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 Chemical Structure

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

  • 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

 

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

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (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

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目录号：
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