1. Apoptosis Cell Cycle/DNA Damage
  2. Apoptosis NEKs
  3. T-1101

T-1101 (TAI-95) is an orally active inhibitor for mitose regulating highly expressed oncoprotein 1 (Hec1). T-1101 blocks the interaction between Hec1 and NEK2, exhibits cytotoxicity in human liver cancer cells with GI50 of 15-70 nM. T-1101 induces apoptosis in Huh-7. T-1101 exhibits antitumor efficacy in mouse models.

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T-1101 Chemical Structure

T-1101 Chemical Structure

CAS No. : 1438638-83-5

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Description

T-1101 (TAI-95) is an orally active inhibitor for mitose regulating highly expressed oncoprotein 1 (Hec1). T-1101 blocks the interaction between Hec1 and NEK2, exhibits cytotoxicity in human liver cancer cells with GI50 of 15-70 nM. T-1101 induces apoptosis in Huh-7. T-1101 exhibits antitumor efficacy in mouse models[1].

IC50 & Target

NEK2

 

Cellular Effect
Cell Line Type Value Description References
COLO 205 GI50
29.1 nM
Compound: 9j
Antiproliferative activity against human COLO 205 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
Antiproliferative activity against human COLO 205 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
[PMID: 32113126]
HeLa IC50
21.1 nM
Compound: 9j
Antiproliferative activity against human HeLa cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
Antiproliferative activity against human HeLa cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
[PMID: 32113126]
Huh-7 GI50
34.98 nM
Compound: 9j
Antiproliferative activity against human Huh-7 cells by CellTiter 96 Aqueous One Solution Reagent based assay
Antiproliferative activity against human Huh-7 cells by CellTiter 96 Aqueous One Solution Reagent based assay
[PMID: 32113126]
Huh-7 GI50
59.9 nM
Compound: 9j
Anticancer activity against human Huh-7 cells after 24 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
Anticancer activity against human Huh-7 cells after 24 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
[PMID: 32113126]
K562 IC50
18 nM
Compound: 9j
Antiproliferative activity against human K562 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
Antiproliferative activity against human K562 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
[PMID: 32113126]
MDA-MB-231 IC50
14.8 nM
Compound: 9j
Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
[PMID: 32113126]
MDA-MB-468 IC50
21.5 nM
Compound: 9j
Antiproliferative activity against human MDA-MB-468 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
Antiproliferative activity against human MDA-MB-468 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
[PMID: 32113126]
U2OS GI50
83.2 nM
Compound: 9j
Antiproliferative activity against human U2OS cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
Antiproliferative activity against human U2OS cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
[PMID: 32113126]
U-937 GI50
12.4 nM
Compound: 9j
Antiproliferative activity against human U-937 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
Antiproliferative activity against human U-937 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
[PMID: 32113126]
Molecular Weight

493.60

Formula

C24H23N5O3S2

CAS No.
SMILES

O=C(C1=CC=NC=C1)NC2=NC(C3=C(C)C=C(SC4=NC=C(OCCOC)N=C4)C=C3C)=CS2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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T-1101
Cat. No.:
HY-120356
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