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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
26 Results for "
spindle assembly checkpoint
" in MedChemExpress (MCE) Product Catalog:
Products (26)
26 Results for "spindle assembly checkpoint" in MCE Product Catalog:
7
7 Publications Verification
proTAME, a cell-permeable proagent form of TAME, is an anaphase promoting complex/cyclosome (APC/C) inhibitor. proTAME causes cell cycle arrest in metaphase .
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2 Cited Publications
BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity .
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1 Cited Publications
Synonyms: ZIO 301; D 24851
Domaines de recherche:
Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis .
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1 Cited Publications
Cat. No.: HY-P71540
Pureté: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: HsMAD2; MAD 2; MAD2 like 1; MAD2 mitotic arrest deficient like 1; MAD2-like protein 1; Mad2l1; MD2L1_HUMAN; Mitotic arrest deficient 2-like protein 1; Mitotic spindle assembly checkpoint protein MAD2A; REV7
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.
Target:
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M2I-1 is a Mad2 inhibitor targeting the binding of Mad2 to Cdc20, an essential protein-protein interaction (PPI) within the spindle assembly checkpoint (SAC) .
Domaines de recherche:
Apcin-A is a small molecule inhibitor that selectively targets the cell division cycle protein Cdc20 and is a derivative of Apcin (HY-110287). Apcin-A competitively binds to the D-box binding pocket of Cdc20 and inhibits substrate ubiquitination mediated by the anaphase promoting complex APC/C-Cdc20. Apcin-A also blocks the binding of Cdc20 to substrates (such as securin and cyclin B1), inhibiting anaphase initiation and cell cycle exit. Apcin-A can promote or prolong mitotic slippage in coordination with p31 comet under conditions of high spindle assembly checkpoint (SAC) activity. Apcin-A can be used to develop anti-mitotic drugs and overcome tumor chemotherapy resistance. Apcin-A can be used to synthesize PROTAC CP5V (HY-130257)[1][2][3].
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AM-5308 is the inhibitor for KIF18A (IC50=47 nM) that inhibits KIF18A-mediated microtubule ATPase activity. AM-5308 activates mitotic checkpoints, regulates cell division processes, including chromosome segregation and spindle assembly. AM-5308 exhibits antitumor activity .
Cat. No.: HY-19916
CAS No.: 1263384-43-5
Synonyms: BAL-101553
Domaines de recherche:
Lisavanbulin (BAL-101553) is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin is a BBB-penetrant and orally active antitumor agent, especially in tumors that express high levels of end-binding protein 1. Lisavanbulin has ability to target tumor cell proliferation and affects the tumor microenvironment by reducing tumor microvasculature. Lisavanbulin is also a spindle assembly checkpoint activator. Lisavanbulin induces cell cycle arrest and subsequent death or aberrant chromosome segregation. Lisavanbulin can be studied in research for diffuse large B cell lymphoma (DLBCL) and glioblastoma .
Cat. No.: HY-132884
CAS No.: 2820453-41-4
TTK inhibitor 3 is a potent and selective TTK (an essential spindle assembly checkpoint enzyme) inhibitor with an IC50 value of 3.0 nM.
Cat. No.: HY-164955
CAS No.: 1817791-70-0
Target:
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TTK/PLK1-IN-1 (Formula I) is the inhibitor for threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1) with IC50 of 7 nM and 72 nM. TTK/PLK1-IN-1 regulates spindle assembly checkpoint (SAC), and exhibits antitumor efficacy against TNBC .
Cat. No.: HY-19916A
CAS No.: 1387574-54-0
Synonyms: BAL-101553 dihydrochloride
Domaines de recherche:
Lisavanbulin (BAL-101553) dihydrochloride is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin dihydrochloride exhibits antitumor activity, especially in tumors that express high levels of end-binding protein 1. Lisavanbulin dihydrochloride has ability to target tumor cell proliferation and affects the tumor microenvironment by reducing tumor microvasculature. Lisavanbulin dihydrochloride is also a spindle assembly checkpoint activator. Lisavanbulin dihydrochloride induces cell cycle arrest and subsequent death or aberrant chromosome segregation. Lisavanbulin dihydrochloride can be studied in research for diffuse large B cell lymphoma (DLBCL) and glioblastoma .
Cat. No.: HY-110347
CAS No.: 1883548-93-3
Mps1-IN-1 dihydrochloride is a potent and ATP-competitive Mps1 kinase inhibitor with an IC50 of 367 nM. Mps1-IN-1 dihydrochloride inhibit Mps1 mitotic kinase activity and abrogates spindle assembly checkpoint (SAC) function. Mps1-IN-1 dihydrochloride decreases the viability of both cancer and ‘normal’ cells .
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.
Cat. No.: HY-124519
CAS No.: 331749-88-3
Synonyms: Cent-1
Target:
Domaines de recherche:
Centmitor-1 (Cent-1) is a mitotic arrest inducer. Centmitor-1 modulates microtubule plus-ends and reduced microtubule dynamics. In cells, Centmitor-1 causes mitotic arrest characterized by chromosome alignment defects, multipolar spindles, centrosome fragmentation, and activated spindle assembly checkpoint .
Cat. No.: HY-13224A
CAS No.: 758722-12-2
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AZD4877 hydrochloride is a synthetic dynein inhibitor with potential anti-tumor activity. AZD4877 selectively inhibits the microtubule dynein KSP (also known as kinesin-5 or Eg5), which may lead to inhibition of mitotic spindle assembly. The action of AZD4877 may activate the spindle assembly checkpoint, leading to cell cycle arrest at the mitotic stage. AZD4877 may induce cell death in actively dividing tumor cells. AZD4877 may be less likely to cause peripheral neuropathy associated with microtubule-targeted compounds as it is not involved in post-mitotic processes. AZD4877 is essential for the formation of bipolar spindles and the proper segregation of sister chromosomes .
Cat. No.: HY-13649R
CAS No.: 204205-90-3
Synonyms: ZIO 301 (Standard); D 24851 (Standard)
Domaines de recherche:
Indibulin (Standard) is the analytical standard of Indibulin. This product is intended for research and analytical applications. Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis .
Cat. No.: HY-184760
CAS No.: 3022872-60-9
Domaines de recherche:
Tubulin polymerization-IN-93 is a β-tubulin polymerization inhibitor. Tubulin polymerization-IN-93 disrupts the microtubule network structure. Tubulin polymerization-IN-93 activates the spindle assembly checkpoint and promotes Mitotic catastrophe. Tubulin polymerization-IN-93 activates the mitochondrial Apoptotic pathway. Tubulin polymerization-IN-93 exhibits anticancer activity against acute myeloid leukemia .
Cat. No.: HY-100341R
CAS No.: 312271-03-7
Domaines de recherche:
M2I-1 (Standard) is the analytical standard of M2I-1 (HY-100341). This product is intended for research and analytical applications. M2I-1 is a Mad2 inhibitor targeting the binding of Mad2 to Cdc20, an essential protein-protein interaction (PPI) within the spindle assembly checkpoint (SAC) .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
