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CI-994

Cat. No. M2236

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CI-994 Structure
Synonym:

Tacedinaline, PD 123654

Size Price Availability Quantity
10mM*1mL in DMSO USD 55 In stock
10mg USD 50 In stock
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Quality Control & Documentation
Biological Activity

CI-994 (N-acetyldinaline) is a novel oral agent which inhibits HDAC1, with a wide spectrum of antitumor activity in preclinical models, in vitro and in vivo. CI-994 inhibits growth of LNCaP cell with IC50 of 7.4 μM. CI-994 inhibits growth of rat leukemia BCLO cells with IC50 of 2.5 μM. The effect of CI-994, as demonstrated by recovery experiments, was cytostatic and seemed to be superimposable in both cell lines. Cytofluorimetric analysis to assess cell cycle perturbation and apoptosis was performed after 24 h of treatment, indicating a cell block with concomitant increase at G0/G1 phase, a reduction at S phase level at 20, 40, 80, and 160 microM, and apoptosis at the higher concentration (160 microM). CI-994 is currently in a phase III clinical trial in patients with lung cancer.

Product Citations
Customer Product Validations & Biological Datas
Source AIDS Res Hum Retroviruses (2016). Figure 3. CI-994
Method Immunoblots
Cell Lines CD4+ T cells
Concentrations 0.57 μM
Incubation Time 24 h
Results Both vorinostat and panobinostat, but not tacedinaline, increased CDK9 T-loop phosphorylation in CCL19-treated cells compared to control cells. Vorinostat and panobinostat, but not tacedinaline, also increased histone H3 acetylation in CCl19-treated cells.
Chemical Information
Molecular Weight 269.3
Formula C15H15N3O2
CAS Number 112522-64-2
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Bryan McClarty, et al. Dose Effects of Histone Deacetylase Inhibitor Tacedinaline (CI-994) on Antipsychotic Haloperidol-Induced Motor and Memory Side Effects in Aged Mice

[2] Hee Yeon Kim, et al. Combination Treatment of CI-994 With Etoposide Potentiates Anticancer Effects Through a Topoisomerase II-Dependent Mechanism in Atypical Teratoid/Rhabdoid Tumor (AT/RT)

[3] Di Guo, et al. Histone deacetylase inhibitor CI-994 inhibits osteoclastogenesis via suppressing NF-κB and the downstream c-Fos/NFATc1 signaling pathways

[4] Suxiang Zhang, et al. Class I histone deacetylase (HDAC) inhibitor CI-994 promotes functional recovery following spinal cord injury

[5] I Hubeek, et al. CI-994 (N-acetyl-dinaline) in combination with conventional anti-cancer agents is effective against acute myeloid leukemia in vitro and in vivo

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Keywords: CI-994, Tacedinaline, PD 123654 supplier, HDAC, inhibitors, activators

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