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SU6656
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SU6656图片
CAS NO:330161-87-0
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)371.45
FormulaC19H21N3O3S
CAS No.330161-87-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 74 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)10% DMSO+dd H2O: 16 mg/mL
Synonyms

SU 6656; SU-6656; SU6656;

Chemical Name: (Z)-N,N-dimethyl-2-oxo-3-((4,5,6,7-tetrahydro-1H-indol-2-yl)methylene)indoline-5-sulfonamide

InChi Key: LOGJQOUIVKBFGH-YBEGLDIGSA-N

InChi Code: InChI=1S/C19H21N3O3S/c1-22(2)26(24,25)14-7-8-18-15(11-14)16(19(23)21-18)10-13-9-12-5-3-4-6-17(12)20-13/h7-11,20H,3-6H2,1-2H3,(H,21,23)/b16-10-

SMILES Code: O=S(C1=CC2=C(NC(/C2=C\C(N3)=CC4=C3CCCC4)=O)C=C1)(N(C)C)=O

实验参考方法
In Vitro

In vitro activity: 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. Pretreating Jurkat T-cells with SU 6656 leads to increased VSV-G luciferase activity. 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.


Kinase Assay: 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 Assay: 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.

In VivoSU 6656 markedly and dose-dependently attenuates mecamylamine-induced experimental nicotine withdrawal syndrome in mice measured in terms of WSS and anxiety score. 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.
Animal modelInbred Swiss albino male mice
Formulation & Dosage10% DMSO in water; 1.5, 3, and 6 mg/kg; i.p. injection
References

Mol Cell Biol. 2000 Dec;20(23):9018-27; Nicotine Tob Res. 2012 Apr;14(4):407-14.

生物活性


Effect of SU6656 on tyrosine phosphorylation. Mol Cell Biol.2000 Dec;20(23):9018-27.



SU6656 inhibits PDGF-stimulated c-Myc induction. Mol Cell Biol. 2000 Dec;20(23):9018-27.


Effects of PP2, SU6656, and SU6657.



Inhibition of PDGF-stimulated NIH 3T3 cell DNA synthesis. Mol Cell Biol. 2000 Dec;20(23):9018-27.