sevenspikes.themes.common.filters
sevenspikes.themes.common.closemenu

AP20187,≥99.5% (HPLC)

别名:(2S,2′S)-1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-2-piperidinecarboxylic acid, 2,2′-[[2-[(dimethylamino)methyl]-1,3-propanediyl]bis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene[(1R)-3-(3,4-dimethoxyphenyl)propylidene]]] ester

CAS号 195514-80-8 经验分子式(希尔表示法) C82H107N5O20 分子量 1482.75 MDL number MFCD28167729
制造商品牌: BSZH 科学公司
货号(SKU): HY-13992
CAS号: 195514-80-8
MDL号: MFCD28167729
增值税发票 √ 免费送货 √ 订货电话:010-68689484
¥4,360.00

产品描述

Biochem/physiol Actions

AP20187 is a synthetic and cell-permeable FK506 (tacrolimus) analog that acts as a chemical dimerizer, a chemical inducer of dimerization (CID), to reversibly dimerize and activate fusion proteins containing a growth factor receptor signaling DmrB domain. It has been used to induce oligomerization of cell surface receptor proteins and to study the activity and/or re-localization of any protein that affected by oligomerization. AP20187 has been found to act as a senolytic. In a transgenic mouse model that expresses the FK506-binding protein–caspase 8 (FKBP–Casp8) fusion protein, AP20187 activated FKBP-fused Casp8 in senescent cells resulting in apoptosis of the cells resulting in delayed tumorigenesis , diminished age-related organ deterioration, and extended life span.

AP20187是合成的且细胞可渗透的FK506(他克莫司)类似物,充当化学二聚体,二聚化(CID)的化学诱导剂,可逆地二聚化并激活包含生长因子受体信号转导DmrB结构域的融合蛋白。 它已被用来诱导细胞表面受体蛋白质的寡聚化,并研究任何受寡聚化影响的蛋白质的活性和/或重新定位。 已发现AP20187可以起到缓和作用。 在表达FK506结合蛋白-caspase 8(FKBP–Casp8)融合蛋白的转基因小鼠模型中,AP20187激活衰老细胞中FKBP融合的Casp8,导致细胞凋亡,导致肿瘤发生延迟,与年龄相关的器官退化减少, 并延长了使用寿命。

Description

AP20187 (B/B Homodimerizer) is a cell-permeable ligand used to dimerize FK506-binding protein (FKBP) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.

IC50 & Target

FKBP homodimerizer[1]

In Vitro

When LNCaP cells are treated with AP20187 (B/B Homodimerizer) (100 nM), ro-iCaspase-9 levels are significantly reduced, and the smaller processed active caspase-9 becomes apparent[2].

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

In Vivo

Real-time PCR analysis shows that AP20187 (B/B Homodimerizer) (0.5 mg/kg, 2 mg/kg, or 5 mg/kg) treatment significantly increases the levels of CHOP mRNA in the CNS of PLP/Fv2E-PERK mice at PID12. AP20187 treatment significantly alleviates EAE-induced myelin damage in these mice. AP20187 (B/B Homodimerizer) treatment significantly reduces the number of degenerating axons and increases the density of axons in the demyelinating lesions in the lumbar spinal cord of PLP/Fv2E-PERK mice[2].

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

Molecular Weight

1482.75

Formula

C₈₂H₁₀₇N₅O₂₀

CAS No.

195514-80-8

SMILES

COC1=C(OC)C=C(CC[C@H](C2=CC=CC(OCC(NCC(CN(C)C)CNC(COC3=CC=CC([C@H](OC([C@H]4N(C([C@@H](CC)C5=CC(OC)=C(OC)C(OC)=C5)=O)CCCC4)=O)CCC6=CC(OC)=C(OC)C=C6)=C3)=O)=O)=C2)OC([C@@H]7CCCCN7C([C@H](C8=CC(OC)=C(OC)C(OC)=C8)CC)=O)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder-20°C3 years
 4°C2 years
In solvent-80°C6 months
 -20°C1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 57 mg/mL (38.44 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
ConcentrationSolventMass1 mg5 mg10 mg
1 mM0.6744 mL3.3721 mL6.7442 mL
5 mM0.1349 mL0.6744 mL1.3488 mL
10 mM0.0674 mL0.3372 mL0.6744 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (1.69 mM); Clear solution

     
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (1.69 mM); Clear solution

References
  • [1]. Ahmed S, et al. Photocleavable dimerizer for the rapid reversal of molecular trap antagonists. J Biol Chem. 2014 Feb 21;289(8):4546-52.

    [2]. Lin W, et al. Oligodendrocyte-specific activation of PERK signaling protects mice against experimental autoimmune encephalomyelitis. J Neurosci. 2013 Apr 3;33(14):5980-91.

    [3]. Haas ME, et al. The Role of Proprotein Convertase Subtilisin/Kexin Type 9 in Nephrotic Syndrome-Associated Hypercholesterolemia. Circulation. 2016 Jul 5;134(1):61-72.

商品规格
属性名称属性值
储存温度 Storage temp.-20°C低温冷冻
全球实时库存 Availability √美国St. Louis ≥ 99 | 欧洲Eur. ≥ 10 | 東京Tokyo ≥ 22 | 香港与北京 ≥ 32