Name: TAI-1
Price: 298.00 USD

- Overview
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    Background
    
    TAI-1 is a highly potent, first-in-class inhibitor of Hec1 with IC50 of TAI-1 has a GI50 of 13.48 nM (K562 cells), which is close to 1000 times improvement in potency compared to INH1 (GI50 =11.7 μM). TAI-1 showed strong inhibition across a broad spectrum of tumor cells. TAI-1 interrupted Hec1-Nek2 protein interaction, led to Nek2 degradation, induced significant chromosomal misalignment in metaphase, and induced apoptotic cell death. TAI-1 was orally active in in vivo animal models of triple negative colon cancer, breast cancer and liver cancer. Preliminary toxicity shows no effect on the organ weights, body weights and blood indices at efficacious doses. TAI-1 shows high specificity to cancer cells and to target and had no effect on the cardiac channel hERG. TAI-1 is synergistic with topotecan, doxorubicin and paclitaxel in breast, leukemia and liver cancer cells. Sensitivity to TAI-1 was associated with the status of P53 and RB gene. Knockdown of P53 and RB in cancer cells increased sensitivity to TAI-1.
    
    [1]. Huang LY, Lee YS, Huang JJ et al. Characterization of the biological activity of a potent small molecule Hec1 inhibitor TAI-1. J Exp Clin Cancer Res. 2014 Jan 9;33:6. doi: 10.1186/1756-9966-33-6.
- Properties
  - Alternative Name
    
    4-(4-(4-methoxyphenoxy)-2,6-dimethylphenyl)-N-(1-(pyridin-4-yl)vinyl)thiazol-2-amine
    
    CAS Number
    
    1334921-03-7
    
    Molecular Formula
    
    C24H21N3O3S
    
    Molecular Weight
    
    431.51
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥43.2 mg/mL in DMSO; insoluble in H2O; ≥3.17 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

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