NEKs
NIMA–related Kinases; NIMA (never in mitosis gene a)-related Expressed Kinases
NIMA-related Kinases (NEKs) are a class of serine/threonine protein kinases ubiquitous in eukaryotic organisms. NEKs play pivotal roles in cell cycle regulation, including chromosome condensation, mitotic entry, centrosome duplication, and mitotic exit.
The NEK family comprises 11 members in humans (NEK1-NEK11). NEK family members are widely involved in key biological processes such as cell cycle regulation, ciliogenesis, and DNA damage repair, making them potential therapeutic targets for diseases.
Abnormal activation or mutations of NEKs are closely associated with cancers, genetic diseases, neurodegenerative diseases, and other conditions[1][2][3][4].
References:
- [1]. Gaji RY, et al. Protein kinases in Toxoplasma gondii. Int J Parasitol. 2021 May;51(6):415-429. [Content Brief]
- [2]. Guo L, et al. Nek11 regulates asymmetric cell division during mouse oocyte meiotic maturation. Biochem Biophys Res Commun. 2016 Jun 10;474(4):667-672. [Content Brief]
- [3]. Pilakowski J, et al. Design, synthesis and biological evaluation of novel aminopyrazole- and 7-azaindole-based Nek1 inhibitors and their effects on zebrafish kidney development. Bioorg Med Chem Lett. 2021 Dec 1;53:128418. [Content Brief]
- [4]. Kenna KP, et al. NEK1 variants confer susceptibility to amyotrophic lateral sclerosis. Nat Genet. 2016 Sep;48(9):1037-42. [Content Brief]
NEKs Isoform Specific Products
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NEKs Related Products (48)
Related Products (48)
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NEKs Isoform Comparison
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NEK7 degrader-2
0 ImagesCat. No.: HY-177559CAS No.: 3037413-54-7NEK7 degrader-2 is a NEK7 molecular glue degrader that promotes the formation of the NEK7-compound-CRBN/DDB1 ternary complex. NEK7 degrader-2 reduces the release of IL-1β after NLRP3 inflammasome activation induced by LPS (HY-D1056). NEK7 degrader-2 can be applied in studies related to NEK7-dependent NLRP3 inflammasome activation and inflammatory responses.
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ABS-752
0 ImagesCat. No.: HY-W599279CAS No.: 2761170-84-5ABS-752 is an orally active prodrug targeting CRBN-modulating molecular glue with selectivity in protein degradation. ABS-752 preferentially degrades GSPT1 and induces cytotoxicity through this degradation, while it also degrades NEK7, SALL4 and CK1α, with weaker degradation potency against CK1α. As a prodrug, ABS-752 requires metabolic activation to ABT-002 to form the active complex; VAP-1 mediates its conversion to an aldehyde intermediate. ABS-752 induces cell death, reduces cell viability, and exhibits antitumor activity, leading to regression and inhibition of tumor growth. ABS-752 shows no cytotoxicity in primary human hepatocytes. ABS-752 can be used in the research of hepatocellular carcinoma.
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PLK1-IN-17
0 ImagesCat. No.: HY-184863CAS No.: 1034617-66-7PLK1-IN-17 is a potent PLK1 inhibitor with an IC50 of 2 nM. PLK1-IN-17 shows high selectivity for PLK2 and CDK2/A, moderate selectivity for PLK3, only weak activity against CK2, FLT3 and NEK6, and no activity against PDGFR, ALK and another 37 kinases. PLK1-IN-17 inhibits the proliferation of ovarian cancer cells and can be used in ovarian cancer-related research.
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MBM-55 (Standard)
0 ImagesMBM-55 (Standard) is the analytical standard of MBM-55 (HY-101029). This product is intended for research and analytical applications. MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
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CK7 (Standard)
0 ImagesCat. No.: HY-103646RCAS No.: 507487-89-0CK7 (Standard) is the analytical standard of CK7 (HY-103646). This product is intended for research and analytical applications. CK7, a Cdk2/9 inhibitor, can be used for the synthesis of Nek1 inhibitor BSc5231 and BSc5367.
