Nek

MBM-17 (compound 42c) is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM.

MBM-55 (compound 42g) is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM.

INH1 is a Hec1 inhibitor. It binds Hec1, inhibiting its association with Nek2 and kinetochores.

INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.

CMP3a is a NEK2 kinase inhibitor. CMP3a efficiently attenuated GBM growth in a mouse model and exhibited a synergistic effect with radiotherapy. Targeting NEK2 attenuates glioblastoma growth and radioresistance by destabilizing histone methyltransferase EZH2.

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.

BSc5367 is a potent inhibitor of NIMA-related protein kinase 1 (Nek1), exhibiting an IC50 of 11.5 nM. Nek1 is integral to cell cycle regulation, DNA repair, and microtubule dynamics, with its dysfunction implicated in various conditions such as amyotrophic lateral sclerosis (ALS), polycystic kidney disease (PKD), and radiotherapy-resistant cancers. This reagent is valuable for research into the molecular mechanisms underlying these diseases and for exploring potential therapeutic interventions.

Ofirnoflastum is a selective inhibitor of the serine/threonine-protein kinase Nek7. This compound demonstrates significant anti-inflammatory properties, making it a valuable tool for research into inflammation-related pathways and diseases. Its mechanism of action and specificity towards Nek7 facilitate investigations in various cellular processes, particularly those associated with cellular stress responses and mitotic regulation.

ZINC05007751 is a selective inhibitor of the NIMA-related kinase NEK6, exhibiting an IC50 of 3.4 μM. This compound demonstrates notable antiproliferative effects across various human cancer cell lines and synergizes with Cisplatin and Paclitaxel in BRCA2-mutated ovarian cancer models. ZINC05007751 displays high specificity for NEK6 and NEK1, with minimal activity against NEK2, NEK7, and NEK9, making it a valuable tool for studying NEK6-related pathways in cancer research.

Nek2/Hec1-IN-3 is a potent inhibitor of the Hec1/Nek2 interaction, specifically designed to disrupt the binding between these two proteins. This compound exhibits significant biological activity by interfering with the Nek2-mediated regulation of cell division, making it a valuable tool for research in neoplastic diseases and cancer biology. Its application in studying tumorigenesis and cell cycle dysregulation facilitates a deeper understanding of oncogenic pathways.

JH295 hydrate is a selective and irreversible inhibitor of NIMA-related kinase 2 (Nek2), exhibiting an IC50 value of 770 nM. This compound targets cellular Nek2 by inducing alkylation at Cys22, while showing no activity against critical mitotic kinases such as Cdk1, Aurora B, or Plk1, thereby maintaining bipolar spindle assembly and the spindle assembly checkpoint. Additionally, JH295 hydrate functions as a click chemistry reagent, possessing an alkyne group that allows for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it valuable in various research applications.

Nek2/Hec1-IN-2 is a potent inhibitor of the Nek2 and Hec1 kinases. It effectively disrupts cell division processes, demonstrating inhibitory activity against cancer cell proliferation with an IC50 greater than 25 μM. This compound is valuable for research into mitotic regulation and therapeutic strategies targeting cancer cell growth.

HCI-2184 is a potent Nek2 inhibitor with an IC50 value of 39.90 nM. This compound enhances the efficacy of Bortezomib by significantly inhibiting proteasome activity. HCI-2184 is valuable for research applications focused on cell cycle regulation and cancer therapeutics.

Nek2-IN-6 is a selective inhibitor of never in mitosis (NIMA) related kinase 2 (Nek2), a critical regulator of mitotic processes. This compound demonstrates significant biological activity in inhibiting this kinase, making it valuable for exploring its role in cell division and related pathologies. Nek2-IN-6 is well-suited for research applications focused on cancer biology, particularly in studies examining the mitotic spindle assembly and its implications in tumorigenesis.

NEK7-IN-1 is a potent inhibitor of NIMA-related kinase 7 (NEK7), exhibiting an IC50 of less than 100 nM. It effectively suppresses the release of IL-1β, with an IC50 of less than 50 nM. This compound is valuable for research into inflammatory responses and the molecular pathways involving NEK7. Its application extends to studies focused on cellular processes influenced by NEK7 modulation.

Nek2-IN-5 is a potent and irreversible inhibitor of Nek2 (Never in mitosis gene a-related kinase 2). This compound features a clickable alkyne group, enabling it to undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-bearing molecules. Nek2-IN-5 is valuable in research applications focused on cell cycle regulation and cancer biology, providing insights into the role of Nek2 in cellular processes.