SU6656

Protein target name:

SRC, YES1, LYN, FYN

Mechanism of action:

ATP Competitive Inhibitor

Recommended Concentration for use in cells:

up to 2 uM

Probe Availability

Probe Information

Target and Probe Information

Target Details

Target class:

Protein kinase

Subclass:

HUGO ID:

HGNC:11283 HGNC:12841 HGNC:6735 HGNC:4037

Entrez gene ID:

6714 7525 4067 2534

UNIPROT ID:

P12931 P07947 P07948 P06241

Target alias:

ASV; SRC1; THC6; c-SRC; p60-Src; Yes; c-yes; HsT441; P61-YES; JTK8; p53Lyn; p56Lyn; SLK; SYN; p59-FYN

Probe Details

Chemical Probes Portal ID:

CPP1227

Probe alias:

Su6656; SU 6656; SU-6656; K88

PubChem CID:

5312137

ChEMBL ID:

CHEMBL605003

SMILES string:

CN(C)S(=O)(=O)C1=CC\2=C(C=C1)NC(=O)/C2=C\C3=CC4=C(N3)CCCC4

InChi Key:

LOGJQOUIVKBFGH-YBEGLDIGSA-N

Orthogonal probe:

eCF506

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50

280 nM SRC170 nM FYN20 nM YES1130 nM LYN

Potency assay:

Biochemical Kinase Assay

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

2WEL

Structure-activity relationship:

Off target activity

Probe Selectivity in Vitro:

SU6656 does not inhibit the PDGF receptor and exhibited greater-than-6.5-fold selectivity for Src relative to several other kinases tested (Csk, Frk, Abl, FGFR1, IGF1R, Lck, Met).

In cell validation

On target activity in cells

Potency in cells:

% inh

49-100%

Potency assay (cells):

Inhibition PDGF-stimulated c-Myc induction, Inhibition of PDGF-stimulated NIH 3T3 cell DNA synthesis, Immunoblots (enolase phosphorylation), morphological assay using Src-transformed NIH 3T3 cells (podosome rosettes)

In vivo validation

Organism:

Swiss albino male mice

Dose:

2-4 mg?kg

Route of delivery:

Intraperitoneal

Primary Reference

Reference (doi):

10.1128/mcb.20.23.9018-9027.2000 10.3109/00207454.2013.879869

Reference (PMID):

11074000 24397498

SU6656

Probe Availability

Probe Information

Target Details

ASV; SRC1; THC6; c-SRC; p60-Src; Yes; c-yes; HsT441; P61-YES; JTK8; p53Lyn; p56Lyn; SLK; SYN; p59-FYN

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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SU6656

Probe Availability

Probe Information

Target Details

ASV; SRC1; THC6; c-SRC; p60-Src; Yes; c-yes; HsT441; P61-YES; JTK8; p53Lyn; p56Lyn; SLK; SYN; p59-FYN

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?