PFI-6

Inhibitor of MLLT1, MLLT3

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe PFI-6 is in the process of SERP review.

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Information

MLLT1
MLLT3

Inhibitor

up to 1 uM

DOI - 10.1101/2021.02.08.430291

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q03111

Target Class: Epigenetic

Target SubClass: YEATS

Potency: IC 50

Potency Value: 140 nM

Potency Assay: Homogeneous Time-Resolved Fluorescence assay, Biolayer Interferometry assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Protein ENL, YEATS1, LTG19, ENL, MLLT1, ENL_HUMAN, ...

DOI Reference: 10.1101/2021.02.08.430291

Uniprot ID: Q03111

Target Class: Epigenetic

Target SubClass: YEATS

Potency: Kd

Potency Value: 82 nM

Potency Assay: ITC

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Protein ENL, YEATS1, LTG19, ENL, MLLT1, ENL_HUMAN, ...

DOI Reference: 10.1101/2021.02.08.430291

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

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.

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

Presented potency data at the level <0.2 uM seem to be sufficient to support the application of compound PFI-6 as chemical probe for MLLT1/3. However, the side-by-side comparison with the negative control PFI-6N is recommended. The in vivo and toxicity data were not provided therefore application of PFI-6 in an in vivo setting is currently not recommended.

(last updated: 22 Mar 2023 )