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

BPA-B9 是一种 RXRα 配体和拮抗剂，靶向 pRXRα-PLK1 相互作用。BPA-B9 具有出色的 RXRα 结合亲和力 (KD=39.29 ± 1.12 nM)。 BPA-B9 通过诱导有丝分裂停滞和细胞凋亡 (apoptosis) 来抑制癌细胞的增殖。

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BPA-B9

BPA-B9 Chemical Structure

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BPA-B9 相关抗体

Top Publications Citing Use of Products

查看 RAR/RXR 亚型特异性产品:

查看所有亚型
RXRα RXRβ RXRγ

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.196 μM
Compound: B9; BPA-B9
Antiproliferative activity against wild type human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against wild type human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 37058970]
A549 IC50
0.201 μM
Compound: B9; BPA-B9
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 37058970]
A549 IC50
3.362 μM
Compound: B9; BPA-B9
Antiproliferative activity against RXRalpha knockout human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against RXRalpha knockout human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 37058970]
HCC1937 IC50
0.561 μM
Compound: B9; BPA-B9
Antiproliferative activity against human HCC1937 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCC1937 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 37058970]
HK-2 IC50
0.372 μM
Compound: B9; BPA-B9
Cytotoxicity against HK-2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxicity against HK-2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 37058970]
HaCaT IC50
0.051 μM
Compound: B9; BPA-B9
Cytotoxicity against human HaCaT cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxicity against human HaCaT cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 37058970]
HeLa IC50
0.077 μM
Compound: B9; BPA-B9
Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 37058970]
HepG2 IC50
0.128 μM
Compound: B9; BPA-B9
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 37058970]
L02 IC50
0.064 μM
Compound: B9; BPA-B9
Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 37058970]
MCF-10A IC50
18.58 μM
Compound: B9; BPA-B9
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 37058970]
MCF7 IC50
2.344 μM
Compound: B9; BPA-B9
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 37058970]
MDA-MB-231 IC50
0.016 μM
Compound: B9; BPA-B9
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 37058970]
NCI-H460 IC50
0.253 μM
Compound: B9; BPA-B9
Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
[PMID: 37058970]
体外研究
(In Vitro)

BPA-B9 (0-250 nM, 24 h) 在 MDA-MB-231 细胞中诱导细胞凋亡[1]。
BPA-B9 (0-125 nM, 12 h) 在G2/M期抑制A549细胞周期[1]。
BPA-B9 (0-500 nM, 0-24 h) 诱导裂解 PARP 表达的剂量和时间依赖性增加，抗凋亡蛋白 Bcl-2 和 Mcl-1 剂量依赖性降低 [1].
BPA-B9 对 TNBC 细胞系 MDA-MB-231 表现出优异的抗增殖活性 (IC50=16 ± 3 nM，SI > 3)，并对 HCC1937、A549、H460、 HepG2 和 HeLa 细胞的 IC50 值分别为 0.561 μM、0.201 μM、0.253 μM、0.128 μM 和 0.077 μM[1]。

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

BPA-B9 相关抗体:

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.
体内研究
(In Vivo)

BPA-B9 (0-25 mg/kg，腹腔注射，每天一次，连续15天）在体内具有显着的抗癌功效，且无明显副作用[1]。
BPA-B9 (25 mg/kg，腹腔注射或口服，一次)显示出比 XS-060 (HY-149085) 更好的药代动力学[1]。

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
分子量

414.50

Formula

C25H26N4O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BPA-B9 相关分类

  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

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

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× = ×
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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:

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

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