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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Based on 1 publication(s) in Google Scholar

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.
Appearance

Solid

Color

Light yellow to green yellow

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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (87.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5052 mL 17.5260 mL 35.0521 mL
5 mM 0.7010 mL 3.5052 mL 7.0104 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5052 mL 17.5260 mL 35.0521 mL 87.6301 mL
5 mM 0.7010 mL 3.5052 mL 7.0104 mL 17.5260 mL
10 mM 0.3505 mL 1.7526 mL 3.5052 mL 8.7630 mL
15 mM 0.2337 mL 1.1684 mL 2.3368 mL 5.8420 mL
20 mM 0.1753 mL 0.8763 mL 1.7526 mL 4.3815 mL
25 mM 0.1402 mL 0.7010 mL 1.4021 mL 3.5052 mL
30 mM 0.1168 mL 0.5842 mL 1.1684 mL 2.9210 mL
40 mM 0.0876 mL 0.4382 mL 0.8763 mL 2.1908 mL
50 mM 0.0701 mL 0.3505 mL 0.7010 mL 1.7526 mL
60 mM 0.0584 mL 0.2921 mL 0.5842 mL 1.4605 mL
80 mM 0.0438 mL 0.2191 mL 0.4382 mL 1.0954 mL
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Arborinine Related Classifications

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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