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SU6656

Catalog No. T6997   CAS 330161-87-0

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

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SU6656 Chemical Structure
SU6656, CAS 330161-87-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 47.00
5 mg In stock $ 77.00
10 mg In stock $ 142.00
25 mg In stock $ 283.00
50 mg In stock $ 473.00
100 mg In stock $ 702.00
1 mL * 10 mM (in DMSO) In stock $ 81.00
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Purity: 98.21%
Purity: 97%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SU 6656 is a selective inhibitor of Src family kinases, with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.
Targets&IC50 YES:20 nM, Fyn:170 nM, Lyn:130 nM, Src:280 nM
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]
In vivo SU 6656 markedly and dose-dependently attenuates mecamylamine-induced experimental nicotine withdrawal syndrome in mice measured in terms of WSS and anxiety score.[4] Once-daily administration of SU 6656 (1.5, 3, and 6 mg/kg, i.p.) markedly and dose-dependently attenuates the naloxone-induced morphine withdrawal syndrome.[5]
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 ?nal 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 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 ?eld pictures of cells are recorded by Olympus CK40 microscope using Leica DC Viewer software.(Only for Reference)
Molecular Weight 371.45
Formula C19H21N3O3S
CAS No. 330161-87-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 69 mg/mL (185.8 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Blake RA, et al. Mol Cell Biol. 2000, 20(23), 9018-9027. 2. McCarthy SD, et al. J Acquir Immune Defic Syndr.2014, 66(2), 118-126. 3. Cicha I, et al. Int J Biochem Cell Biol. 2014 Jan;46:39-48. 4. Rehni AK, et al. Nicotine Tob Res. 2012, 14(4), 407-414. 5. Rehni AK, et al. Behav Pharmacol. 2011, 22(2), doi: 10.1097/FBP.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Pancreatic Cancer Compound Library Bioactive Lipid Compound Library NO PAINS Compound Library Anti-Breast Cancer Compound Library Anti-Liver Cancer Compound Library Anti-Prostate Cancer Compound Library Neural Regeneration Compound Library

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Keywords

SU6656 330161-87-0 Angiogenesis Cytoskeletal Signaling PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors Src Akt FAK PTK2 protein tyrosine kinase 2 SU-6656 Focal adhesion kinase PTK2 SU 6656 Inhibitor Protein kinase B PKB inhibit inhibitor

 

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