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SML1408

(R)-PFI-2

≥97% (HPLC)

Synonym(s):

(R)-8-Fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide hydrochloride

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About This Item

Empirical Formula (Hill Notation):
C23H25F4N3O3S · HCl
CAS Number:
1627607-87-7
Molecular Weight:
535.98
UNSPSC Code:
12352200
PubChem Substance ID:
329825855
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
powder
Quality level:
100
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Quality Level

100

assay

≥97% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear (warmed)

storage temp.

2-8°C

SMILES string

FC1=C2C(CCNC2)=CC(S(N[C@H](CC3=CC=CC(C(F)(F)F)=C3)C(N4CCCC4)=O)(=O)=O)=C1.[H]Cl

InChI

1S/C23H25F4N3O3S.ClH/c24-20-13-18(12-16-6-7-28-14-19(16)20)34(32,33)29-21(22(31)30-8-1-2-9-30)11-15-4-3-5-17(10-15)23(25,26)27;/h3-5,10,12-13,21,28-29H,1-2,6-9,11,14H2;1H/t21-;/m1./s1

InChI key

ZADKZNVAJGEFLC-ZMBIFBSDSA-N

Biochem/physiol Actions

(R)-PFI-2 is a histone-lysine N-methyltransferase (HKMT) inhibitor selective for SETD7 (also known as SET9).
(R)-PFI-2 is a histone-lysine N-methyltransferase (HKMT) inhibitor selective for SETD7 (also known as SET9). (R)-PFI-2 has an IC50 value of 2 nM and 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. For full characterization details, please visit the PFI-2 probe summary on the Structural Genomics Consortium (SGC) website.

(S)-PFI-2, an enantiomer of (R)-PFI-2, is used as a negative control. (S)-PFI-2 is available from Sigma. To learn more about and purchase (S)-PFI-2, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

Features and Benefits

(R)-PFI-2 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Other Notes

(R)-PFI-2 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the (R)-PFI-2 probe summary on the Chemical Probes Portal website.

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000083758
0000083771
0000042134
0000011426
085M4614V

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Maria Bichmann et al.
Molecular neurodegeneration, 16(1), 46-46 (2021-07-04)
Human tauopathies including Alzheimer's disease (AD) are characterized by alterations in the post-translational modification (PTM) pattern of Tau, which parallel the formation of insoluble Tau aggregates, neuronal dysfunction and degeneration. While PTMs on aggregated Tau have been studied in detail