ABL127

Cat. No.: HY-108317 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

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
Solution
10 mM * 1 mL in DMSO	USD 251	In-stock	Estimated Time of Arrival: December 31
Oil + Solvent
10 mM * 1 mL ready for reconstitution	USD 251	In-stock	Estimated Time of Arrival: December 31
Oil
5 mg	USD 228	Get quote	Estimated Time of Arrival: December 31
10 mg		Get quote
50 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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]

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].

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].

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

Molecular Weight

332.35

Appearance

Oil

Formula

C₁₇H₂₀N₂O₅

CAS No.

1073529-41-5

SMILES

O=C(N1N(C(OC)=O)[[email protected]@](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)

*"≥" 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

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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
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
3.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (285 KB) SDS (252 KB)

COA (259 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]

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.

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Keywords:

ABL1271073529-41-5ABL 127ABL-127OthersInhibitorinhibitorinhibit

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ABL127

Customer Review

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

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