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INH154 

Cat. No.: HY-117154
Handling Instructions

INH154 is a highly potent inhibitor for Nek2 and Hec1 binding (INH), with IC50s of 200 nM and 120 nM for INH in Hela and MB468 cells.

For research use only. We do not sell to patients.

INH154 Chemical Structure

INH154 Chemical Structure

CAS No. : 1587705-63-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
25 mg USD 560 In-stock
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50 mg USD 950 In-stock
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100 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

INH154 is a highly potent inhibitor for Nek2 and Hec1 binding (INH), with IC50s of 200 nM and 120 nM for INH in Hela and MB468 cells.

IC50 & Target

IC50: 200 nM (INH in Hela cells), 120 nM (INH in MB468 cells)[1].

In Vitro

INH154 is highly potent in treating breast tumors with co-elevated expression of Hec1 and Nek2. INH154 is the most potent inhibitor of tumor cell growth. The IC50 values of INH154 in HeLa and MDA-MB-468 cancer cells are 0.20 and 0.12 μM, respectively. INH154 also suppresses the growth of leukemia, osteosarcoma, and glioblastoma cells[1].

In Vivo

Tumor growth rates in mice treated with INH154 are evidently slower than those in control animals in a dose-dependent manner. In agreement with the tumor-growth data, the tumor proliferation index, determined by measuring BrdU staining, is clearly reduced in residual tumors treated with INH154 in comparison with vehicle alone. The expression levels of Nek2 and Hec1 S165 phosphorylation are also substantially reduced in INH154-treated tumors than in vehicle-treated tumors. On the other hand, mice body weights are measured during the 6.5 weeks treatment period and show little difference among treated and control groups. In addition, the toxicity of INHs by treating normal BALB/c ByJNarl mice with high dosage of INH154 (20 mg/kg) shows no significant difference of body weights, blood chemistry, and complete blood count (CBC) analysis among these groups of animals[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5476 mL 12.7382 mL 25.4764 mL
5 mM 0.5095 mL 2.5476 mL 5.0953 mL
10 mM 0.2548 mL 1.2738 mL 2.5476 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
Human triple negative breast cancer MDA-MB-468 cells, which expressed high levels of both Hec1 and Nek2, are used to test the efficacy of tumor growth in mouse xenograft. While tumor volumes reach ~100mm3, mice are randomly divided into 5 treatment groups and began to receive thrice-weekly intraperitoneal (i.p.) injections of vehicle control, 10 mg/kg INH41, 50 mg/kg INH41, 5 mg/kg INH154 or 20 mg/kg INH154. Treatment is continued for 6.5 weeks and the tumor sizes were measured[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

392.52

Formula

C₂₂H₂₄N₄OS

CAS No.

1587705-63-2

SMILES

O=C(C1=CC=NC=C1)NC2=NC(C3=C(C)C=C(N4CCCCC4)C=C3C)=CS2

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
INH154
Cat. No.:
HY-117154
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INH154

Cat. No.: HY-117154