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Chlorpropham is a carbamate herbicide and plant growth regulator. Chlorpropham inhibits mitosis and cell division by interfering with the organisation of the spindle microtubules .
1-Oleoyl lysophosphatidic acid (1-Oleoyl-sn-glycero-3-phosphate) sodium, a potent bioactive phospholipid, is a LPA receptor activator. 1-Oleoyl lysophosphatidic acid sodium can promote mitosis by inducing DNA synthesis. 1-Oleoyl lysophosphatidic acid sodium is also involved in normal and pathological emotional responses, including anxiety and depression .
P62-mediated mitophagy inducer (PMI) is a P62-mediated mitophagy activator. P62-mediated mitophagy inducer activates mitochondrial autophagy without recruitment of Parkin or collapse of the mitochondrial membrane potential and remains active in cells lacking a fully functional PINK1/Parkin pathway. P62-mediated mitophagy inducer serves as a pharmacological tool to study the molecular mechanisms of mitosis, avoiding toxicity and some of the non-specific effects associated with the sudden dissipation of mitochondria lacking membrane potential .
Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis .
Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts .
Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1 .
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 .
S-72 inhibits tubulin polymerization and further triggers mitosis-phase cell cycle arrest and cell apoptosis, in addition to suppressing STAT3 signaling .
HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1 (plk1), without significant effect on tubulin polymerization.
N-Boc-dolaproine (Dap) is the amino acid residue of the pentapeptide Dolastatin 10 (HY-15580). Dolastatin 10 inhibits tubulin polymerization and mitosis and has anticancer activity .
N-Boc-dolaproine-methyl is the amino acid residue of the pentapeptide Dolastatin 10 (HY-15580). Dolastatin 10 inhibits tubulin polymerization and mitosis and has anticancer activity .
N-Boc-dolaproine-OH ((+)-phenylethylamine) is the amino acid residue of the pentapeptide Dolastatin 10 (HY-15580). Dolastatin 10 inhibits tubulin polymerization and mitosis and has anticancer activity .
N-Boc-dolaproine-OH dicyclohexylamine is the amino acid residue of the pentapeptide Dolastatin 10 (HY-15580). Dolastatin 10 inhibits tubulin polymerization and mitosis and has anticancer activity .
MPI-0441138 is an inducer of apoptosis and an inhibitor of mitosis. MPI-0441138 can induce DNA breaks and induce cytochrome c translocation, leading to tumor cell death .
Synstab A is a mitosis modulator to promote interactions between α- and β-tubulin. Synstab A can polymerizes microtubules from purified tubulin, and produces microtubule bundles in interphase cells .
N-Boc-dolaproine dicyclohexylamine is an amino acid residue of the pentapeptide Dolastatin 10 (HY-15580). Dolastatin 10 inhibits tubulin polymerization and mitosis and has anticancer activity. And contains dicyclohexylamine .
N-Boc-dolaproine-amide-Me-Phe is the amino acid residue of the pentapeptide Dolastatin 10 (HY-15580). Dolastatin 10 inhibits tubulin polymerization and mitosis and has anticancer activity .
AG126 is a tyrosine kinase inhibitor, can inhibit the phosphorylation of ERK1 and ERK2 at 25-50 μM. AG126 can be used in meiosis, mitosis, and postmitotic research .
Chlorpropham-d7 is the deuterium labeled Chlorpropham[1]. Chlorpropham is a carbamate herbicide and plant growth regulator. Chlorpropham inhibits mitosis and cell division by interfering with the organisation of the spindle microtubules[2][3].
(S)-Monastrol ((+)-Monastrol) is an allosteric inhibitor of the mitotic kinesin Eg5 that exhibits an antiproliferative effect against several cancer cell lines. (S)-Monastrol arrests mammalian cells in mitosis with monopolar spindles .
(2S,3R)-Dap-NE hydrochloride is the amino acid residue of the pentapeptide Dolastatin 10 (HY-15580). Dolastatin 10 inhibits tubulin polymerization and mitosis and has anticancer activity .
(2R,3R)-Dap-NE hydrochloride is the amino acid residue of the pentapeptide Dolastatin 10 (HY-15580). Dolastatin 10 inhibits tubulin polymerization and mitosis and has anticancer activity .
14,15-EET-SI is a sulfonimide (SI) analog metabolized from 14,15-EET, which is also an effective mitogen. 14,15-EET-SI can stimulate the incorporation of [3H] thymidine, activate pp60c-src and initiate the tyrosine kinase cascade, mediating their mitotic effects. Additionally, 14,15-EET-SI can increase cell proliferation as well as the expression of c-fos and egr-1 mRNA .
FT709 is a potent and selective USP9X inhibitor, an IC50 of 82 nM. USP9X has been linked with centrosome function, chromosome alignment during mitosis, EGF receptor degradation, chemo-sensitization, and circadian rhythms .
UMK57 is a small molecule compound that specifically promotes k-MT attachment error correction to inhibit chromosome missegregation, which can improve chromosome segregation fidelity by destabilizing kinetochore microtubule (k-MT) attachment during mitosis .
SSE15206 is a microtubule polymerization inhibitor (GI50 = 197 nM in HCT116 cells) that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells .
Cemadotin (LU103793) is an analogue of Dolastatin 15 (HY-P1126) which is naturally occurring cytotoxic peptides. Cemadotin blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin can be used to research anticancer .
Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
P34cdc2 Kinase Fragment is associated with the completion of DNA replication in yeast mitosis. P34cdc2 Kinase can phosphorylate mitogen-activated protein 2 (MAP2) to regulate microtubules polymerization in Xenopus oocytes meiosis .
PM050489 is an effective polyketone inhibitor of Microtubule/Tubulin that can be isolated from Madagascan sponge Lithoplocamia lithistoides. PM050489 inhibits mitosis with an IC50 value of 26.4 nM. PM050489 has antitumor activity and can be used in cancer research .
TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death .
Dihydrobaicalein is a PLK1 Inhibitor with an IC50 of 6.3 μM. Dihydrobaicalein also inhibits VRK2 and PLK2. Dihydrobaicalein is a natural product that can be isolated from Scutellaria scandens .
Tubulin polymerization-IN-57 (compound 5a) is a tubulin inhibitor and is an α-naphthoxy-substituted carbendazim (HY-13582) derivative. Tubulin polymerization-IN-57 induces mitotic arrest and inhibits cancer cell proliferation .
EAPB 02303 is a microtubule-disrupting agent and inhibitor. EAPB 02303 induces mitosis arrest and impairment of spindle assembly. Thus, EAPB 02303 induces apoptosis and exhibits antitumor activity. EAPB 02303 also exhibits a potent synergy with Paclitaxel (HY-B0015) at lower concentrations .
SIC5-6 is a potent Separase inhibitor. Separase, a large cysteine protease, involves in chromosome segregation during mitosis and meiosis, DNA damage repair, centrosome disengagement and duplication, spindle stabilization and elongation. Separase is highly overexpressed in many solid cancers, serves as an attractive chemotherapeutic target .
Estramustine phosphate sodium, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine phosphate sodium depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine phosphate sodium can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate cancer .
Estramustine phosphate, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine phosphate depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine phosphate can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate cancer .
Trenimon is a compound with anti-cancer effects. Trenimon shows mutagenic actions in many species by inducing point and chromosomal mutations, sister-chromatid exchanges, recombination phenomena and phage induction. Trenimon can be used for the research of cancer .
EDTA-AM (ethylenediaminetetraacetic acid, acetoxymethyl ester) is the membrane-permeant form of the metal chelator EDTA (HY-Y0682). Live cells passively load EDTA-AM by incubating with EDTA-AM. Once internalized, cytoplasmic esterase decomposes AM esters, releasing the active ligand EDTA, which isolates metal ions within the cell. EDTA-AM induces an arrest of mitotic progression and chromosome decondensation .
SSE1806 is a derivative of podophyllotoxin (a natural antimitotic agent) and a microtubule/tubulin inhibitor with significant anticancer and antiproliferative activities. The GI50 of SSE1806 on cancer cell growth ranges from 1.29-21.15 μM. SSE1806 causes mitotic abnormalities and G2/M phase arrest, increases p53 expression, and inhibits colon cancer organoid growth. SSE1806 is able to overcome multidrug resistance in cell lines overexpressing MDR-1 .
ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 µM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity .
R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kd values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence .
Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells .
MKC-1 (Ro-31-7453) is an orally active and potent cell cycle inhibitor with broad antitumor activity. MKC-1 inhibits the Akt/mTOR pathway. MKC-1 arrests cellular mitosis and induces cell apoptosis by binding to a number of different cellular proteins including tubulin and members of the importin β family .
Tubulysin A (TubA) is an anticancer and antiangiogenic agent with anti-microtubule, anti-mitosis and anti-proliferative activity against a variety of cancer cells with IC50 values in the pmol range. It can induce apoptosis of cancer cells and has no effect on normal cells. Tubulysins are a group of potent cytotoxins consisting of nine members (A-I). Tubulysin A can synthesize ADC as ADC Cytotoxin< b>ADC Cytotoxin .
AZD4877 is another isostere to Ispinesib (HY-50759)and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity .
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
Tubulin polymerization-IN-46 (compound 9q) is a microtubule/Tubulin inhibitor that inhibits tubulin polymerization and induces apoptosis. Tubulin polymerization-IN-46 inhibits mitosis and arrests MCF-7 cells in the G2/M phase. Tubulin polymerization-IN-46 has anti-proliferative activity against MCF-7 breast cancer cells with an IC50 of 10 nM .
AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor (IC50: 6.50 μM) that inhibits the catalytic activity and non-catalytic functions of Aurora A. Aurora A regulates the assembly of the bipolar mitotic spindle and the fidelity of chromosome segregation during mitosis and has non-catalytic functions. AurkA allosteric-IN-1 blocks the interaction of AurkA with the activator TPX2 by binding to the Y pocket of AurkA .
Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors .
Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects .
MELK-8a (NVS-MELK8a) is a highly potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor with IC50 of 2 nM. MELK-8a also inhibits Flt3 (ITD), Haspin, PDGFRα with IC50s of 0.18, 0.19, and 0.42 μM, respectively. MELK plays an essential role in regulating cell mitosis in a subset of cancer cells .
Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC) .
FiVe1 is a potent vimentin (VIM; the intermediate filament and mesenchymal marker) inhibitor . FiVe1 promotes VIM disorganization and phosphorylation during metaphase, leading to mitotic catastrophe, multinucleation, and the loss of stemness.?FiVe1 selectively and irreversibly inhibits the growth of multiple FOXC2-expressing breast cancer cell lines (HMLER cells (IC50:?267 nM); FOXC2-HMLER cells (IC50:?447 nM). FiVe1 inhibits the migration of mesenchymally transformed cells .
(±)14,15-Epoxyeicosatrienoic acid ((±)14(15)-EET) is the Cytochrome P450 metabolite of arachidonic acid. While CYP3A4 may be involved in breast cancer cell growth, (±)14,15-Epoxyeicosatrienoic acid may promote mitosis and anchorage-dependent cloning through STAT3 affected by CYP3A4. (±)14,15-Epoxyeicosatrienoic acid exhibits STAT3-dependent cell growth promotion and may also participate in the autocrine/paracrine pathway that drives cell growth .
FTI-2153 is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity .
FTI-2153 TFA is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 TFA is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity .
DNA is prone to numerous forms of damage that can injure cells and impair fitness. Cells have developed an array of mechanisms to repair these injuries. Proliferating cells are especially vulnerable to DNA damage due to the added demands of cellular growth and division. Cell cycle checkpoints represent integral components of DNA repair that coordinate cooperation between the machinery of the cell cycle and several biochemical pathways that respond to damage and restore DNA structure. By delaying progression through the cell cycle, checkpoints provide more time for repair before the critical phases of DNA replication, when the genome is replicated, and of mitosis, when the genome is segregated. Loss or attenuation of checkpoint function may increase spontaneous and induced gene mutations and chromosomal aberrations by reducing the efficiency of DNA repair.
MCE owns a unique collection of 2001 cell cycle/DNA damage-related compounds which can be used in the research of the same.
EDTA-AM (ethylenediaminetetraacetic acid, acetoxymethyl ester) is the membrane-permeant form of the metal chelator EDTA (HY-Y0682). Live cells passively load EDTA-AM by incubating with EDTA-AM. Once internalized, cytoplasmic esterase decomposes AM esters, releasing the active ligand EDTA, which isolates metal ions within the cell. EDTA-AM induces an arrest of mitotic progression and chromosome decondensation .
Head activator neuropeptide is a mitogen for mammalian cell lines of neuronal or neuroendocrine origin. Head activator neuropeptide signals by binding GPR37 and stimulates cells to enter mitosis .
Cemadotin (LU103793) is an analogue of Dolastatin 15 (HY-P1126) which is naturally occurring cytotoxic peptides. Cemadotin blocks cells at mitosis, and exhibits Ki value of 1 μM for inhibiting tubulin. Cemadotin can be used to research anticancer .
P34cdc2 Kinase Fragment is associated with the completion of DNA replication in yeast mitosis. P34cdc2 Kinase can phosphorylate mitogen-activated protein 2 (MAP2) to regulate microtubules polymerization in Xenopus oocytes meiosis .
Dihydrobaicalein is a PLK1 Inhibitor with an IC50 of 6.3 μM. Dihydrobaicalein also inhibits VRK2 and PLK2. Dihydrobaicalein is a natural product that can be isolated from Scutellaria scandens .
PM050489 is an effective polyketone inhibitor of Microtubule/Tubulin that can be isolated from Madagascan sponge Lithoplocamia lithistoides. PM050489 inhibits mitosis with an IC50 value of 26.4 nM. PM050489 has antitumor activity and can be used in cancer research .
(±)14,15-Epoxyeicosatrienoic acid ((±)14(15)-EET) is the Cytochrome P450 metabolite of arachidonic acid. While CYP3A4 may be involved in breast cancer cell growth, (±)14,15-Epoxyeicosatrienoic acid may promote mitosis and anchorage-dependent cloning through STAT3 affected by CYP3A4. (±)14,15-Epoxyeicosatrienoic acid exhibits STAT3-dependent cell growth promotion and may also participate in the autocrine/paracrine pathway that drives cell growth .
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 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., .
Chlorpropham-d7 is the deuterium labeled Chlorpropham[1]. Chlorpropham is a carbamate herbicide and plant growth regulator. Chlorpropham inhibits mitosis and cell division by interfering with the organisation of the spindle microtubules[2][3].
Nek2-IN-5 (compound 6) is a potent and irreversible Nek2 ((Never in mitosis gene a)-related kinase 2) inhibitior . Nek2-IN-5 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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