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T-26c

Protein target name:
MMP13Mechanism of action:
InhibitorRecommended Concentration for use in cells:
10-100 nM
Probe Information
In vitro validation
Potency:
IC500.0069 nM
Potency assay:
Inhibition of the human MMP13 catalytic domainPDB ID for probe-target interaction (3D structure):
3WV1Potency (off target):
IC50Off target protein and potency:
MMP2: 18 nM, MMP10: 160 nMMMP3: 600 nM, MMP8: 780 nMPotency assay (off target):
MMP1, MMP7, MMP9, MMP14, TACE > 10,000 nMIn cell validation
Potency assay (cells):
In nasal septum cartilage explants (bovine), T-26c inhibited cytokine-induced collagen degradation by MMPs (87.4% inhibition at 0.1 uM).In vivo validation
Organism:
Guinea pig (male)Dose:
10 mg/kg (oral); 1 mg/kg (IV)Route of delivery:
OralIntravenousSystemic clearance:
431 mL/h/kg (IV)Fraction of probe bound to plasma protein:
0.28Cmax:
911 ng/mL (oral)Tmax:
.83 h (oral)Primary Reference
Reference (PMID):
25192810External Resources
Available data:
SGC Chemical Probes