Biological Information

Background Information:

LMPTP (low molecular weight phosphotyrosine protein phosphatase) is a ubiquitously expressed protein tyrosine phosphatase involved in the modulation of signal transduction by the insulin, platelet derived growth factor (PDGF), and T-cell receptors. The ACP-1 (acid phosphatase ) gene encodes three transcriptional variants (A, B, and C) of LMPTP; the resulting proteins of which are distinct enzyme isoforms with unique chemical properties and activity. Human LMPTP polymorphisms that confer below-normal enzyme activity (i.e. AA or AB allele carriers) are associated with allergic atopic eczema/dermatitis syndrome (AEDS), obesity, diabetes, dyslipidemia and rheumatoid arthritis. Further, total serum IgE levels are lower in carriers of the ACP-1 genotype (CB), which confers above-normal enzyme activity. Over expression of LMPTP enzyme in cells transformed by PTK oncogenes leads to decreased proliferation indicating a possible role in preventing cancer cell proliferation. Therefore, inhibition of LMPTP-B may exacerbate the above noted disease states.

Family:

Phosphatase

Sub Family:

Acid Phosphatase

Class:

Protein Tyrosine

Protein Name:

ACP1

Uniprot Number:

P24666

Protein Aliases:

acid phosphatase of erythrocyte|low molecular weight phosphotyrosine protein phosphatase|red cell acid phosphatase

Gene Name:

ACP1

Gene ID:

52

Gene Aliases:

HAAP|LMW-PTP

Accession Number:

NM_004300

Organism:

Human

Construct Details:

Full Length, Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Spectrofluorimetry

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Human recombinant protein phosphatase LMPTP-B expressed in E. coli is used. Test compound and/or vehicle is preincubated with 2.2 U/ml enzyme‡ for 15 minutes at 37°C in modified HEPES buffer pH 7.2. The reaction is initiated by addition of 100 µM DiFMUP for 60 minutes. Determination of the amount of DiFMU formed is read spectrofluorimetrically at 358 nm/450 nm. Compounds are screened at 10 µM.

Substrate:

100 µM DiFMUP

Incubation:

60 min at 37°C

Control Inhibitor:

(NH₄)₆Mo₇O₂₄

Criteria For Significance:

≥ 50% of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 uM

Test Sample Requirements:

Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).

Minimum Order Quantity:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

61671

Name

Trisodium vanadate

Measurement

0.45μM - IC50

PubChem ID

91826558

Name

Na2MoO4.7H2O

Measurement

23μM - IC50

PubChem ID

329770925

Name

(NH4)6Mo7O24

Measurement

1.8μM - IC50

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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