2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. NEKs
  5. NEKs Inhibitor

NEKs Inhibitor

NEKs Isoform Comparison

NEKs Inhibitors (24):

Cat. No. Product Name Effect Purity
  • HY-159520
    Ofirnoflastum
    		Inhibitor 99.93%
    Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC50 of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7-NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1, caspase-8, NF-κB, and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia.
  • HY-120356A
    T-1101 tosylate
    		Inhibitor 98.91%
    T-1101 tosylate (TAI-95 tosylate) is the tosylate salt form of T-1101 (HY-120356). T-1101 tosylate is an orally active inhibitor for mitose regulating highly expressed oncoprotein 1 (Hec1). T-1101 tosylate blocks the interaction between Hec1 and NEK2, exhibits cytotoxicity in human liver cancer cells with GI50 of 15-70 nM. T-1101 tosylate induces apoptosis in Huh-7. T-1101 tosylate exhibits antitumor efficacy in mouse models.
  • HY-108919
    CG-1521
    		Inhibitor
    CG-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.
  • HY-183068
    AP4-43
    		Inhibitor
    AP4-43 is an orally active CLK1, CLK4, PI3K, DDR1, EGFR and NEK4 inhibitor. AP4-43 reduces growth of mammalian colorectal cancer organoids. AP4-43 improves survival in a transgenic Drosophila model of KRAS-mutant colorectal cancer. AP4-43 can be used for the research of KRAS-mutant colorectal cancer.
  • HY-101029
    MBM-55
    		Inhibitor 99.94%
    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.
  • HY-16660
    INH1
    		Inhibitor 99.85%
    INH1 specifically disrupts the Hec1/Nek2 interaction via direct Hec1 binding. INH1 shows promising cancer inhibition activity both in vitro and in vivo.
  • HY-156437
    NBI-961
    		Inhibitor 99.73%
    NBI-961 is a potent NEK2 inhibitor that inhibits proteasomal degradation. NBI-961 induces G2/mitosis arrest and apoptosis in diffuse large B cell lymphoma (DLBCL) cells.
  • HY-163358
    SLC3037
    		Inhibitor 99.85%
    SLC3037 is a NLRP3 inhibitor which blocks NLRP3 from binding to NEK7 or oligomerization, inhibiting inflammasome caused by MSU and other inflammasome activators. SLC3037 can be used for research of gout, cardiovascular diseases, metabolic syndrome or neurodegenerative diseases.
  • HY-100541
    INH6
    		Inhibitor 99.53%
    INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC50 of 2.4 μM.
  • HY-B0790
    TAI-1
    		Inhibitor 98.60%
    TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells.
  • HY-103646
    CK7
    		Inhibitor 99.72%
    CK7, a Cdk2/9 inhibitor, can be used for the synthesis of Nek1 inhibitor BSc5231 and BSc5367.
  • HY-174270
    NLRP3-IN-79
    		Inhibitor 99.10%
    NLRP3-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.
  • HY-176463
    Nek2/Hec1-IN-3
    		Inhibitor 98.05%
    Nek2/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.
  • HY-101030A
    MBM-17S
    		Inhibitor
    MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice.
  • HY-169933
    NEK7-IN-1
    		Inhibitor
    NEK7-IN-1 (Compound I-15) is the inhibitor for NIMA-related kinase 7 NEK7 with IC50 <100 nM. NEK7-IN-1 inhibits the IL-1β release with IC50 <50 nM.
  • HY-101029A
    MBM-55S
    		Inhibitor
    MBM-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.
  • HY-101030
    MBM-17
    		Inhibitor
    MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It 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.
  • HY-168737
    NEK7-IN-2
    		Inhibitor
    NEK7-IN-2 (compound 23) is a potent inhibitor of NLRP3-NEK7 interaction. NEK7-IN-2 can enhance the thermal stability of NEK7 and regulatie NLRP3 inflammasome assembly. NEK7-IN-2 inhibits IL-1β releases.
  • HY-117398
    HCI-2184
    		Inhibitor
    HCI-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.
  • HY-120356
    T-1101
    		Inhibitor
    T-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.