MKI-3
MKI-3 is a selective microtubule-associated serine/threonine kinase-like (MASTL) inhibitor with an IC50 of 5.72 nM and a Kd of 1.89 nM. MKI-3 disrupts the MASTL-ENSA-Aurora A signaling axis. MKI-3 induces chromosomal instability, mitotic catastrophe and apoptosis (apoptosis) in cancer cells. MKI-3 is applicable to research related to triple-negative breast cancer.
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- CAS No.: 3084702-28-0
- 화학식: C21H19N7O
- 분자량:385.42
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
MKI-3 inhibits cellular MASTL activity with an IC50 of 114.9 nM[1].
MKI-3 (72 h) inhibits proliferation of breast cancer cell lines 4T1, MCF7, MDA-MB-231, and BT549 with IC50 values of 42.01 nM, 93.61 nM, 91.44 nM, and 160.9 nM, respectively[1].
MKI-3 (250 nM; 12 h) suppresses the MASTL-ENSA-Aurora A signaling axis, inducing apoptotic markers, in BT549 and 4T1 breast cancer cells[1].
MKI-3 (250 nM; 24 h) activates PP2A in BT549 breast cancer cells[1].
MKI-3 (250 nM; 24 h) induces mitotic defects including aberrant nuclear morphology, multipolar spindles, and centrosome abnormalities in BT549 breast cancer cells[1].
MKI-3 (250 nM; 48 h) antiproliferative activity in BT549 breast cancer cells is mediated in part by PP2A activation, as co-treatment with 20 nM okadaic acid rescues cell viability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BT549 and 4T1 breast cancer cells
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Concentration:250 nM
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Incubation Time:12 h
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Result:Reduced levels of phosphorylated ENSA (pENSA) and phosphorylated Aurora A (p-Aurora A), and increased levels of cleaved poly(ADP-ribose) polymerase (PARP) and gamma H2A histone family member X (γ-H2AX), markers of mitotic apoptosis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4T1 syngeneic mouse model[1]
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Dosage:8 mg/kg
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Administration:i.p.; daily; 2 weeks
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Result:Reduced mean nuclear size diameter.
Increased cells staining positive for phospho-histone H3 and cleaved caspase-3.
Significantly reduced phosphorylation of ENSA and Aurora A in tumor tissues, with near-complete suppression relative to controls.
Chemical Information
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CAS No. 3084702-28-0
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분자량 385.42
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화학식 C21H19N7O
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SMILES
O=C(C1=CC=C(NC2=NC3=CC=CC=C3C(NC4=NNC(C5CC5)=C4)=N2)C=C1)N
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MKI-3 Related Classifications
HY-182391 Related Classifications
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