LSN-3213128

Inhibitor of ATIC

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe LSN-3213128 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

ATIC

Inhibitor

up to 200 nM

More...

Probe Availability:

In Vitro Validations

Uniprot ID: P31939

Target Class: Other

Target SubClass: formyltransferase and cyclohydrolase

Potency: IC50

Potency Value: 16 ± 11 nM

Potency Assay: Enzymatic Assay

PDB ID for probe-target interaction (3D structure): 5UZ0

Structure-activity relationship: yes

Target aliases:

Bifunctional purine biosynthesis protein ATIC, PUR ...

DOI Reference: 10.1021/acs.jmedchem.7b01046

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Enzymatic Assay, Eurofins

Probe Selectivity in Vitro:

Selective for AICARFT with IC50s >100 μM against TS, SHMT1, MTHFD1, MTHFD2 and MTHFD2L. The compound has been profiled in a panel of protein kinase assays at CEREP Panlabs (Eurofins) and has no significant protein kinase activity.

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Concentration note: The compound is a straightforward competitive inhibitor. So the inhibitory effect of the compound greatly differs depending on the cellular folate concentration.

(last updated: 4 Aug 2021 )