2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis Epigenetics
  3. MASTL Apoptosis Aurora Kinase PARP Caspase
  4. 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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MKI-3

MKI-3 Chemical Structure

CAS No. : 3084702-28-0

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MKI-3 Related Antibodies

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Aurora Kinase Aurora A Aurora B Aurora C

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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[1].

In Vitro

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.

MKI-3 Related Antibodies

Western Blot Analysis[1]

Cell Line: BT549 and 4T1 breast cancer cells
Concentration: 250 nM
Incubation Time: 12 h
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.
In Vivo

MKI-3 (8 mg/kg; i.p.; daily; 2 weeks) significantly reduces tumor growth in a 4T1 triple-negative breast cancer mouse model, induces mitotic cell death, and suppresses the MASTL−ENSA−Aurora A signaling pathway[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4T1 syngeneic mouse model[1]
Dosage: 8 mg/kg
Administration: i.p.; daily; 2 weeks
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.
Molecular Weight

385.42

Formula

C21H19N7O
CAS No.
SMILES

O=C(C1=CC=C(NC2=NC3=CC=CC=C3C(NC4=NNC(C5CC5)=C4)=N2)C=C1)N
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MKI-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MKI-33084702-28-0MKI3MKI 3MASTLApoptosisAurora KinasePARPCaspaseMicrotubule‐associated serine/threonine kinase likepoly ADP ribose polymeraseendosulfine alphaBT549protein phosphatase 2AMCF74T1MDA-MB-231triple-negative breast cancerAurora AENSAInhibitorinhibitorinhibit

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