Home Epigenetics HDAC inhibitor Tacedinaline (CI994) For research use only.

Tacedinaline (CI994)

Synonyms: PD-123654, GOE-5549, Acetyldinaline

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.

Tacedinaline (CI994) Chemical Structure

Tacedinaline (CI994) Chemical Structure

CAS No. 112522-64-2

Purity & Quality Control

Tacedinaline (CI994) Related Products

Signaling Pathway

HDAC Signaling Pathways

HDAC Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-231 cells Growth inhibition assay 5 days Growth inhibition of human MDA-MB-231 cells after 5 days by MTT assay, GI50=0.17 μM 18543902
human PC3 cells Growth inhibition assay 5 days Growth inhibition of human PC3 cells after 5 days by MTT assay, GI50=0.29 μM 18543902
human HCT116 cells Cytotoxic assay Cytotoxicity against human HCT116 cells by MTT assay, IC50=4 μM 17941625
293T cells Function assay Inhibition of HDAC in 293T cells, IC50=6 μM 17941625
human LNCap Proliferation assay Antiproliferative activity against human LNCap by MTT assay， IC50=7.4 μM 18166465
human NCI-H661 cells Proliferation assay 48 h Antiproliferative activity against human NCI-H661 cells after 48 hrs, IC50=20 μM 18692397
human NCI-H661 cells Function assay 6 h Inhibition of HDAC in human NCI-H661 cells assessed as histone H4 acetylation after 6 hrs by Western blot analysis 18692397
Click to View More Cell Line Experimental Data

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
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]
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 30108928
In Vivo
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]
Animal Research Animal Models human prostate tumor model LNCaP
Dosages 535 mg/kg
Administration Administered via oral gavage

Chemical Information & Solubility

Molecular Weight 269.3 Formula

C15H15N3O2
CAS No. 112522-64-2 SDF Download Tacedinaline (CI994) SDF
Smiles CC(=O)NC1=CC=C(C=C1)C(=O)NC2=CC=CC=C2N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 54 mg/mL ( (200.51 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : 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.

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