Tacedinaline (CI994)

For research use only.

Catalog No.S2818 Synonyms: PD-123654, GOE-5549, Acetyldinaline

32 publications

Tacedinaline (CI994) Chemical Structure

CAS No. 112522-64-2

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 90 In stock
USD 70 In stock
USD 270 In stock
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Selleck's Tacedinaline (CI994) has been cited by 32 publications

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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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-231 cells NVvGeY5CT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWK1JIRigXN? MnfVS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB3IHThfZMh[nliTWTUJIF{e2G7LDDHTVUxRTBwMUeg{txO NX;ES5VROTh3NEO5NFI>
human PC3 cells NHjyWVFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXnMbVFwPSCmYYnz MWfHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiNTDkZZl{KGK7IF3UWEBie3OjeTygS2k2OD1yLkK5JO69VQ>? M1TTV|E5PTR|OUCy
human HCT116 cells NXzOc5o{S3m2b4TvfIlkyqCjc4PhfS=> MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTRizszN MYexO|k1OTZ{NR?=
293T cells MV3GeY5kfGmxbjDhd5NigQ>? M1jMN2lvcGmkaYTpc44hd2ZiSFTBR{BqdiB{OUPUJINmdGy|LDDJR|UxRTZizszN M17ke|E4QTRzNkK1
human LNCap NIC5ZXFRem:uaX\ldoF1cW:wIHHzd4F6 NYKyR2tNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMUmNieCCkeTDNWHQh[XO|YYpvwKwhUUN3ME23MlQh|ryP NYnKWos2OThzNk[0OlU>
human NCI-H661 cells NXXKSHlmWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlHMOFghcA>? MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IOlYyKGOnbHzzJIFnfGW{IES4JIhzeyxiSVO1NF0zOCEQvF2= NXrWeZN3OTh4OUKzPVc>
human NCI-H661 cells M3TCZ2Z2dmO2aX;uJIF{e2G7 NVPGTYRQPiCq NFG2VWZKdmirYnn0bY9vKG:oIFjERWMhcW5iaIXtZY4hVkOLLVi2OlEh[2WubIOgZZN{\XO|ZXSgZZMhcGm|dH;u[UBJPCCjY3X0fYxifGmxbjDh[pRmeiB4IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MVmxPFY6OjN7Nx?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 30108928     


Dose-dependent antiproliferative activities of chlordinaline against six cancer cell lines. The values represent the means of three experiments. (A) Treatment in A549 cells. (B) Treatment in A375 cells. (C) Treatment in SMMC7721 cells. (D) Treatment in HepG2 cells. (E) Treatment in H1299 cells. (F) Treatment in H460 cells.

30108928
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

Cell Research:

[3]

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  • 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.


    (Only for Reference)
Animal Research:

[4]

- Collapse
  • Animal Models: human prostate tumor model LNCaP
  • Dosages: 535 mg/kg
  • Administration: Administered via oral gavage
    (Only for Reference)

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(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+ddH2O
For best results, use promptly after mixing.
5mg/mL

* 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.

Chemical Information

Molecular Weight 269.3
Formula

C15H15N3O2

CAS No. 112522-64-2
Storage powder
in solvent
Synonyms PD-123654, GOE-5549, Acetyldinaline
Smiles CC(=O)NC1=CC=C(C=C1)C(=O)NC2=CC=CC=C2N

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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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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID