Biological Information

Background Information:

Plasmin, a trypsin-like serine protease, is generated by proteolytic cleavage of plasminogen, a circulating proenzyme in the liver and secreted in plasma. As a fibrinolytic enzyme, plasmin degrades fibrin into soluble fibrin degradation products. Apart from blood clot dissolution, plasmin is involved in processes such as wound healing, angiogenesis, inflammation, tumor progression and neuronal degeneration. Plasmin is also implicated to play a role in the conversion of proenzyme involved in the complement pathways and in the generation of insulin and bradykinin.

Family:

Protease

Sub Family:

Chymotrypsin

Class:

Serine Peptidase

Protein Name:

Plasmin

Uniprot Number:

P00747

Gene Name:

PLG

Gene ID:

5340

Accession Number:

NM_000301

Organism:

Human

Construct Details:

Endogenous

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Spectrofluorimetry

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Human plasma plasmin is used. Test compound and/or vehicle is preincubated with 2 mU/ml enzyme in modified Tris-HCl buffer pH 7.6 for 15 minutes at 37˚C. The reaction is initiated by addition of 50 μM D-Val-Leu-Lys-AMC for another 60-minute incubation period. Determination of the amount of AMC formed is read spectrofluorimetrically at Excitation: 360 nm; Emission: 465 nm. Compounds are screened at 10 μM.

Substrate:

50 μM D-Val-Leu-Lys-AMC

Incubation:

60 min at 37°C

Control Inhibitor:

Patamostat

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

5311176

Name

PPACK

Measurement

0.37μM - IC50

PubChem ID

65921

Name

Patamostat

Measurement

0.026μM - IC50

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei