SU6656

SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

SU6656 Chemical Structure

SU6656 Chemical Structure

CAS No. 330161-87-0

Purity & Quality Control

SU6656 Related Products

Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 insect cells Function assay Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells, IC50=0.77 μM 20117004
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Biological Activity

Description SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.
Targets
YES [1] Lyn [1] Fyn [1] Src [1]
20 nM 130 nM 170 nM 280 nM
In vitro
In vitro

In NIH 3T3 cells, SU 6656 inhibits the PDGF-stimulated S-phase induction with IC50 of 0.3-0.4 μM. SU 6656 also inhibits PDGF- and serum-mediated NIH 3T3 cell proliferation, as well as epidermal growth factor and colony-stimulating factor 1-stimulated DNA synthesis in normal and colony-stimulating factor 1 receptor transfected NIH 3T3 cells. SU6656 inhibits PDGF-stimulated c-Myc induction and ERK2 activation.[1] Pretreating Jurkat T-cells with SU 6656 leads to increased VSV-G luciferase activity.[2] SU 6656 impairs TGF-β-mediated upregulation of CTGF mRNA and protein in proximal epithelial HKC-8 cells, and also reduces CTGF expression in cells exposed to autocrine growth factors. SU 6656 interferes with Aurora kinase activity resulting in inhibition of cell division and formation multilobular nuclei.[3]

Kinase Assay Biochemical kinase assays for IC50 determination and kinetic studies
IC50 measurements are made using poly-Glu–Tyr (4:1), or, in the case of Lck, poly-Lys–Tyr (4:1) as a peptide substrate. The divalent cation is 20 mM MgCl2 (in the case of Src, Fyn, Yes, Lyn, Csk, Frk, or Abl) or 10 mM MnCl2 (in the case of FGFR1, IGF1R, Lck, or Met). The final ATP concentrations are as follows: Src, 10 μM; Fyn, 6 μM; Yes, 100 μM; Lyn, 2 μM; Csk, 10 μM; Frk, 10 μM; Abl, 4 μM; FGFR1, 10 μM; IGF1R, 2 μM; Lck, 2 μM; Met, 5 μM; PDGFR, 6 μM. IC50 measurements of PDGFRb autophosphorylation are determined on immunoprecipitated PDGFRb. Km values are calculated using the Eadie-Hofstee method.
Cell Research Cell lines HKC-8 cells
Concentrations 5 μM
Incubation Time 48 h
Method

HKC-8 cells are seeded at different cells densities (10,000 cells/cm2 and 50,000 cells/cm2) and cultured in the presence or absence of SU 6656 for 24 and 48 h. Bright field pictures of cells are recorded by Olympus CK40 microscope using Leica DC Viewer software.

Experimental Result Images Methods Biomarkers Images PMID
Western blot phospho-c-Abl / c-Abl / phospho-c-Src / c-Src p-p38 / p38 / p-CREB / CREB p-STAT3 / STAT3 23049975
Immunofluorescence E-cadherin / Fibronectin p-p38 23246962
In Vivo
In vivo

SU 6656 markedly and dose-dependently attenuates -induced experimental nicotine withdrawal syndrome in mice measured in terms of WSS and anxiety score.[4]

Animal Research Animal Models Inbred Swiss albino male mice
Dosages 3 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 371.45 Formula

C19H21N3O3S

CAS No. 330161-87-0 SDF Download SU6656 SDF
Smiles CN(C)S(=O)(=O)C1=CC2=C(C=C1)NC(=O)C2=CC3=CC4=C(N3)CCCC4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 74 mg/mL ( (199.21 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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