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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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Anticancer agent 160 Chemical Structure

Anticancer agent 160 Chemical Structure

CAS No. : 2983122-03-6

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Description

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[1].

IC50 & Target

Caspase 3

23.4 nM (EC50)

In Vitro

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.

Apoptosis Analysis[1]

Cell Line: MEF(Wt, Bax only, Bak only)
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 10000 nM
Incubation Time: 24 h((WT and Bax-only), 48 h (Bak-only)
Result: Showed a dose-dependent suppression of caspase activation in all three types of MEFs.

Apoptosis Analysis[1]

Cell Line: Showed a dose-dependent suppression of caspase activation in all three types of MEFs.
Concentration: 0 nM, 1.6 nM,8 nM, 40 nM, 200 nM, 10 μM
Incubation Time: 4 h
Result: Suppressed STS-induced caspase activation in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: Neuro2a
Concentration: 0 nM, 40 nM, 200 nM, 10 μM
Incubation Time: 24 h
Result: Suppressed Etoposide -induced caspase activation in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: ARPE19
Concentration: 500 nM
Incubation Time: 24 h
Result: Significantly inhibited Obatoclax-induced apoptosis in ARPE19 cells comparing to control.

Immunofluorescence[1]

Cell Line: iBax cells
Concentration: 500 nM
Incubation Time: 48 h
Result: The frequency of the punctuated staining was significantly reduced by M109S.
In Vivo

M109S(10mg/kg p.o., three time in 48 h) protects the retina from the bright-light-induced photoreceptor death[1].
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.

Animal Model: Abca4-/-Rdh8-/- mice
Dosage: 10mg/kg
Administration: Oral Gavage (PO)
Result: Comparing to micewith M109S, the number of AF spots was similar to that detected in the dark-adapted mice
Animal Model: Mice and Rat
Dosage: Intraperitoneal injection (IP, 1 mg/kg), Intravenous injection (IV, 5 mg/kg), or Oral gavage (OP, 10 mg/kg).
Administration: Intraperitoneal injection (IP, 1 mg/kg), Intravenous injection (IV, 5 mg/kg), or Oral gavage (OP, 10 mg/kg).
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.
Molecular Weight

475.53

Formula

C28H29NO6

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Anticancer agent 160 Related Classifications

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  • 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.

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Product Name:
Anticancer agent 160
Cat. No.:
HY-156186
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