2. Epigenetics
  3. Histone Demethylase
  4. Arborinine

Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity .

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Arborinine Chemical Structure

Arborinine Chemical Structure

CAS No. : 5489-57-6

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Arborinine Related Antibodies

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Description

Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity [1][2].

IC50 & Target[2]

LSD1

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
35 μM
Compound: 5
Cytotoxicity against human A549 cells after 48 hrs by resazurin reduction assay
Cytotoxicity against human A549 cells after 48 hrs by resazurin reduction assay
[PMID: 20413315]
DLD-1 IC50
74 μM
Compound: 5
Cytotoxicity against human DLD1 cells after 48 hrs by resazurin reduction assay
Cytotoxicity against human DLD1 cells after 48 hrs by resazurin reduction assay
[PMID: 20413315]
In Vitro

Arborinine (0, 5, 15, 30 µM; 48 h) increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein[1].
Arborinine (20 µM) decreases the expression of UBE2O protein level in 786O cells[1].
Arborinine (20 µM) induces cell cycle arrest at the S phase and inhibits cell apoptosis[1].

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

Arborinine Related Antibodies

Cell Proliferation Assay[1]

Cell Line: 786O, A498, 769P, Caki1, OSRC2 cells
Concentration: 0-100 µM
Incubation Time: 48, 72 h
Result: Showed antiproliferative activity with IC50s of 30.62, 39.09, 15.67, 31.42, 30.35 µM at 48 h, 20.92, 27.01, 14.94, 30.26, 17.37 µM at 72 h for 786O, A498, 769P, Caki1, OSRC2 cells, respectively.

Western Blot Analysis[1]

Cell Line: 786O cells
Concentration: 0, 5, 15, 30 µM
Incubation Time: 48 h
Result: Increased the expression of H3K4me1/2 and H3K9me1/2 protein in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: 786O and A498 cells
Concentration: 20 µM
Incubation Time:
Result: Induced increased population in S phase and decreased population in G1 phase, significantly inhibited both early and late apoptosis of ccRCC cells
In Vivo

Arborinine (40, 80 mg/kg; p.o.; for 21 days) shows antitumor activity in mouse[2].

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

Animal Model: BALB/c nude mice (SGC-7901 cells and SGC-7901/ADR cells)[2]
Dosage: 40, 80 mg/kg
Administration: P.o.; for 21 days
Result: Inhibited the growth of tumors while unchanged the body weights.
Molecular Weight

285.29

Formula

C16H15NO4
CAS No.
SMILES

O=C1C2=C(C=CC=C2)N(C)C3=CC(OC)=C(OC)C(O)=C13
Structure Classification
Initial Source

Globigerina parva
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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Arborinine 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:

Arborinine5489-57-6Histone DemethylaseH3K4me1/2H3K9me1/2E-cad786O cellsS phaseantitumororally activeInhibitorinhibitorinhibit

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