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PFI-2

Cat. No. M5128
PFI-2 Structure
Synonym:

(R)-PFI-2

Size Price Availability
10mg USD 160  USD160 Out of stock
50mg USD 540  USD540 Out of stock
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Quality Control & Documentation
Biological Activity

(R)-PFI-2 shows 500-fold more inhibitory activity against human SETD7 than its enantiomer, (S)-PFI-2. In a cellular environment, through direct interactions with SETD7, affects Yes-Associated protein localization and phenocopies Setd7 genetic deletion on Hippo pathway signaling.

Chemical Information
Molecular Weight 499.52
Formula C23H25F4N3O3S
CAS Number 1627676-59-8
Solubility (25°C) DMSO 99 mg/mL
Water 4 mg/mL warmed
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] Barsyte-Lovejoy D,et.al. Proc Natl Acad Sci U S A. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.

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  Catalog
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Keywords: PFI-2, (R)-PFI-2 supplier, Histone Methyltransferase, inhibitors, activators


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