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PTP Inhibitor I

Cat. No. M20414
PTP Inhibitor I Structure
Synonym:

α-Bromo-4-hydroxyacetophenone, 2-Bromo-4'-hydroxyacetophenone, 4-Hydroxyphenacyl bromide, 4-Hydroxyphenacyl bromide, SHP-1 Inhibitor II

Size Price Availability Quantity
100mg USD 50  USD50 In stock
500mg USD 70  USD70 In stock
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Quality Control & Documentation
Biological Activity

PTP Inhibitor I is a cell-permeable, protein tyrosine phosphatase (PTP) inhibitor with Ki values of 43 and 42 μM for SHP-1(ΔSH2) and PTP1B, respectively.

Chemical Information
Molecular Weight 215.04
Formula C8H7BrO2
CAS Number 2491-38-5
Solubility (25°C) DMSO 43 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Mauro Siragusa, et al. Cardiovasc Res. VE-PTP inhibition elicits eNOS phosphorylation to blunt endothelial dysfunction and hypertension in diabetes

[2] Bigyan Sharma, et al. Eur J Med Chem. Recent advance on PTP1B inhibitors and their biomedical applications

[3] Rehan M Hussain, et al. Expert Opin Investig Drugs. Tie-2/Angiopoietin pathway modulation as a therapeutic strategy for retinal disease

[4] Wen-Shan Liu, et al. J Cell Biochem. Exploring the effect of inhibitor AKB-9778 on VE-PTP by molecular docking and molecular dynamics simulation

[5] Jae Eun Park, et al. Biochem Biophys Res Commun. PTP inhibitor IV protects JNK kinase activity by inhibiting dual-specificity phosphatase 14 (DUSP14)

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  Catalog
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Keywords: PTP Inhibitor I, α-Bromo-4-hydroxyacetophenone, 2-Bromo-4'-hydroxyacetophenone, 4-Hydroxyphenacyl bromide, 4-Hydroxyphenacyl bromide, SHP-1 Inhibitor II supplier, Phosphatase, inhibitors, activators


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