- Cat. No.
- A12499
MBM-17
MBM-17 (compound 42c) is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM.
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Nek inhibitors target NIMA-related kinases, chiefly Nek2, a centrosomal kinase active in mitosis. NIMA-related kinases (Nek) are named after the never in mitosis A (NIMA) kinase of the fungus Aspergillus nidulans. Nek2 regulates centrosome separation, and in 1998 centrosomal Nek2-associated protein 1 (C-Nap1) was identified as a candidate substrate. Nek2 also binds the kinetochore protein Hec1 (highly expressed in cancer 1). In 2008, INH1 was reported to bind Hec1 directly, disrupt the Hec1/Nek2 interaction and suppress tumor cell growth. INH154 is a later compound from the same Hec1-targeting series. JH295, MBM-55 and NBI-961 are listed as Nek2 kinase inhibitors.
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.
Synonyms: Hec1/Nek2 Mitotic Pathway Inhibitor I
INH1 is a Hec1 inhibitor. It binds Hec1, inhibiting its association with Nek2 and kinetochores.
JH295 is a selective and irreversible inhibitor of NIMA-related kinase 2 (Nek2), demonstrating an IC50 of 770 nM. It functions by alkylating Cys22, effectively inhibiting Nek2 activity without affecting other mitotic kinases such as Cdk1, Aurora B, or Plk1. JH295 does not interfere with bipolar spindle assembly or the spindle assembly checkpoint. Additionally, it features an alkyne group, enabling its use as a click chemistry reagent for copper-catalyzed azide-alkyne cycloaddition (CuAAc) applications.
Synonyms: INH 6,INH-6
INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.
Synonyms: Nek2-IN-4
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.
NBI-961 is a potent inhibitor of NEK2, a serine/threonine kinase involved in cell cycle regulation. By inhibiting proteasomal degradation, NBI-961 effectively induces G2/mitosis arrest and apoptosis in diffuse large B cell lymphoma (DLBCL) cells. This compound serves as a valuable tool for research into the therapeutic targeting of NEK2 in cancer biology.
(Rac)-CCT 250863 is a selective and reversible inhibitor of NEK 2, with an IC50 of 0.073 µM. This compound effectively induces cell cycle arrest and demonstrates antiproliferative activity in both Pomalidomide-sensitive and resistant cell lines. Additionally, (Rac)-CCT 250863 promotes apoptosis when used in combination with Pomalidomide, making it a valuable tool for research in cancer therapeutics and cell cycle regulation.
MBM-17S is a highly potent inhibitor of NIMA-related kinase 2 (Nek2) with an IC50 of 3 nM. This compound demonstrates significant antiproliferative effects on cancer cells by promoting cell cycle arrest and inducing apoptosis. MBM-17S exhibits notable antitumor activities while maintaining a favorable safety profile in murine models. Its ability to target Nek2 makes it a valuable reagent for cancer research and therapeutic studies.
MBM-55S is a highly selective inhibitor of NIMA-related kinase 2 (Nek2) with an IC50 of 1 nM, demonstrating potency against this target. It exhibits significant selectivity for most kinases, with minor activity against RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). The compound effectively inhibits cancer cell proliferation by inducing cell cycle arrest and apoptosis, displaying notable antitumor activity without apparent toxicity in murine models. This makes MBM-55S a valuable tool for cancer research and therapeutic development.
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.
Synonyms: Ofirnoflast
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.
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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.