|CAS No.||112522-64-2||Synonyms||PD-123654, GOE-5549, Acetyldinaline|
|Chemical Name||Benzamide, 4-(acetylamino)-N-(2-aminophenyl)-|
|Solubility (25°C) *||In vitro||DMSO||54 mg/mL (200.51 mM)|
|In vivo||5% DMSO+40% PEG 300+ddH2O||5mg/mL|
* <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.
|Description||Tacedinaline (CI994) 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.|
|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.  CI-994 inhibits growth of LNCaP cell with IC50 of 7.4 μM.  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.  CI-994 inhibits growth of rat leukemia BCLO cells with IC50 of 2.5 μM. |
|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. |
|Cell lines||LNCaP cell lines|
|Incubation Time||2-4 days|
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 Models||human prostate tumor model LNCaP|
|Formulation||5% ethanol, 1% P.O.E. and 94% dH20|
|Administration||Administered via oral gavage|
Data from [Data independently produced by , , J Biol Chem, 2016, 291(14):7386-95]
A, 5×106 HeLa, A549, 293T, and H1299 cells were seeded in 10-cm cell culture dishes on day 0 and treated with dimethyl sulfoxide, 10 μM CI994, or 1 μM RGFP966 for 12 h. Cell lysates were collected for Western blotting analysis of Apaf-1 and -actin.
Data from [Data independently produced by , , Cell Oncol (Dordr), 2017, 40(3):263-279]
Apoptosis marker analysis. Daoy and D283 Med cells were exposed to various HDACi 24 h before total RNA samples were prepared for qRT-PCR. Daoy cells were exposed to DMSO, 25 nM TSA, 1 μM SAHA, 1.5 μM MS-275, 0.7 μM mocetinostat, 7 μM tacedinaline, 1.5 nM romidepsin and 2 μM parthenolide, respectively. D283 Med cells were exposed to DMSO, 40 nM TSA, 1.5 μM SAHA, 2 μM MS-275, 0.3 μM mocetinostat, 8 μM tacedinaline, 1 nM romidepsin and 4 μM parthenolide, respectively. Expression of the apoptosis markers BAX and BCL2, as well as the apoptotic BAX/BCL2 ratios, are shown. * p < 0.05; **p < 0.01.
Acetylation site specificities of lysine deacetylase inhibitors in human cells. [Scholz C, et al. Nat Biotechnol, 2015, 10.1038/nbt.3130]PubMed: 25751058
Acetylation of p53 Protein at Lysine 120 Up-regulates Apaf-1 Protein and Sensitizes the Mitochondrial Apoptotic Pathway. [Yun T, et al. J Biol Chem, 2016, 291(14):7386-95]PubMed: 26851285
A substrate-independent TR-FRET histone deacetylase inhibitor assay. [Marks BD, et al. J Biomol Screen, 2011, 16(10):1247-53]PubMed: 21940713
Synergistic anti-cancer effects of epigenetic drugs on medulloblastoma cells. [Yuan J, et al. Cell Oncol (Dordr), 2017, 40(3):263-279]PubMed: 28429280
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