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AP20187 (Synonyms: B/B Homodimerizer)

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

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.

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
Estimated Time of Arrival: December 31
1 mg USD 360 In-stock
Estimated Time of Arrival: December 31
5 mg USD 960 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1560 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3120 In-stock
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.

    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 (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].

    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].

    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 (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].

    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 (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.

    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([C@@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