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TP-060

2D structure
Target UGCG 
Mode of action Allosteric inhibitor (Noncompetitive against UDP-glucose)
Control TP-060n
Recommended cellular usage concentration ≤ 1 µM
In vivo use yes
Synonyms T-036, Glucosylceramide synthase-IN-1
Donated by Takeda


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: IC50 = 31 nM (GCS enzymatic assay)
Selectivity within target family: > 30-fold Not tested: Presumably high selectivity according to the allosteric binding mode.
Selectivity outside target family 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)
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: Cellular GlcCer reduction: EC50 = 7.6 nM
Control compound (100 times less potent than the probe) TP-060n: IC50 > 100 µM (GCS enzymatic assay); EC50 > 10 µM (cellular GlcCer reduction)