GI254023X

Protein target name:

ADAM10

Mechanism of action:

Inhibitor

Recommended Concentration for use in cells:

up to 10 uM

Probe Availability

MedChemExpress

TOCRIS

Selleck Chemicals

Probe Information

Target and Probe Information

Target Details

Target class:

Other

Define other target class:

Metallopetidase

Subclass:

ADAM family

HUGO ID:

HGNC:188

Entrez gene ID:

102

UNIPROT ID:

O14672

Target alias:

RAK; kuz; AD10; AD18; MADM; CD156c; CDw156; HsT18717

Probe Details

Chemical Probes Portal ID:

CPP2382

Probe alias:

GI4023, SRI028594

PubChem CID:

9952396

ChEMBL ID:

CHEMBL1229516

SMILES string:

O=C(N[C@H](C(NC)=O)C(C)(C)C)[C@@H]([C@@H](N(C=O)O)C)CCCC1=CC=CC=C1

InChi Key:

GHVMTHKJUAOZJP-CGTJXYLNSA-N

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50

5.3 nM

Potency assay:

Enzyme inhibition assay using fluorogenic substrate

Off target activity

Potency (off target):

IC50

Probe Selectivity in Vitro:

100 fold selective over ADAM17 (541 nM):

Selectivity over other Recombinant MMPs 1 / 3 / 9 / 13 is 108 / 187 / 2.5 / 1.1 nM respectively.

In cell validation

On target activity in cells

Potency in cells:

IC50

1500 nM CX3CL1, 400 nM CXCL16, 1800 nM IL6R

Potency assay (cells):

Ability to block shedding of cell-expressed IL6R, CX3CL1 and CXCL16 (ELISA)

In vivo validation

Organism:

Mouse

Dose:

100 mg/Kg

Route of delivery:

Intraperitoneal

Primary Reference

Reference (doi):

10.2174/1386207053258488 10.1182/blood-2002-12-3775

Reference (PMID):

15777180 12714508

GI254023X

Probe Availability

Probe Information

Target Details

RAK; kuz; AD10; AD18; MADM; CD156c; CDw156; HsT18717

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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GI254023X

Probe Availability

Probe Information

Target Details

RAK; kuz; AD10; AD18; MADM; CD156c; CDw156; HsT18717

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?