427 mL 3.7133 mL 7.4267 mL 18.5667 mL
10 mM 0.3713 mL 1.8567 mL 3.7133 mL 9.2833 mL
15 mM 0.2476 mL 1.2378 mL 2.4756 mL 6.1889 mL
20 mM 0.1857 mL 0.9283 mL 1.8567 mL 4.6417 mL
25 mM 0.1485 mL 0.7427 mL 1.4853 mL 3.7133 mL
30 mM 0.1238 mL 0.6189 mL 1.2378 mL 3.0944 mL
40 mM 0.0928 mL 0.4642 mL 0.9283 mL 2.3208 mL
50 mM 0.0743 mL 0.3713 mL 0.7427 mL 1.8567 mL
60 mM 0.0619 mL 0.3094 mL 0.6189 mL 1.5472 mL
80 mM 0.0464 mL 0.2321 mL 0.4642 mL 1.1604 mL
100 mM 0.0371 mL 0.1857 mL 0.3713 mL 0.9283 mL
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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.

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Tacedinaline
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