AP20187 (Synonyms: B/B Homodimerizer)

Name: AP20187
Brand: MedChemExpress
SKU: HY-13992
Rating: 5.0 (30 reviews)

Cat. No.: HY-13992 Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 195514-80-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 816	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 816	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 320	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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

Customer Review

Based on 30 publication(s) in Google Scholar

28 Publications Citing Use of MCE AP20187

: 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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Protocol
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References
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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.

Molecular Weight

1482.75

Formula

C₈₂H₁₀₇N₅O₂₀

CAS No.

195514-80-8

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

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

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.

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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: 6 mg/mL (4.05 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 6 mg/mL.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (60.0 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% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: 6 mg/mL (4.05 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 6 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (60.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

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 4

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 5

Add each solvent one by one: 4% Ethanol 10% PEG-400 2% Tween-80 84% H2O
Solubility: 2.4 mg/mL (1.62 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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.

Purity & Documentation

Purity: 99.86%

Select Batch:

Data Sheet (281 KB) SDS (251 KB)

COA (253 KB) HNMR (249 KB) LCMS (88 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]

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	[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]

Complete Stock Solution Preparation Table

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

AP20187 Related Classifications

Metabolic Disease

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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AP20187 (Synonyms: B/B Homodimerizer)

Customer Review

AP20187 Related Antibodies

28 Publications Citing Use of MCE AP20187

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Biological Activity

Protocol

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References

Customer Review

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Complete Stock Solution Preparation Table

AP20187 Related Classifications

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