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AP20187 

Cat. No.: HY-13992 Purity: 99.80%
Handling Instructions

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

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

AP20187 Chemical Structure

AP20187 Chemical Structure

CAS No. : 195514-80-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 2544 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
1 mg USD 360 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 960 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 1560 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
25 mg USD 2280 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 3120 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

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

    Western blotting analysis of lysates from 3×HA-IκBα-expressing HT-29 cells treated as indicated for 8 h.

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

    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 MCE. Usage Cited in: FASEB J. 2018 Jun 18:fj201800548.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    AP20187 is a cell-permeable molecule 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 (100 nM), ro-iCaspase-9 levels are significantly reduced, and the smaller processed active caspase-9 becomes apparent[2].

    In Vivo

    Real-time PCR analysis shows that AP20187 (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 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].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 57 mg/mL (38.44 mM)

    *"≥" 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      AP20187 is dissolved in 4% ethanol, 10% PEG-400, 1.75% Tween-20 in H2O[3].

    References
    Cell Assay
    [2]

    For the in vitro study, 16 h after ADV infection, cells are treated with R1881 (10 nM), AP20187 (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].

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

    Animal Administration
    [2]

    Mice[2]
    To activate the transgene Fv2E-PERK in oligodendrocytes, PLP/Fv2E-PERK transgenic mice are given intraperitoneal injections of AP20187 daily at a dose of 0.5 mg/kg, 2 mg/kg, or 5 mg/kg. Lyophilized AP20187 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.

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

    References
    Molecular Weight

    1482.75

    Formula

    C₈₂H₁₀₇N₅O₂₀

    CAS No.

    195514-80-8

    SMILES

    COC1=C(OC)C=C(CC[[email protected]](C2=CC=CC(OCC(NCC(CN(C)C)CNC(COC3=CC=CC([[email protected]](OC([[email protected]]4N(C([[email protected]@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([[email protected]@H]7CCCCN7C([[email protected]](C8=CC(OC)=C(OC)C(OC)=C8)CC)=O)=O)C=C1

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.80%

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    Product Name:
    AP20187
    Cat. No.:
    HY-13992
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    AP20187

    Cat. No.: HY-13992