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T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. T-1101 tosylate is inactive toward normal cells, kinases and hERG
TAB29 is a potent inhibitor of peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) with an IC50 of 874 nM, possesses therapeutic potential for human cancers .
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 .
ZL-Pin01 is a high potent covalent Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) inhibitor. ZL-Pin01 shows potent disruption of the Pin1-substrate interaction with an IC50 of 1.33 μM .
ZL-Pin13 is a high potent cell-active covalent inhibitor targeting the Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) with an IC50 of 67 nM. ZL-Pin13 effectively inhibits the proliferation and downregulated the Pin1 substrates in MDA-MB-231 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 .
BSc5367 is a potent Nek1 inhibitor with an IC50 of 11.5 nM. NIMA-related protein kinase Nek1 is crucially involved in cell cycle regulation, DNA repair and microtubule regulation and dysfunctions of Nek1 play key roles in amyotrophic lateral sclerosis (ALS), polycystic kidney disease (PKD) and several types of radiotherapy resistant cancer .
ZINC05007751 is a potent NIMA-related kinase NEK6 inhibitor with an IC50 of 3.4 μM. ZINC05007751 shows antiproliferative activity against a panel of human cancer cell lines, and displays a synergistic effect with Cisplatin and Paclitaxel in a BRCA2 mutated ovarian cancer cell line. ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity was observed against NEK2, NEK7, and NEK9 .
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 .
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 .
PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development .
The NEK2 protein is a key kinase that coordinates important events in cell division and chromatin dynamics. In mitotic cells, it critically controls centrosome separation and bipolar spindle formation by phosphorylating CROCC, CEP250 and NINL. NEK2 Protein, Human is the recombinant human-derived NEK2 protein, expressed by E. coli , with tag free. and T175A, , , , mutation. ,
The NEK2 protein is a key kinase that coordinates important events in cell division and chromatin dynamics. In mitotic cells, it critically controls centrosome separation and bipolar spindle formation by phosphorylating CROCC, CEP250 and NINL. NEK2 Protein, Human (His) is the recombinant human-derived NEK2 protein, expressed by E. coli , with N-6*His labeled tag and T175A, , , , mutation. ,
The NEK9 protein is a pleiotropic mitotic regulator that oversees spindle dynamics and chromosome segregation. It phosphorylates a variety of substrates, including histones, myelin basic protein, β-casein, and BICD2. NEK9 Protein, Human (Sf9, GST) is the recombinant human-derived NEK9 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of NEK9 Protein, Human (Sf9, GST) is 978 a.a., .
NEK7 Protein, a pivotal kinase, crucially drives mitotic cell cycle progression by enhancing centrosome microtubule nucleation, ensuring robust spindle formation, and aiding cytokinesis. Its phosphorylation of EML4 at 'Ser-146' facilitates chromosome congression. NEK7 extends its impact by phosphorylating RPS6KB1 and activating NLRP3 inflammasome assembly, promoting CASP1 activation. Independently, NEK7 unlocks NLRP3 within the microtubule organizing center, ensuring mutual exclusivity between inflammasome response and cell division by interacting with NEK9. These multifaceted functions position NEK7 as a key orchestrator in mitotic progression and the inflammasome response, highlighting its regulatory significance. NEK7 Protein, Human (His-SUMO) is the recombinant human-derived NEK7 protein, expressed by E. coli. The total length of NEK7 Protein, Human (His-SUMO) is 302 a.a., with molecular weight of 50 kDa.
The NEK7 protein is a key kinase that crucially drives mitotic cell cycle progression by enhancing centrosomal microtubule nucleation, ensuring robust spindle formation, and aiding in cytokinesis. Phosphorylation of EML4 at “Ser-146” promotes chromosome aggregation. NEK7 Protein, Human (sf9, His-GST) is the recombinant human-derived NEK7 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of NEK7 Protein, Human (sf9, His-GST) is 302 a.a., with molecular weight of ~58 kDa.
NEK3 Protein influences neuronal morphogenesis and polarity through effects on microtubules. NEK3 Protein regulates microtubule acetylation in neurons. NEK3 Protein contributes to prolactin-mediated phosphorylation of PXN and VAV2. NEK3 Protein, Mouse (sf9, His-GST) is the recombinant mouse-derived NEK3 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of NEK3 Protein, Mouse (sf9, His-GST) is 509 a.a., with molecular weight of ~72 KDa.
The NEK6 protein is a key kinase essential for driving mitotic cell cycle progression, ensuring chromosome segregation, robust spindle formation, and cytokinesis. It phosphorylates ATF4, CIR1, PTN, RAD26L, RBBP6, RPS7, RPS6KB1, TRIP4, STAT3 and histone H1/H3, affecting a variety of cellular processes. NEK6 Protein, Human (Sf9, GST) is the recombinant human-derived NEK6 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of NEK6 Protein, Human (Sf9, GST) is 312 a.a., .
The PIN1 protein is a peptidyl-prolyl cis/trans isomerase that complexly regulates multiple cellular processes by binding and isomerizing phosphorylated Ser/Thr-Pro motifs. This molecular switch induces conformational changes in phosphorylated proteins that affect mitosis, kinase activity, oncogene transactivation, centrosome amplification, and cell transformation. PIN1 Protein, Human is the recombinant human-derived PIN1 protein, expressed by E. coli , with tag free. The total length of PIN1 Protein, Human is 163 a.a., with molecular weight of ~18 kDa.
The PIN1 protein is a peptidyl-prolyl cis/trans isomerase that complexly regulates multiple cellular processes by binding and isomerizing phosphorylated Ser/Thr-Pro motifs. This molecular switch induces conformational changes in phosphorylated proteins that affect mitosis, kinase activity, oncogene transactivation, centrosome amplification, and cell transformation. PIN1 Protein, Human (His) is the recombinant human-derived PIN1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of PIN1 Protein, Human (His) is 163 a.a., with molecular weight of ~19 kDa.
PIN4 isoform 1 functions as a ribosomal RNA processing factor in ribosome biogenesis and interacts with tightly bent AT-rich stretches of double-stranded DNA. Meanwhile, PIN4 isoform 2 specifically binds to double-stranded DNA. PIN4 Protein, Human (His) is the recombinant human-derived PIN4 protein, expressed by E. coli , with N-6*His labeled tag. The total length of PIN4 Protein, Human (His) is 156 a.a., with molecular weight of ~18.0 kDa.
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
JH295 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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