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  3. FKBP
  4. AP20187

B/B Homodimerizer  (Synonyms: AP20187)

製品番号: HY-13992 純度: 99.85%
COA 取扱説明書 Technical Support

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.

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CAS 番号 : 195514-80-8

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 815 在庫あり
Solution
10 mM * 1 mL in DMSO USD 815 在庫あり
Solid
1 mg $110 在庫あり
5 mg $320 在庫あり
10 mg $500 在庫あり
25 mg $950 在庫あり
50 mg $1340 在庫あり
100 mg $1880 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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

カスタマーレビュー

Based on 48 publication(s) in Google Scholar

B/B Homodimerizer 関連抗体

Top Publications Citing Use of Products

顧客検証

IHC
Flow Cytometry
WB
In Vivo Efficacy Study

    AP20187 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2025 Oct 27.  [Abstract]

    Representative IHC staining of MPten prostate tumors from p21-ATTAC mice treated with AP20187 (2 mg/kg; ip) or vehicle controls for 2 weeks.

    AP20187 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2025 Oct 27.  [Abstract]

    AP20187 (2 mg/kg; ip). Flow cytometry analysis was performed on the number of CD8+ T cells and iMCs, as well as CD8+ T cell activation markers, in MPten prostate tumors of mice treated with p21-ATTAC.

    AP20187 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2025 Oct 27.  [Abstract]

    Kaplan-Meier survival curve of MPten prostate tumor-bearing p21-ATTAC mice (8 days post-transplantation) treated with vehicle, AP20187 (AP) (2mg/kg; ip) continuously, or AP for 2 weeks followed by continuous anti-PD-1 treatment.

    AP20187 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Apr 27;9(5):500.  [Abstract]

    Schematic representation of the oligomerizable MLKL (acMLKL) (upper) and western blotting analysis of lysates from HT-29 cells stimulated with DMSO or AP20187 for 2 h (lower).

    AP20187 purchased from MedChemExpress. Usage Cited in: FASEB J. 2018 Jun 18:fj201800548.  [Abstract]

    HEK293T cells that stably express FKBP3-His-ASK1 and Flag-GIT1 or Flag-GIT1 (ΔCC2) are pretreated with 100 nM AP20187 for 0.5 h followed by OGD/R for 1 h. Activation of ASK1 is assessed by the activating phosphorylation of ASK1, JNK, and p38 as determined by Western blot analysis.

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    製品説明

    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]
    体外実験

    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].

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

    B/B Homodimerizer 関連抗体
    体内実験

    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].

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

    1482.75

    分子式

    C82H107N5O20
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    Ethanol : ≥ 71.43 mg/mL (48.17 mM)

    DMSO : ≥ 57 mg/mL (38.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.6744 mL 3.3721 mL 6.7442 mL
    5 mM 0.1349 mL 0.6744 mL 1.3488 mL
    10 mM 0.0674 mL 0.3372 mL 0.6744 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.85%

    COA (253 KB) HNMR (216 KB) LCMS (88 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [2]

    For the in vitro study, 16 h after ADV infection, cells are treated with R1881 (10 nM), AP20187 (B/B Homodimerizer) (10 nM), both, or neither for 8 h. Cells are then rinsed with PBS and fixed with 4% paraformaldehyde for 1 h at room temperature. After rinsing with PBS, cells are incubated in ice-cold permeabilization solution (0.1% Triton X-100, 0.1% sodium citrate) for 2 min at 0°C. Cells are rinsed with PBS and stained with TUNEL reaction mixture for 60 min at 37°C. After another PBS wash, cells are incubated with Converter-AP for 30 min at 37°C. Cells are rinsed and incubated with substrate 5-bromo-4-chloro-3-indolyl phosphate/nitroblue tetrazolium for 30 min. After a final PBS rinse (repeated twice), cells are microphotographed[2].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [2]

    Mice[2]
    To activate the transgene Fv2E-PERK in oligodendrocytes, PLP/Fv2E-PERK transgenic mice are given intraperitoneal injections of AP20187 (B/B Homodimerizer) daily at a dose of 0.5 mg/kg, 2 mg/kg, or 5 mg/kg. Lyophilized AP20187 (B/B Homodimerizer) is dissolved in 100% ethanol at a concentration of 62.5 mg/mL stock solution and stored at −20°C. Injection solutions consist of 4% ethanol, 10% PEG-400, and 2% Tween-20 in water. The transgenic mice receiving only the vehicle (4% ethanol, 10% PEG-400, 2% Tween-20 in water) served as controls.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / Ethanol 1 mM 0.6744 mL 3.3721 mL 6.7442 mL 16.8606 mL
    5 mM 0.1349 mL 0.6744 mL 1.3488 mL 3.3721 mL
    10 mM 0.0674 mL 0.3372 mL 0.6744 mL 1.6861 mL
    15 mM 0.0450 mL 0.2248 mL 0.4496 mL 1.1240 mL
    20 mM 0.0337 mL 0.1686 mL 0.3372 mL 0.8430 mL
    25 mM 0.0270 mL 0.1349 mL 0.2698 mL 0.6744 mL
    30 mM 0.0225 mL 0.1124 mL 0.2248 mL 0.5620 mL
    Ethanol 40 mM 0.0169 mL 0.0843 mL 0.1686 mL 0.4215 mL
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    AP20187 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    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:

    AP20187195514-80-8B/B HomodimerizerAP 20187AP-20187FKBPFK506-binding proteinInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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