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Cat. No. Product Name CAS No. Information
PC-61480

INH154

1587705-63-2

INH154 is a novel small molecules disrupting Hec1/Nek2 interaction, inhibits HeLa and MDA-MB-468 cancer cells growth with IC50 of 0.20 and 0.12 uM, respectively; suppresses the growth of leukemia, osteosarcoma, and glioblastoma cells, but has no significant growth inhibitory effects on non-tumorigenic fibroblast, HS27 and mammary epithelial cells; triggers Nek2 degradation and eventually cell death, suppresses tumor growth in mice without obvious toxicity.

PC-42194

INH-6

1001753-24-7

A small molecule inhibitor of Nek2/Hec1 that inhibits cell growth of MB231, MB468, HeLa and K562 cells with IC50 of 1.7, 2.1, 2.4 and 2.5 uM, respectively; triggers mitotic abnormalities and induces apoptosis.

PC-61484

HCI-2389

A potent, specific, irreversible NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 16.65 nM; significantly decreases level of phosphorylated PP1-α in HeLa cellsat 10 nM, significantly increases the effectiveness of bortezomib in inhibiting proteasome activity at concentrations as low as 10 nM; inhibits the degradation of Cyclin B and Cdc2, successfully mitigates drug resistance in bortezomib-resistant multiple myeloma.
PC-61483

Nek2 inhibitor (R)-21

1364269-10-2 A potent and selective NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 22 nM, >200-fold selectivity over Plk1, Mps1, Aurora A and CDK2; also shows >100-fold selectivity over a panel of 24 kinases; down-regulates C-Nap1 phosphoryation with IC50 of 0.8 uM, shows antiproliferative effect on U2OS, MDA-MB-231, HeLa and MCF7 cell with GI50 of 1.82, 4.16, 0.59 and 2.17 uM, respectively; is a valuable tool for investigating the role of Nek2 in the cell cycle and its function in mitotic organization.
PC-61482

TAI-95

1438638-83-5 A potent, orally abioavailable Hec1 inhibitor that disrupts Hec1-Nek2 protein interaction wide anti-cancer spectrum (GI50=14.29-73.65 nM, breast cancer cell lines); demonstrates strong inhibition of in vivo tumor growth of breast cancer models without inducing weight loss or other obvious toxicity; induces apoptotic cell death, shows activity on MDR cell lines and leads to downregulation of the expression of P-glycoprotein (Pgp), also increases the potency of cytotoxic Pgp substrates, including doxorubicin and topotecan.
PC-61481

TAI-1

1334921-03-7 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.
PC-61479

Nek2 inhibitor 72

A potent, ATP-competitive and relative selective Nek2 inhibitor with IC50 of 0.27 uM; displays >10-fold selectivity over CDK2.

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