PFI-6

Protein target name:

MLLT1, MLLT3

Mechanism of action:

Inhibitor

Recommended Concentration for use in cells:

up to 1 uM

Probe Information

Target and Probe Information

Target Details

Target class:

Epigenetics

Subclass:

YEATS

HUGO ID:

HGNC:7134 HGNC:7136

Entrez gene ID:

4298 4300

UNIPROT ID:

Q03111 P42568

Target alias:

ENL; LTG19; YEATS1; AF9; YEATS3

Probe Details

Chemical Probes Portal ID:

CPP2277

SMILES string:

O=C(N(C)C)C1=C(O)C=C(C2=CC(C(N[C@@H]3CCC4=C3C=CC=C4)=O)=NO2)C=C1

InChi Key:

IXWUILRSNIQHDM-QGZVFWFLSA-N

Control compound:

PFI-6N

Orthogonal probe:

SGC-iMLLT, NVS-MLLT-1

Physico-chemical properties

Solubility - preferred solvent:

DMSO

Solubility - concentration:

10 uM

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50, KD

140 nM MLLT1, 160 nM MLLT3 IC5082 nM MLLT1, 76 nM MLLLT3 KD

Potency assay:

Homogeneous Time Resolved Fluorescence assay, Biolayer Interferometry assay, ITC

Off target activity

Probe Selectivity in Vitro:

IC50 >40 uM against YEATS2/4. PFI-6 is universally inactive in the SGC Bromodomain panel.

Outside target family: PFI-6 showed no activity in an Invitrogen panel of 40 kinases (screening conducted at 10 µM). PFI-6 showed no activity in a panel of 25 PDEs, ion channels and GPCRs >50µM.

In cell validation

On target activity in cells

Potency in cells:

IC50

760 nM

Potency assay (cells):

Fluorescence Recovery After Photobleaching (FRAP) assay

Target engagement assay (cells):

Fluorescence Recovery After Photobleaching (FRAP) assay

Primary Reference

Reference (doi):

10.1101/2021.02.08.430291

External Resources

Available data:

SGC Chemical Probes

PFI-6

Probe Information

Target Details

ENL; LTG19; YEATS1; AF9; YEATS3

Probe Details

Physico-chemical properties

In vitro validation

In cell validation

Primary Reference

External Resources

Supporting Organizations

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PFI-6

Probe Information

Target Details

ENL; LTG19; YEATS1; AF9; YEATS3

Probe Details

Physico-chemical properties

In vitro validation

In cell validation

Primary Reference

External Resources

Supporting Organizations

Interested in supporting the portal?