2. Epigenetics
  3. MicroRNA
  4. Rubone

Rubone, a chalcone analog, is a modulator of miR-34a. Rubone upregulates miR-34a expression in a p53 dependent manner, downregulates the downstream target Bcl-2 and Cyclin D1 expression, and suppresses hepatocellular carcinoma (HCC) growth in vivo. Rubone enhances the anticancer effect of Paclitaxel (PTX; HY-B0015) in PTX-resistant prostate cancer cell lines by reversing the expression of miR-34a downstream targets.

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Rubone Chemical Structure

Rubone Chemical Structure

CAS No. : 73694-15-2

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Rubone Related Antibodies

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Description

Rubone, a chalcone analog, is a modulator of miR-34a. Rubone upregulates miR-34a expression in a p53 dependent manner, downregulates the downstream target Bcl-2 and Cyclin D1 expression, and suppresses hepatocellular carcinoma (HCC) growth in vivo. Rubone enhances the anticancer effect of Paclitaxel (PTX; HY-B0015) in PTX-resistant prostate cancer cell lines by reversing the expression of miR-34a downstream targets[1][2][3].

In Vitro

Rubone (0-60 μM) exhibits significantly high cytotoxicity in DU145-TXR and PC3-TXR cells, suggesting that Rubone has stronger anticancer effect in advanced prostate cancer cells, which has lower miR-34a expression[3].
Rubone (5, 10 uM; 48 h) significantly reverses the expression of miR-34a downstream gene targets of DU145-TXR and PC3-TXR cell lines[3].
Rubone (5, 10 uM; 48 h) upregulates miR-34a in PTX-resistant DU145-TXR and PC3-TXR cell lines in a dose dependent manner[3].
Rubone (5 μM; for 2 weeks) and PTX (for 2 weeks) combination therapy inhibit PC3-TXR cell growth and sphere formation in 3D model, including 3D on top and hanging drop model. Rubone and PTX combination therapy inhibit cell invasion, migration, and cancer stem-like cells (CSCs) population in a p53-independent pathway. Rubone monotherapy or Rubone and PTX combination significantly enhances TAp73 and Elk-1 expression[3].

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

Rubone Related Antibodies

Cell Cytotoxicity Assay[3]

Cell Line: DU145, PC3, PTX resistant DU145-TXR, PC3-TXR, LNCaP, LNCaP developed C4-2 cells
Concentration: 0-60 μM
Incubation Time:
Result: Exhibited significantly higher cytotoxicity in DU145-TXR and PC3-TXR cells.

Western Blot Analysis[3]

Cell Line: DU145-TXR and PC3-TXR cell lines
Concentration: 5, 10 uM
Incubation Time: 48 h
Result: Significantly reversed the expression of miR-34a downstream gene targets of DU145-TXR and PC3-TXR cell lines, including E-cadherin, SIRT1, and Cyclin D1, whereas E-cadherin expression was not reversed in DU145-TXR cell line.

Real Time qPCR[3]

Cell Line: DU145-TXR and PC3-TXR cell lines
Concentration: 5, 10 uM
Incubation Time: 48 h
Result: Upregulated miR-34a in PTX-resistant DU145-TXR and PC3-TXR cell lines in a dose dependent manner.
In Vivo

Rubone monotherapy (20 mg/kg loaded PEG-PCD micelles; iv for five doses every other day) or combination therapy with PTX (10 mg/kg for each drug loaded PEG-PCD micelles) significantly upregulates miR-34a expression in tumor. The combination therapy inhibits tumor growth. Rubone monotherapy failed to suppress tumor cell proliferation[3].

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

Animal Model: 8 weeks old male nude mice transfected prostate cancer cells[3]
Dosage: 20 mg/kg or 10 mg/kg for each drug (PTX and Rubone) loaded PEG-PCD micelles
Administration: Intravenously for five doses every other day
Result: Had little effect on body weight loss and inhibited tumor growth.
Monotherapy or combination therapy with PTX significantly upregulated miR-34a expression in tumor.
Alone or with PTX significantly reversed E-cadherin, Cyclin D1, and SIRT1 expression.
Molecular Weight

374.38

Formula

C20H22O7
CAS No.
SMILES

O=C(/C=C/C1=CC(OC)=C(C=C1OC)OC)C2=C(C=C(C=C2O)OC)OC
Structure Classification
Initial Source
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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Rubone 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:

Rubone73694-15-2MicroRNAmiRNAchalconemiR-34ap53Bcl-2Cyclin D1hepatocellular carcinomaHCCPTXprostate cancerDU145PC3Inhibitorinhibitorinhibit

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