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PFI-2 hydrochloride

Cat. No. M9449
PFI-2 hydrochloride Structure
Synonym:

PFI-2 HCl; (R)-PFI-2 hydrochloride

Size Price Availability Quantity
10mg USD 150 In stock
50mg USD 525 In stock
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Quality Control
Biological Activity

PFI-2 hydrochloride is a potent, highly selective and cell-active inhibitor of the methyltransferase activity of SETD7, with IC50 of 2 nM. PFI-2 has been shown to bind to SETD7 by ITC (Kd=18nM) and biotinylated PFI-2 interacts with SETD7 in pull-down studies. Treatment of low-density MEFs with (R)-PFI-2 resulted in higher nuclear YAP levels indicating an effect on the Hippo pathway.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 535.98
Formula C23H25F4N3O3S.HCl
CAS Number 1627607-87-7
Purity 100.00%
Solubility DMSO ≥ 20 mg/mL
Storage at -20°C
References

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
Barsyte-Lovejoy D, et al. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8. PMID: 25136132.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PFI-2 hydrochloride, PFI-2 HCl; (R)-PFI-2 hydrochloride supplier, Histone Methyltransferase, inhibitors

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