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
All Product Categories
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NEKs Related Products (48)
Related Products (48)
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NEKs Isoform Comparison
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CK7
0 ImagesCK7, a Cdk2/9 inhibitor, can be used for the synthesis of Nek1 inhibitor BSc5231 and BSc5367.
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ABS-752 hydrochloride
0 ImagesABS-752 hydrochloride is an orally active prodrug targeting CRBN-modulating molecular glue with selectivity in protein degradation. ABS-752 hydrochloride 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 hydrochloride requires metabolic activation to ABT-002 to form the active complex; VAP-1 mediates its conversion to an aldehyde intermediate. ABS-752 hydrochloride induces cell death, reduces cell viability, and exhibits antitumor activity, leading to regression and inhibition of tumor growth. ABS-752 hydrochloride shows no cytotoxicity in primary human hepatocytes. ABS-752 hydrochloride can be used in the research of hepatocellular carcinoma.
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NLRP3-IN-79
0 ImagesNLRP3-IN-79 is an orally active NLRP3 inhibitor. NLRP3-IN-79 inhibits NLRP3 inflammasome with an IC50 of 10.69 nM. NLRP3-IN-79 blocks NLRP3 inflammasome assembly by directly binding to NLRP3 and disrupting the NEK7-NLRP3 interaction. NLRP3-IN-79 can be used for the study of NLRP3-driven diseases model, including systemic inflammation, peritonitis, and colitis.
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Nek2/Hec1-IN-3
0 ImagesNek2/Hec1-IN-3 (Compound 11-28) is a Hec1/Nek2 interaction inhibitor. Nek2/Hec1-IN-3 disrupts Nek2/Hec1 binding and can be used for research of neoplastic diseases.
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MBM-17S
0 ImagesCat. No.: HY-101030ACAS No.: 2083621-91-2
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JH295 hydrate
0 ImagesJH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint. JH295 (hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Nek2-IN-4
0 ImagesCat. No.: HY-137046CAS No.: 2225902-88-3Nek2-IN-4 is a potent NEK2 inhibitor with an IC50 value of 15 nM. Nek2-IN-4 inhibits cell proliferation. Nek2-IN-4 has the potential for the research of pancreatic cancer.
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MBM-55S
0 ImagesCat. No.: HY-101029ACAS No.: 2083624-07-9MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S 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-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice.
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MBM-17
0 ImagesCat. No.: HY-101030CAS No.: 2083621-90-1
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NEK7 degrader-3
0 ImagesCat. No.: HY-185311CAS No.: 3119435-52-5NEK7 degrader-3 is an orally active and brain-penetrant NEK7 molecular glue degrader with a DC50 of 33.1 nM. NEK7 degrader-3 mediates interaction between NEK7 and E3 ligase cereblon, promoting proteasomal degradation of NEK7 and attenuating NLRP3 inflammasome-mediated inflammatory responses. NEK7 degrader-3 inhibits caspase-1 activity, cytokine release of IL-1β, IL-1α, and IL-18, and pyroptosis-related plasma membrane permeabilization. NEK7 degrader-3 shows antiinflammatory activity in an LPS (HY-D1056)-induced neuroinflammation mouse model. NEK7 degrader-3 can be used for the research of neuroinflammation.
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HCI-2184
0 ImagesCat. No.: HY-117398CAS No.: 1341200-61-0HCI-2184 is a Nek2 inhibitor with an IC50 of 39.90 nM. HCI-2184 significantly increases the effectiveness of Bortezomib (HY-10227) in inhibiting proteasome activity.
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T-1101
0 ImagesCat. No.: HY-120356CAS No.: 1438638-83-5Synonyms: TAI-95T-1101 (TAI-95) is an orally active inhibitor for mitose regulating highly expressed oncoprotein 1 (Hec1). T-1101 blocks the interaction between Hec1 and NEK2, exhibits cytotoxicity in human liver cancer cells with GI50 of 15-70 nM. T-1101 induces apoptosis in Huh-7. T-1101 exhibits antitumor efficacy in mouse models.
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CG-1521
0 ImagesCat. No.: HY-108919CAS No.: 674767-29-4CG-1521 is a histone deacetylase (HDAC) inhibitor that stabilizes Ac-Lys373 P53, increases P21 levels and HDAC2 degradation. CG-1521 can inhibit proliferation, induce cell cycle arrest and apoptosis. CG-1521 promotes Bax translocation to the mitochondria and cleavage. CG-1521 downregulates KIF4, Aurora B and Nek2 protein expression and DNA synthesis. CG-1521 can be used for the research of prostate cancer and inflammatory breast cancer.
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ABT-002
0 ImagesCat. No.: HY-175283CAS No.: 2438239-83-7ABT-002 is a molecular glue degrader targeting GSPT1 and NEK7. ABT-002 is the active metabolite of ABS-752 (HY-W599279). ABT-002 is promising for research of hepatocellular carcinoma (HCC).
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NEK7 degrader-4
0 ImagesCat. No.: HY-177433CAS No.: 3069891-88-6NEK7 degrader-4 is a NEK7 molecular glue degrader with a DC50 of 9 nM. NEK7 degrader-4 can be used for autoinflammatory and autoimmune disorders like multiple sclerosis, neurodegeneraive diseases like Alzheimer's disease and cardiovascular and melabolic disorders like pericarditis and Type 2 diabetes research.
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Nek2-IN-6
0 ImagesCat. No.: HY-150046CAS No.: 2410376-96-2
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GSK461364 analogue 1
0 ImagesCat. No.: HY-111090CAS No.: 929095-23-8GSK461364 analogue 1 is a thiophene-based PLK1 inhibitor with a PLK1 IC50 of 2 nM and a PLK3 IC50 of 630 nM. GSK461364 analogue 1 also acts as an inhibitor of Nek2 kinase (IC50: 21 nM). GSK461364 analogue 1 has a solubility of ≥190 μM in pH 7.4 PBS and a human plasma protein binding rate of 91.5%. GSK461364 analogue 1 can be used in studies related to colon cancer, lung cancer, breast cancer and ovarian cancer.
