INH6
INH6 is a potent inhibitor of Hec1/Nek2 [1].
Hec1 is an oncogene that involved in spindle checkpoint signaling and is overexpressed in many human cancers. Nek2 is a serine/threonine-protein kinase that phosphorylates Hec1, which is critical for its mitotic function and cell survival [1].
INH6 is a potent Hec1/Nek2 inhibitor. INH6 inhibited Hec1/Nek2 function through protein degradation that led to chromosome mis-segregation and cell death. In MDA-MB468 and MDA-MB231 human breast cancer cell lines, HeLa human cervical cancer line and K562 human erythromyeloblastoid leukemia cell line, INH6 exhibited significantly anti-proliferation activities with IC50 values of 2.1, 1.7, 2.4 and 2.5 µM, respectively. In HeLa cell extract, INH6-conjugated matrix selectively co-precipitated with cellular Hec1, which suggested that INH6 bound to cellular Hec1. In Hela cells, INH6 (6.25 µM) reduced Nek2 by 50% at 8-11 h. In addition, INH6 slightly reduced Hec1 over time. Also, INH6 increased mitotic population with multipolar spindle configurations. In HeLa cells expressing the chromosome marker protein H2B-GFP, INH6 increased chromosome misalignment. In HeLa cells, INH6 exhibited progressive morphological changes of dying cells and induced apoptosis by 20% [1].
Reference:
[1]. Qiu XL, Li G, Wu G, et al. Synthesis and biological evaluation of a series of novel inhibitor of Nek2/Hec1 analogues. J Med Chem, 2009, 52(6): 1757-1767.
Storage | Desiccate at -20°C |
M.Wt | 322.42 |
Cas No. | 1001753-24-7 |
Formula | C19H18N2OS |
Solubility | ≥32.2 mg/mL in DMSO; insoluble in H2O; ≥3.55 mg/mL in EtOH with gentle warming and ultrasonic |
SDF | Download SDF |
Canonical SMILES | O=C(C1=CC=CC=C1)NC2=NC(C3=C(C)C=C(C)C=C3C)=CS2 |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Description | INH6 is a potent inhibitor of Hec1 | |||||
Targets | Hec1/Nek2 complex | |||||
IC50 |
Quality Control & MSDS
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Chemical structure
