TAI-1

Research use only, not for human use.

A potent, small molecule Hec1 inhibitor that disrupts Hec1-Nek2 protein interaction wide anti-cancer spectrum.

A potent, small molecule Hec1 inhibitor that disrupts Hec1-Nek2 protein interaction wide anti-cancer spectrum (GI50=13.48 nM K562 cells); displays 1,000 times improvement in potency compared to INH1, shows nM levels for the majority of the NCI-60 panel; targets the Hec1-Nek2 pathway, induces chromosomal misalignment and apoptosis, effectively inhibits tumor growth in multiple cancer xenograft models.

TAI-1 disrupts Hec1-Nek2 protein interaction, leads to Nek2 degradation, induces significant chromosomal misalignment in metaphase, and induces apoptotic cell death.TAI-1 induces cancer cell death through the induction of cleavage of apoptotic proteins Caspase 3 and PARP and degradation of anti-apoptotic proteins MCL-1 and suggests that TAI-1 leads to activation of the apoptotic pathways.TAI-1 is effective in many cancer cells, such as Chronic myeloid leukemia, Cervical cancer, Breast, metastatic-pleural, invasive ductal carcinoma, Acute myeloid leukemia, Myelogenous leukemia, Colorectal carcinoma cells, with GI50 less than 100 nM.

TAI-1 (20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID) inhibits tumor growth in multiple cancer xenograft models. Animal Model:C.B-17 SCID mice (6-7 weeks, 21-24 g). Dosage:20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID.Administration:QDx28 cycles.Result:Led to significant tumor growth retardation in Huh-7 and modest tumor inhibition was noted tor the Colo205 and MDA-MB-231 models.

TAI1 | Hec1 inhibitor HAI-1

Cell Cycle/DNA Damage

Hec1/Nek2

Hec1

Cancer

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1334921-03-7

431.51

C24H21N3O3S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (231.74 mM)

O=C(C1=CC=NC=C1)NC2=NC(C3=C(C)C=C(OC4=CC=C(OC)C=C4)C=C3C)=CS2

N-(4-(4-(4-methoxyphenoxy)-2,6-dimethylphenyl)thiazol-2-yl)isonicotinamide

(-20℃)

With Ice Pack

≥ 2 years