Cat. No.: HY-13992

AP20187

(Synonyms: B/B Homodimerizer)

54 Cited Publications

Customer Review

Based on 54 publication(s) in Google Scholar

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.

Purity: 99.85%
CAS No.: 195514-80-8
Formula: C₈₂H₁₀₇N₅O₂₀
Molecular Weight:1482.75

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AP20187 Chemical Structure

CAS No.: 195514-80-8

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Top Publications Citing

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (54)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

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].

MedChemExpress (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].

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

Chemical Information

CAS No. 195514-80-8
Appearance Solid
Molecular Weight 1482.75
Formula C₈₂H₁₀₇N₅O₂₀
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
Synonyms

B/B Homodimerizer
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (54)

All IHCFlow CytometryWBIn Vivo Efficacy Study

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Journal Impact Factor

Nature

Metastatic recurrence in colorectal cancer arises from residual EMP1+ cells. [Abstract]

2022 Nov;611(7936):603-613. PMID: 36352230
Cancer Cell

Interleukin-1α release during necrotic-like cell death generates myeloid-driven immunosuppression that restricts anti-tumor immunity. [Abstract]

2024 Dec 9;42(12):2015-2031.e11. PMID: 39577420
Circulation

The Role of Proprotein Convertase Subtilisin/Kexin Type 9 in Nephrotic Syndrome-Associated Hypercholesterolemia. [Abstract]

2016 Jul 5;134(1):61-72. PMID: 27358438
Cancer Discov

P21-positive senescent stromal cells promote prostate cancer immune suppression and progression that can be reversed by senolytic therapy. [Abstract]

2025 Oct 27. PMID: 41135083

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.
Cell Metab

Endothelial senescent-cell-specific clearance alleviates metabolic dysfunction in obese mice. [Abstract]

2025 Dec 2;37(12):2455-2465.e6. PMID: 41270738
Cell Metab

Obesity-Induced Cellular Senescence Drives Anxiety and Impairs Neurogenesis. [Abstract]

2019 May 7;29(5):1061-1077.e8. PMID: 30612898
Nat Cancer

Mex3a marks drug-tolerant persister colorectal cancer cells that mediate relapse after chemotherapy. [Abstract]

2022 Sep;3(9):1052-1070. PMID: 35773527
Cell Stem Cell

Zonation of Ribosomal DNA Transcription Defines a Stem Cell Hierarchy in Colorectal Cancer. [Abstract]

2020 Jun 4;26(6):845-861.e12. PMID: 32396863
Mol Cell

Mechanism of RACK1-dependent ZAKα activation at stalled and collided ribosomes. [Abstract]

2026 Jun 18;86(12):2341-2357.e10. PMID: 42214329
Nat Commun

Cytokine-armed pyroptosis induces antitumor immunity against diverse types of tumors. [Abstract]

2024 Dec 30;15(1):10801. PMID: 39737979
Nat Commun

Caspase-1 initiates apoptosis in the absence of gasdermin D. [Abstract]

2019 May 7;10(1):2091. PMID: 31064994
Cell Death Differ

RIP3-mediated necroptosis is regulated by inter-filament assembly of RIP homotypic interaction motif. [Abstract]

2021 Jan;28(1):251-266. PMID: 32737444
J Clin Invest

Aged murine bone marrow myeloid and mesenchymal cells develop unique senescence phenotypes. [Abstract]

2026 Jan 27:e195772. PMID: 41592025
Cell Discov

Discovery of a cooperative mode of inhibiting RIPK1 kinase. [Abstract]

2021 Jun 1;7(1):41. PMID: 34075030
Mol Ther

An in vivo CRISPR screen unveils promising target genes to improve CAR-T cell efficacy in a solid tumor model. [Abstract]

2026 Jul 1;34(7):3976-4000. PMID: 41935953
J Neuroinflammation

Senescent cell reduction does not improve recovery in mice under experimental autoimmune encephalomyelitis (EAE) induced demyelination. [Abstract]

2025 Apr 7;22(1):101. PMID: 40197319
Cell Death Dis

Quantitative analysis of phosphoproteome in necroptosis reveals a role of TRIM28 phosphorylation in promoting necroptosis-induced cytokine production. [Abstract]

2021 Oct 23;12(11):994. PMID: 34689152
Cell Death Dis

Necroptosis promotes cell-autonomous activation of proinflammatory cytokine gene expression. [Abstract]

2018 Apr 27;9(5):500. PMID: 29703889

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).
EMBO J

Cardiolipin inhibits the non-canonical inflammasome by preventing LPS binding to caspase-4/11. [Abstract]

2025 Aug;44(16):4419-4442. PMID: 40670771
EMBO J

Neutrophils induce paracrine telomere dysfunction and senescence in ROS-dependent manner. [Abstract]

2021 May 3;40(9):e106048. PMID: 33764576
J Transl Med

Senescence-induced endothelial-to-mesenchymal transition accelerates the subretinal fibrosis in neovascualr age-related macular degeneration. [Abstract]

2026 Jan 22;24(1):251. PMID: 41572339
J Transl Med

Cellular senescence in the response of HR+ breast cancer to radiotherapy and CDK4/6 inhibitors. [Abstract]

2023 Feb 10;21(1):110. PMID: 36765430
Aging Cell

Targeting senescent cells alleviates obesity-induced metabolic dysfunction. [Abstract]

2019 Jun;18(3):e12950. PMID: 30907060
Cell Death Discov

Interplay of telomerase non-canonical functions in NK cell resistance to iCasp9-mediated apoptosis. [Abstract]

2026 Jun 12. PMID: 42285928
Cell Death Discov

RIPK1 S213E mutant suppresses RIPK1-dependent cell death by preventing interactions with RIPK3 and CASP8. [Abstract]

2025 Jul 25;11(1):345. PMID: 40715038
EMBO Rep

Targeting intratumor heterogeneity suppresses colorectal cancer chemoresistance and metastasis. [Abstract]

2023 Aug 3;24(8):e56416. PMID: 37338390
Commun Biol

Cholesterol inhibits assembly and oncogenic activation of the EphA2 receptor. [Abstract]

2025 Mar 11;8(1):411. PMID: 40069393
Cancers (Basel)

Stromal Senescence following Treatment with the CDK4/6 Inhibitor Palbociclib Alters the Lung Metastatic Niche and Increases Metastasis of Drug-Resistant Mammary Cancer Cells. [Abstract]

2023 Mar 22;15(6):1908. PMID: 36980794
Methods

Quantifying membrane protein oligomerization with fluorescence cross-correlation spectroscopy. [Abstract]

2018 May 1:140-141:40-51. PMID: 29448037
FASEB J

GPCR kinase 2-interacting protein-1 protects against ischemia-reperfusion injury of the spinal cord by modulating ASK1/JNK/p38 signaling. [Abstract]

2018 Jun 18:fj201800548. PMID: 29912587

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.
Eur J Immunol

Vaccinia virus F1L blocks the ribotoxic stress response to subvert ZAKα-dependent NLRP1 inflammasome activation. [Abstract]

2024 Jul 31:e2451135. PMID: 39086059
Exp Cell Res

GW806742X can induce mouse MLKL activation by directly promoting MLKL kinase like domain dimerization. [Abstract]

2025 Apr 4:114539. PMID: 40189182
J Neurooncol

N-acetylcysteine remodels the tumor microenvironment of primary and recurrent mouse glioblastoma. [Abstract]

2025 May;173(1):131-145. PMID: 39954037
Life Sci Alliance

Congress of multiple dimers is needed for cross-phosphorylation of IRE1α and its RNase activity. [Abstract]

2024 Jun 17;7(9):e202302562. PMID: 38886017
PLoS One

Reduction of fibrosis and immune suppressive cells in ErbB2-dependent tumorigenesis by an LXR agonist. [Abstract]

2021 Mar 29;16(3):e0248996. PMID: 33780491
Microbiol Immunol

Caspase-7 mediates caspase-1-induced apoptosis independently of Bid. [Abstract]

2020 Feb;64(2):143-152. PMID: 31687791
STAR Protoc

Protocol for specific induction of apoptosis or necroptosis in established murine tumors. [Abstract]

2025 Nov 7;6(4):104185. PMID: 41205180
bioRxiv

2026 Jun 8.
bioRxiv

2026 Jun 25.
Georgetown University

2026.
bioRxiv

Two axolotl-adapted cell-ablation platforms reveal macrophage-dependent processes essential for spinal-cord and skeletal regeneration. [Abstract]

2026 Feb 12:2026.02.10.705144. PMID: 41727137
Tap chi Nghien cuu Y hoc

2025 May 05.
bioRxiv

2025 April 22.
bioRxiv

2025 April 02.
bioRxiv

2025 April 10.
bioRxiv

Hypoxia-inducible factor 1 protects neurons from Sarm1-mediated neurodegeneration. [Abstract]

2025 Jan 18:2025.01.17.633664. PMID: 39868134
bioRxiv

2025 February 11.
bioRxiv

Senescent cell clearance ameliorates temporal lobe epilepsy and associated spatial memory deficits in mice. [Abstract]

2024 Jul 31:2024.07.30.605784. PMID: 39211239
bioRxiv

Cholesterol inhibits assembly and activation of the EphA2 receptor. [Abstract]

2024 Jun 10:2024.06.10.598255. PMID: 38915729
bioRxiv

Spatiotemporal binding of cyclophilin A and CPSF6 to capsid regulates HIV-1 nuclear entry and integration. [Abstract]

2024 Apr 9:2024.04.08.588584. PMID: 38645162
bioRxiv

2023 Dec 19.
bioRxiv

Caspase-1 activates gasdermin A in non-mammals. [Abstract]

2024 Jan 3:2023.09.28.559989. PMID: 37987010
bioRxiv

Multiparametric senescent cell phenotyping reveals CD24 osteolineage cells as targets of senolytic therapy in the aged murine skeleton. [Abstract]

2023 Jan 13:2023.01.12.523760. PMID: 36711531
Harvard University

2016 Apr.

Solvent & Solubility

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 4% Ethanol 10% PEG400 2% Tween-80 84% Saline

Solubility: 1.82 mg/mL (1.23 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocol

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].

MedChemExpress (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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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AP20187

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Autophagy Compound Library

Peptidomimetic Library

Anti-Aging Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AP20187

Biological Activity

Chemical Information

Publications (54)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

AP20187

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Autophagy Compound Library

Peptidomimetic Library

Anti-Aging Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AP20187

Biological Activity

Chemical Information

Publications (54)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

AP20187 Related Classifications

Cat. No.: HY-13992