| 名稱 | SU6656 |
| 描述 | 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. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 在NIH 3T3細(xì)胞中，SU 6656以0.3-0.4 μM的IC50抑制了PDGF激活的S期啟動。SU 6656還能抑制PDGF和血清介導(dǎo)的NIH 3T3細(xì)胞增殖，以及表皮生長因子和集落刺激因子1（colony-stimulating factor 1）激活的正常及集落刺激因子1受體轉(zhuǎn)染NIH 3T3細(xì)胞的DNA合成。SU6656阻斷了PDGF激活的c-Myc誘導(dǎo)和ERK2激活。[1] 在Jurkat T細(xì)胞中預(yù)處理SU 6656能夠增加VSV-G熒光素酶活性。[2] SU 6656抑制TGF-β促進(jìn)的近端上皮HKC-8細(xì)胞內(nèi)CTGF mRNA和蛋白的上調(diào)，也減少了自分泌生長因子暴露細(xì)胞中的CTGF表達(dá)。SU 6656干擾Aurora激酶活性，導(dǎo)致細(xì)胞分裂受阻和多葉核的形成。[3] |
| 體內(nèi)活性 | SU 6656 顯著且劑量依賴性地減輕了小鼠中由美卡明引起的實(shí)驗(yàn)性尼古丁撤斷綜合征。[4] 每日一次給藥（1.5、3、6 mg/kg, i.p.）顯著且劑量依賴性地減輕了納洛酮引起的嗎啡撤斷綜合征。[5] |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 69 mg/mL (185.8 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| 關(guān)鍵字 | PTK2 protein tyrosine kinase 2 | SU-6656 | Focal adhesion kinase | FAK | Akt | PTK2 | SU 6656 | Inhibitor | Protein kinase B | Src | PKB | SU6656 | inhibit |
| 相關(guān)產(chǎn)品 | Honokiol | Capivasertib | AKT Kinase Inhibitor | Artemisinin | Staurosporine | Nintedanib | Dasatinib | 2,3-Butanediol | Defactinib | Oridonin | Ethyl gallate | Ibrutinib |
| 相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 激酶抑制劑庫 | 抗衰老化合物庫 | 細(xì)胞骨架化合物庫 | 抗卵巢癌化合物庫 | NO PAINS 化合物庫 | 酪氨酸激酶分子庫 | PI3K/Akt/mTOR 化合物庫 |