NEK2 Inhibitor

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.

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.

INH1 specifically disrupts the Hec1/Nek2 interaction via direct Hec1 binding. INH1 shows promising cancer inhibition activity both in vitro and in vivo.

NBI-961 is a NEK2 catalytic inhibitor with human NEK2 IC₅₀ ~12-fold lower than FLT3. NBI-961 induces proteasomal degradation of NEK2. NBI-961 induces G2/mitosis arrest, apoptosis, and compromises viability in DLBCL cells and patient-derived cells. NBI-961 sensitizes DLBCL cells to doxorubicin and vincristine, and suppresses DLBCL tumor growth in mice. NBI-961 can be used for the research of diffuse large b cell lymphoma.

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.

GSK461364 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.

INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC₅₀ of 2.4 μM.

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.

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.

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.

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.

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.