ABL127

Name: ABL127
Brand: MedChemExpress
SKU: HY-108317
Rating: 4.5 (1 reviews)

Cat. No.: HY-108317 Purity: 99.6%: FAQs
Data Sheet SDS COA Handling Instructions

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ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC₅₀s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.

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

ABL127 Chemical Structure

CAS No. : 1073529-41-5

Size	Price	Stock	Quantity
5 mg	USD 445	In-stock	Estimated Time of Arrival: December 31
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50 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC₅₀s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.

IC₅₀ & Target

IC50: 6.4 nM (PME-1 in HEK293T), 4.2 nM (PME-1 in MDA-MB-231)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	IC₅₀	10 nM Compound: 1, ABL127	Inhibition of PME1 binding to FP-rhodamine in human MDA-MB-231 cells after 30 mins by fluorescence polarization activity-based protein profiling assay Inhibition of PME1 binding to FP-rhodamine in human MDA-MB-231 cells after 30 mins by fluorescence polarization activity-based protein profiling assay	[PMID: 21639134]

In Vitro

Three described PME-1 inhibitors are tested in this assay and a thermal shift with 100 μM ABL127 is detected. Using 25 or 50 μM ABL127 also shows a shift in protein melting temperature. It is found that treatment of Ishikawa cells with ABL127 and AMZ-30 significantly decreases cell proliferation similarly to depletion of PME-1 with shRNA. It is also found that treatment of ECC-1 cells with ABL127 or AMZ-30 affects cell invasion in a dose-dependent manner. The treatment of EC cells with ABL127 leads to a significant ~45 % increase in protein phosphatase 2A (PP2A) activity, while treatment with AMZ-30 leads to a modest ~10 % increase in PP2A activity^[1].

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

In Vivo

No significant decrease in tumor burden can be assessed in these pilot studies^[1]. Gel-based profiles indicate that brain PME-1 is inactivated by ABL127, but overlapping serine hydrolase activities preclude a confident assessment of the extent of inactivation^[2].

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

Molecular Weight

332.35

Formula

C₁₇H₂₀N₂O₅

CAS No.

1073529-41-5

Appearance

Oil

Color

Colorless to off-white

SMILES

O=C(N1N(C(OC)=O)[C@@](C2=CC=CC=C2)(C3CCCC3)C1=O)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (300.89 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	3.0089 mL	15.0444 mL	30.0888 mL
5 mM	0.6018 mL	3.0089 mL	6.0178 mL
10 mM	0.3009 mL	1.5044 mL	3.0089 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (7.52 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.52 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 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 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.52 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)

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: 99.91%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (260 KB) LCMS (264 KB)

Handling Instructions (2659 KB)

References

[1]. Pusey M, et al. Inhibition of protein methylesterase 1 decreased cancerous phenotypes in endometrial adenocarcinoma cell lines and xenograft tumor models. Tumour Biol. 2016 Sep;37(9):11835-11842. [Content Brief]

[2]. Bachovchin DA, et al. Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors. Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):6811-6. [Content Brief]

Kinase Assay ^[1]	Human PME-1 protein lacking the last three amino acids (PME-1des3) is purified from Sf9 cells. The assay is completed by first conducting a 10 min pre-incubation of 1 μM PME-1des3 with 100 μM ABL127, 100 μM AMZ-30, 100 μM EHT, or vehicle (0.05 % DMSO) in the presence of SYBR Orange (1:1000, v/v) at 37°C in 1× NEB buffer 2 (50 mM NaCl, 10 mM Tris-HCl, 10 mM MgCl₂, 1 mM DTT, pH 7.9 at 25 °C); a thermal gradient is performed increasing temperature by 2°C per minute increments from 37 to 95°C, and fluorescence (492 to 610 nm) is acquired on a thermal cycler^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cells are subjected to 5 μg/mL puromycin selection for 10 to 14 days and are clonally expanded. Validated clones are incubated with media and compounds (including ABL127) for the indicated times for phenotypic assays^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	ECC-1 cells are subcutaneously inoculated into the flanks of female SCID mice and are allowed to grow until tumors reached ~400 mm³. A single intratumoral dose of ABL127 diluted in 10% DMSO/PBS is administered. The highest concentration tested is 5 mg/kg of ABL127 due to poor solubility of the compound^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Pusey M, et al. Inhibition of protein methylesterase 1 decreased cancerous phenotypes in endometrial adenocarcinoma cell lines and xenograft tumor models. Tumour Biol. 2016 Sep;37(9):11835-11842. [Content Brief] [2]. Bachovchin DA, et al. Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors. Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):6811-6. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0089 mL	15.0444 mL	30.0888 mL	75.2219 mL
	5 mM	0.6018 mL	3.0089 mL	6.0178 mL	15.0444 mL
	10 mM	0.3009 mL	1.5044 mL	3.0089 mL	7.5222 mL
	15 mM	0.2006 mL	1.0030 mL	2.0059 mL	5.0148 mL
	20 mM	0.1504 mL	0.7522 mL	1.5044 mL	3.7611 mL
	25 mM	0.1204 mL	0.6018 mL	1.2036 mL	3.0089 mL
	30 mM	0.1003 mL	0.5015 mL	1.0030 mL	2.5074 mL
	40 mM	0.0752 mL	0.3761 mL	0.7522 mL	1.8805 mL
	50 mM	0.0602 mL	0.3009 mL	0.6018 mL	1.5044 mL
	60 mM	0.0501 mL	0.2507 mL	0.5015 mL	1.2537 mL
	80 mM	0.0376 mL	0.1881 mL	0.3761 mL	0.9403 mL
	100 mM	0.0301 mL	0.1504 mL	0.3009 mL	0.7522 mL

ABL127 Related Classifications

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:

ABL1271073529-41-5ABL 127ABL-127OthersInhibitorinhibitorinhibit

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ABL127

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