TP-060

TP-060 : Allosteric inhibitor of UGCG

Structure

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Probe TP-060 is in the process of SERP review.

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Information

UGCG

Allosteric

up to 1 uM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q16739

Target Class: Enzyme

Target SubClass: Glycosyltransferase

Potency: IC50

Potency Value: 31 nM

Potency Assay: Enzymatic assay

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

Target aliases:

Ceramide glucosyltransferase, UGCG, CEGT_HUMAN, GC ...

DOI Reference: 10.1021/acs.jmedchem.1c02078

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): In house kinase panel (342 kinases at 1 µM): clean SAFETYscan (DiscoverX (Eurofins) 47 targets at 10 µM): 44 target > 10 µM; HTR1B HTR1B (EC50 = 2.8 μM), nAChR(a4/b2) Blocker (CHRNA4) (IC50 = 6.5 μM), SLC6A4 (IC50 = 0.31 μM)

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In Cell Rating

(last updated: 10 Oct 2023 )