Tacedinaline (CI994)

Catalog No.S2818 Batch:S281803

Technical Data

Formula

C₁₅H₁₅N₃O₂

Molecular Weight

269.3

CAS No.

112522-64-2

Solubility (25°C)*

In vitro

DMSO

54 mg/mL (200.51 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 40%PEG300 2 55%ddH2O

5.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG 300, mix evenly to clarify it; then continue to add 550 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Tacedinaline (CI994, PD-123654, GOE-5549, Acetyldinaline) is a selective class I HDAC inhibitor with IC50 of 0.9, 0.9, 1.2, and >20 μM for human HDAC 1, 2, 3, and 8, respectively. Phase 3.

Targets

HDAC1 ^[1] (Cell-free assay)	HDAC2 ^[1] (Cell-free assay)	HDAC3 ^[1] (Cell-free assay)
0.9 μM	0.9 μM	1.2 μM

In vitro

CI-994 (< 160 mM) shows cytostatic effect with concomitant increase at G0/G1 phase, a reduction at S phase level and increased apoptosis in A-549 and LX-1 cells. ^[2] CI-994 inhibits growth of LNCaP cell with IC50 of 7.4 μM. ^[3] CI-994 exerts activity against several tumor cell lines with greater cytotoxicity against the solid tumors relative to both the leukemia and normal fibroblast cell lines. ^[4] CI-994 inhibits growth of rat leukemia BCLO cells with IC50 of 2.5 μM. ^[5]

In vivo

CI-994 exerts demonstrated antitumor activity against several tumor models, including the chemo-resistant mouse pancreatic ductal carcinoma as well as the human prostate tumor model LNCaP. ^[4]

Protocol (from reference)

Cell Assay:^{^[3]}	Cell lines LNCaP cell lines Concentrations 2.5 μM Incubation Time 2-4 days Method LNCaP cell lines are maintained in RPMI 1640 medium containing 10% fetal bovine serum, 1% penicillin and streptomycin, as the complete culture medium. Cells (2×10⁴) are seeded in 24-well plates and incubated in a 5% CO₂ incubator at 37 °C for 1 day. Cultures are treated with CI-994, alone and in combination on day 2 and 4. Cells are washed on day 2 and 4 and media are changed. Mitochondrial metabolism is measured as a marker for cell growth by adding 100 μL/well MTT (5 mg/mL in medium) with 2 hours incubation at 37 °C on Day 6. Crystals formed are dissolved in 500 μL of DMSO. The absorbance is determined using a microplate reader at 560 nm. The absorbance data are converted into cell proliferation percentage. Each assay is performed in triplicate.
Animal Study:^{^[4]}	Animal Models human prostate tumor model LNCaP Dosages 535 mg/kg Administration Administered via oral gavage

Cell Assay:^{^[3]}

Cell lines
LNCaP cell lines
Concentrations
2.5 μM
Incubation Time
2-4 days
Method
LNCaP cell lines are maintained in RPMI 1640 medium containing 10% fetal bovine serum, 1% penicillin and streptomycin, as the complete culture medium. Cells (2×10⁴) are seeded in 24-well plates and incubated in a 5% CO₂ incubator at 37 °C for 1 day. Cultures are treated with CI-994, alone and in combination on day 2 and 4. Cells are washed on day 2 and 4 and media are changed. Mitochondrial metabolism is measured as a marker for cell growth by adding 100 μL/well MTT (5 mg/mL in medium) with 2 hours incubation at 37 °C on Day 6. Crystals formed are dissolved in 500 μL of DMSO. The absorbance is determined using a microplate reader at 560 nm. The absorbance data are converted into cell proliferation percentage. Each assay is performed in triplicate.

Animal Study:^{^[4]}

Animal Models
human prostate tumor model LNCaP
Dosages
535 mg/kg
Administration
Administered via oral gavage

References

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Customer Product Validation

: Data from [Data independently produced by , , J Biol Chem, 2016, 291(14):7386-95]

: Data from [Data independently produced by , , Cell Oncol (Dordr), 2017, 40(3):263-279]

: Data from [Data independently produced by , , Int J Biochem Cell Biol, 2016, 81(Pt A):82-91]

: Data from [Data independently produced by , , Anticancer Res, 2018, 38(1):271-277]

Selleck's Tacedinaline (CI994) has been cited by 40 publications

In-Cell Testing of Zinc-Dependent Histone Deacetylase Inhibitors in the Presence of Class-Selective Fluorogenic Substrates: Potential and Limitations of the Method [ Biomedicines, 2024, 12(6)1203]	PubMed: 38927410
CUDC-907, a dual PI3K/histone deacetylase inhibitor, increases meta-iodobenzylguanidine uptake (123/131I-mIBG) in vitro and in vivo: a promising candidate for advancing theranostics in neuroendocrine tumors [ J Transl Med, 2023, 21(1):604]	PubMed: 37679770
Histone deacetylase III interactions with BK polyomavirus large tumor antigen may affect protein stability [ Virol J, 2023, 20(1):155]	PubMed: 37464367
MyoD is a 3D genome structure organizer for muscle cell identity [ Nat Commun, 2022, 13(1):205]	PubMed: 35017543
Development of Human Adrenocortical Adenoma (HAA1) Cell Line from Zona Reticularis [ Int J Mol Sci, 2022, 24(1)584]	PubMed: 36614027
Rb-E2F-HDAC Repressor Complexes Control Interferon-Induced Repression of Adenovirus To Promote Persistent Infection [ J Virol, 2022, e0044222]	PubMed: 35546119
Pre-Senescence Induction in Hepatoma Cells Favors Hepatitis C Virus Replication and Can Be Used in Exploring Antiviral Potential of Histone Deacetylase Inhibitors [ Int J Mol Sci, 2021, 22(9)4559]	PubMed: 33925399
Combination Treatment of CI-994 With Etoposide Potentiates Anticancer Effects Through a Topoisomerase II-Dependent Mechanism in Atypical Teratoid/Rhabdoid Tumor (AT/RT) [ Front Oncol, 2021, 11:648023]	PubMed: 34367950
HDAC3 inhibitor RGFP966 controls bacterial growth and modulates macrophage signaling during Mycobacterium tuberculosis infection [ Tuberculosis (Edinb), 2021, 127:102062]	PubMed: 33639591
Protein acetylation derepresses Serotonin Synthesis to potentiate Pancreatic Beta-Cell Function through HDAC1-PKA-Tph1 signaling [ Theranostics, 2020, 10(16):7351-7368]	PubMed: 32641996

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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