Anticancer agent 160
Anticancer agent 160 (Compound 6) is a natural product derived from Parthenium hysterophorus. Anticancer agent 160 is cytotoxic to HCT-116 cells, IC50=5.0 μM.
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- CAS No.: 2983122-03-6
- Formule: C28H29NO6
- Masse moléculaire:475.53
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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
Activité biologique
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Caspase 3 23.4 nM (EC50) |
M109S (0.1-10000 nM, 24-48 h) can inhibit apoptosis induced by Bax as well as Bak[1].
M109S (0-10μM, 4 h) M109S suppresses Staurosporine (HY-15141 STS)-induced apoptosis in MEFs [1].
M109S (0-10μM, 24 h) inhibits Etoposide(HY-13629)-induced apoptosis in Neuro2a cells[1].
M109S (500 nM, 24 h) inhibits Obatoclax(HY-10969A)-induced apoptosis in ARPE19 cells[1].
M109S (500 nM, 48 h) suppresses the conformation change (N-terminal exposure) [1].
M109S (500 nM, 48 h) suppresses the mitochondrial translocation of Bax[1].
M109S(1.0 μM, 4 h) decreases mitochondrial oxygen consumption and reactive oxygen species, whereas M109S(0.1–1 mM)) increases glycolysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MEF(Wt, Bax only, Bak only)
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Concentration:0.1 nM, 1 nM, 10 nM, 100 nM, 10000 nM
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Incubation Time:24 h((WT and Bax-only), 48 h (Bak-only)
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Result:Showed a dose-dependent suppression of caspase activation in all three types of MEFs.
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Cell Line:Showed a dose-dependent suppression of caspase activation in all three types of MEFs.
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Concentration:0 nM, 1.6 nM,8 nM, 40 nM, 200 nM, 10 μM
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Incubation Time:4 h
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Result:Suppressed STS-induced caspase activation in a dose-dependent manner.
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Cell Line:Neuro2a
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Concentration:0 nM, 40 nM, 200 nM, 10 μM
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Incubation Time:24 h
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Result:Suppressed Etoposide -induced caspase activation in a dose-dependent manner.
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Cell Line:ARPE19
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Concentration:500 nM
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Incubation Time:24 h
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Result:Significantly inhibited Obatoclax-induced apoptosis in ARPE19 cells comparing to control.
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Cell Line:iBax cells
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Concentration:500 nM
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Incubation Time:48 h
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Result:The frequency of the punctuated staining was significantly reduced by M109S.
M109S(i.p., 1 mg/kg, i.v., 5 mg/kg, or o.p., 10 mg/kg) is an orally bioactive cell death inhibitor penetrating blood-brain/retina-barrier[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Abca4-/-Rdh8-/- mice
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Dosage:10mg/kg
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Administration:Oral Gavage (PO)
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Result:Comparing to micewith M109S, the number of AF spots was similar to that detected in the dark-adapted mice
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Animal Model:Mice and Rat
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Dosage:Intraperitoneal injection (IP, 1 mg/kg), Intravenous injection (IV, 5 mg/kg), or Oral gavage (OP, 10 mg/kg).
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Administration:Intraperitoneal injection (IP, 1 mg/kg), Intravenous injection (IV, 5 mg/kg), or Oral gavage (OP, 10 mg/kg).
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Result:In mice, M109S reached 1.0 mg/mL (2.6 mM) plasma concentration within 30 min from administration, and it remained at 596± 134 ng/mL (1.6± 0.36 mM) 24 h after the oral gavage administration, the same as in rat. At 24 h after the oral gavage administration, the level of M109S in the plasma was 565.3± 188.3 nM in rats.The level of M109S in the rat retina and brain reached 171.0± 52.0 nM and 222.7± 74.7 nM, respectively, 24 h after its oral administration.
Chemical Information
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CAS No. 2983122-03-6
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Masse moléculaire 475.53
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Formule C28H29NO6
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SMILES
O=C1C=C[C@]2(O)[C@]1(C)[C@H](OC([C@]3(C(C(C4=CC=CC=C45)=O)6C5=O)C[C@@H]7N6CCC7)=O)[C@H]3CC[C@@H]2C
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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