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C3TD879

2D structure
Target CIT 
Targeted domain Kinase domain (active site)
Mode of action Inhibitor (type 1, ATP competitive)
Control C3TD879-N
Recommended cellular usage concentration ≤ 2 µM
In vivo use Yes
Synonyms C3TD-879, GTPL13171
Donated by Center for Therapeutics Discovery, Cleveland Clinic


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: CIT: IC50 = 12 nM (n=5, Eurofins Radiometric Activity Assay GST-CITKKD)
DSF CITKKD-c006 (E. coli dephosphorylated): deltaTm = +2.1°C; DSF CITKKD-c014 (Sf9 hyperphosphorylated): deltaTm = +2.1°C (KD: kinase domain)
Selectivity within target family: > 30-fold Eurofins KinomeScan at 1 µM: > 75-fold selectivity over every human kinase except AAK1 (17-fold) (IC50 [nM]): AAK1 (212), BMP2K (BIKE) (902), MKNK2 (2180), HIPK4 (2275)
NanoBRET IC50 [µM]: AAK1 (6.2), others > 10 µM
Selectivity outside target family Not tested
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: Promega NanoBRET: CIT (full-length) (IC50 = 51 nM); NanoLuc NanoBRET Kd [nM]: CITKD (0.3 ± 0.2, n=2); CIT (9.5 ± 0.5; n=2)
No phenocopy of CIT knockdown in functional assays despite potent target engagement
Control compound (100 times less potent than the probe) C3TD879-N: CIT (IC50 > 30 µM; n=1, Eurofins Radiometric Activity Assay GST-CITKD)
DSF CITKD-c006 (E. coli dephosphorylated): deltaTm = -0.2°C; DSF CITKD-c014 (Sf9 hyperphosphorylated): deltaTm = -0.3°C
No binding in NanoBRET