NMac1
NMac1 is an orally active Nm23/NDPK activator. NMac1 directly binds to Nm23-H1 and activates the NDPK activity of recombinant Nm23-H1 with an EC50 of 10.7 uM. NMac1 induces AMPK activation and inhibits mTOR and ERK, leading to mitochondrial OXPHOS dysregulation and suppressing mitochondrial ROS production, which in turn induces mitochondrial dysfunction in MDA-MB-231 cells. NMac1 inhibits Complex I activity and suppresses changes in morphology and actin cytoskeleton organization following Rac1 activation in MDA-MB-231 cells. NMac1 inhibits tumor invasion, migration and metastasis. NMac1 is useful for studying metastatic tumors, such as breast cancer. NMac1 can be isolated from the ginger cassumunar Roxb.
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- CAS No.: 1332290-68-2
- Formule: C24H28O4
- Masse moléculaire:380.48
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
NMac1 inhibits the proliferation of cancer cells under glucose starvation (IC50s of 7.197 and 2.849 μM) in MDA-MB-231 and MCF7 cells[1].
NMac1 (0-20 μM, 0-20 h) induces AMPK activation and inhibits mTOR and ERK in the absence of glucose in MDA-MB-231 cells[1].
NMac1 (0-20 μM, 0-20 h) induces mitochondrial dysfunction by inhibiting ATP production and reducing the mitochondrial membrane potential in MDA-MB-231 cells[1].
NMac1 (0-10 μM, 0-100 min) induces ATP depletion by reducing oxygen consumption rate, producing mitochondrial ROS and inducing dysregulation of mitochondrial ATP production system OXPHOS in the absence of glucose in MDA-MB-231 cells[1].
NMac1 (250-500 μM, 0-100 min) inhibits complex I activity in MDA-MB-231 cells[1].
NMac1 (0-30 μM, 2-14 days) inhibits the proliferation of MDA-MB-231 spheroid cells in a dose-dependent manner[1].
NMac1 (0-25 μM, 16-24 h) inhibits Rac1 activation through NDPK activation of Nm23-H1, reduces the invasion and migration in MDA-MB-231 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:0, 5, 10, 12.5, 20 μM
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Incubation Time:0, 2, 4, 8, 12, 16, 20 h
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Result:Induced AMPK activation and inhibited mTOR, ERK, and pS6K, rapidly induces AMPK activation within 2 hours under glucose depletion.
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Cell Line:MDA-MB-231 cells
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Concentration:12.5 μM
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Incubation Time:6 h
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Result:Deteriorated the mitochondrial integrity of cells in the absence of glucose, reduced TOM20 levels.
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Cell Line:MDA-MB-231 cells
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Concentration:0, 5, 10, 25 μM
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Incubation Time:16 h
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Result:Reduced Rac1 activation.
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Cell Line:MDA-MB-231 cells
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Concentration:0, 5, 10, 25 μM
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Incubation Time:24 h
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Result:Reduced the invasion and migration in a dose dependent manner, without affecting their proliferation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Breast cancer (MDA-MB-231-Luc-D3H2LN cells, 1 × 106) metastasis NOD/SCID mice model[2]
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Dosage:10 mg/kg
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Administration:p.o., once a day, 21 days
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Result:Significantly inhibited breast cancer metastasis without affecting primary tumor size.
Chemical Information
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CAS No. 1332290-68-2
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Masse moléculaire 380.48
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Formule C24H28O4
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SMILES
COC1=CC(/C=C/C2C(C3=CC=C(OC)C(OC)=C3)C=CCC2)=CC=C1OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Lee JJ,et al. Small molecule activator of Nm23/NDPK as an inhibitor of metastasis. Sci Rep. 2018 Jul 19;8(1):10909. [Content Brief]
[2]. Kim B, et al. Nm23-H1 activator phenylbutenoid dimer exerts cytotoxic effects on metastatic breast cancer cells by inducing mitochondrial dysfunction only under glucose starvation. Sci Rep. 2021 Dec 7;11(1):23549. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NMac1 Related Classifications
HY-115507 Related Classifications
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