2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. RAR/RXR Apoptosis PARP Bcl-2 Family
  4. BPA-B9

BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction. BPA-B9 has excellent RXRα-binding affinity (KD=39.29 ± 1.12 nM). BPA-B9 inhibits the proliferation of cancer cells by inducing mitotic arrest and cell apoptosis.

For research use only. We do not sell to patients.

BPA-B9 Chemical Structure

BPA-B9 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

BPA-B9 Related Antibodies

Top Publications Citing Use of Products

View All PARP Isoform Specific Products:

View All Isoforms

View All Bcl-2 Family Isoform Specific Products:

View All Isoforms

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction. BPA-B9 has excellent RXRα-binding affinity (KD=39.29 ± 1.12 nM). BPA-B9 inhibits the proliferation of cancer cells by inducing mitotic arrest and cell apoptosis[1].

IC50 & Target

PARP

 

Bcl-2

 

Mcl-1

 

In Vitro

BPA-B9 (0-250 nM, 24 h) induces a dose-dependent increase of apoptotic cells in MDA-MB-231 cells[1].
BPA-B9 (0-125 nM, 12 h) inhibits the cell cycle of A549 in the G2/M phase[1].
BPA-B9 (0-500 nM, 0-24 h) induces a dose- and time-dependent increase in the expression of cleaved PARP, and anti-apoptosis proteins Bcl-2 and Mcl-1 were reduced dose-dependently[1].
BPA-B9 shows excellent anti-proliferative activity against TNBC cell line MDA-MB-231 (IC50=16 ± 3 nM, SI > 3), and displays potent activities against HCC1937, A549, H460, HepG2, and HeLa cells with IC50 values of 0.561 μM, 0.201 μM, 0.253 μM, 0.128 μM, and 0.077 μM, respectively[1].

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

BPA-B9 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells and A549 cells
Concentration: 0, 31.25, 62.50, 125, and 250 nM
Incubation Time: 24 h
Result: Induced a dose-dependent t (0, 31.25, 62.50, 125, and 250 nM) increase (7.96, 16.94, 28.30, 30.40, 40.40%) of apoptotic cells in MDA-MB-231 cells.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells and A549 cells
Concentration: 0, 15.625, 31.25, 62.50, and 125 nM
Incubation Time: 12 h
Result: Inhibited the cell cycle of A549 in the G2/M phase. After incubation with BPA-B9 at 62.50 nM and 125 nM, the percentage of A549 cells in the G2/M phase reached 12.89% and 46.49%, respectively, compared to 8.62% in untreated cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 7.8, 31.3, 125, and 500 nM
Incubation Time: 0, 1, 3, 6, 8, 10, 12, 16, and 24 h
Result: Induced a time-dependent increase in the expression of cleaved PARP. Moreover, cleaved PARP was elevated, and anti-apoptosis proteins Bcl-2 and Mcl-1 were reduced dose-dependently.
In Vivo

BPA-B9 (0-25 mg/kg, IP, once every day for 15 days) has significant anticancer efficacy in vivo with no considerable side effects[1].
BPA-B9 (25 mg/kg, IP or PO, once) displays better pharmacokinetics than the lead XS-060 (HY-149085)[1].

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

Animal Model: BALB/c mice (aged 4-6 weeks, with injection of MDA-MB-231 cells)[1]
Dosage: 0, 12.5, 25 mg/kg
Administration: IP, once every day for 15 days
Result: Inhibited tumor growth by causing mitotic arrest, chromosome aberrations, and DNA-damage response. Significantly reduced the tumor volume and the tumor growth inhibition (TGI) of BPA-B9 was 59.3% at a dosage of 25.0 mg/kg/day, but a slight difference was shown at the dose of 12.5 mg/kg/day with no statistical significance.
Animal Model: Sprague-Dawley rats (10-14 weeks, 200-220g)[1]
Dosage: 25 mg/kg
Administration: Oral absorption (p.o.) and intraperitoneal injection (i.p.), once, (Pharmacokinetic Analysis)
Result: The oral absorption of BPA-B9 is very poor, while intraperitoneal injection displayed good absorption.
Pharmacokinetic Parameters of XS-060 in Sprague-Dawley rats[1].
BPA-B9 25 mg/kg (i.p.)
Tmax (h) 0.14 ± 0.10
Cmax (μg/L) 8083.33 ± 1193.04
AUC0-∞ (μg⋅h/L) 14615.65 ± 5508.77
T1/2 (h) 2.23 ± 0.17
CLz/F (L/(h⋅kg)) 1.55 ± 0.73
Vd, z/F (L/kg) 5.15 ± 2.78
Molecular Weight

414.50

Formula

C25H26N4O2
SMILES

O=C(NC1=NC=CC(C2=CC(N3CCC(CC3)CO)=NC=C2)=C1)/C=C/C4=CC=CC=C4
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

BPA-B9 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

BPA-B9RAR/RXRApoptosisPARPBcl-2 FamilyRetinoic acid receptorsRetinoid X receptorspoly ADP ribose polymeraseMDA-MB-231 cellsA549 cellsHCC1937H460HepG2HeLa cellsmitoticpRXRα-PLK1RXRαInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
BPA-B9
Cat. No.:
HY-149086
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.