1G244

Protein target name:

DPP8, DPP9

Mechanism of action:

Inhibitor

Recommended Concentration for use in cells:

up to 8 uM, shows unspecific off-target toxicity at higher concentrations

Probe Availability

MedChemExpress

Probe Information

Target and Probe Information

Target Details

Target class:

DP8; DPRP1; DPRP-1; MST097; MSTP097; MSTP135; MSTP141; DP9; DPLP9; DPRP2; DPP IX; DPRP-2

Probe Details

Chemical Probes Portal ID:

CPP2300

Probe alias:

9XH, cpd 1

PubChem CID:

56658139

ChEMBL ID:

CHEMBL1814633

SMILES string:

N[C@@H](CC(=O)N1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)C(=O)N1Cc2ccccc2C1

InChi Key:

ZKIQFLSGMMYCGS-SANMLTNESA-N

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50, Ki

14 nM DPP8, 53 nM DPP9 (IC50)0.9 nM DPP8, 4.2 nM DPP9 (Ki)

Potency assay:

Enzymatic assay

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

6TRX, 6EOR

Off target activity

Probe Selectivity in Vitro:

Selective over: DPP4 >100,000, FAP >100,000, DPP2 >100,000

In cell validation

On target activity in cells

Potency in cells:

IC50

320 nM

Potency assay (cells):

DPP activity assay in lysate after exposure of intact cells to 1G244

Toxicity

Cytoxicity assay:

Yes

Notes on cytotoxicity:

1G244 shows minimal cytotoxicity against several mammalian cancer cell lines, with CC50 (cytotoxic concentration) values well over 20 μM.

In vivo validation

Organism:

Rat

Dose:

1, 10, 30 mg/Kg1.1 (IV), 2.2 (PO) mg/Kg

Route of delivery:

OralIntravenous

Plasma half life:

7 (IV), 1 (PO) h

Systemic clearance:

23.4 (IV) ml/min/Kg

Cmax:

0.2 nmol/ml (PO)

Vss:

3.2 (IV) L/Kg

AUC:

1.6 (IV), 0.5 (PO) nmol/(mL*h)

Bioavailability:

16.5 % (PO)

Primary Reference

Reference (doi):

10.1039/C5MD00454C 10.1016/j.bcp.2009.03.032 10.1038/nchembio.2229

Reference (PMID):

19439267 27820798

1G244

Probe Availability

Probe Information

Target Details

DP8; DPRP1; DPRP-1; MST097; MSTP097; MSTP135; MSTP141; DP9; DPLP9; DPRP2; DPP IX; DPRP-2

Probe Details

In vitro validation

In cell validation

Toxicity

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?

Search form

1G244

Probe Availability

Probe Information

Target Details

DP8; DPRP1; DPRP-1; MST097; MSTP097; MSTP135; MSTP141; DP9; DPLP9; DPRP2; DPP IX; DPRP-2

Probe Details

In vitro validation

In cell validation

Toxicity

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?