SU6656
目录号 : GC17500
SU6656是一种小分子吲哚酮类化合物，可选择性抑制Src、Yes和Fyn激酶活性，IC50值分别为0.28μM、0.02μM和0.17μM。
Cas No.:330161-87-0
Sample solution is provided at 25 µL, 10mM.
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SU6656 is a small-molecule indolinone that selectively inhibits Src, Yes, and Fyn at IC50 values of 0.28μM, 0.02μM, and 0.17μM, respectively [1]. SU6656 activated AMPK and increased the phosphorylation at Thr172, and inhibited the phosphorylation of Erk1/2[2]. SU6656 has been widely used to regulate insulin secretion in different species[3].
In vitro, SU6656 treatment for 72 hours significantly inhibited BaF3 cell proliferation with an IC50 value of 0.18µM[4]. Treatment with 100μM SU6656 for 72h significantly inhibited FRO cell viability and resulted in increased p21 protein levels in the cells[5]. Treatment with 5μM SU6656 for 72h resulted in a significant increase in both nuclear and cytoplasmic volumes of B lymphoma cells[6].
In vivo, SU6656 treatment (25mg/kg; every other day for 12 weeks; i.p.) significantly increased total body, tibial, and lumbar Bone mineral density (BMD) in skeletally mature mice, without affecting body weight[7]. Intraperitoneal injection of SU6656 at a dose of 3 mg/kg/ day for 20 consecutive days alleviated fibrosis and improved lung function in a silicosis mouse model[8].
References:
[1] Blake R A, Broome M A, Liu X, et al. SU6656, a selective src family kinase inhibitor, used to probe growth factor signaling[J]. Molecular and cellular biology, 2000, 20(23): 9018-9027.
[2] Ross F A, Hawley S A, Auciello F R, et al. Mechanisms of paradoxical activation of AMPK by the kinase inhibitors SU6656 and sorafenib[J]. Cell chemical biology, 2017, 24(7): 813-824. e4.
[3] Cheng H, Straub S G, Sharp G W G. Inhibitory role of Src family tyrosine kinases on Ca2+-dependent insulin release[J]. American Journal of Physiology-Endocrinology and Metabolism, 2007, 292(3): E845-E852.
[4] Mologni L, Rostagno R, Brussolo S, et al. Synthesis, structure–activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors[J]. Bioorganic & medicinal chemistry, 2010, 18(4): 1482-1496.
[5] Kim S H, Kang J G, Kim C S, et al. Inhibition of p21 and Akt potentiates SU6656-induced caspase-independent cell death in FRO anaplastic thyroid carcinoma cells[J]. Hormone and Metabolic Research, 2013, 45(06): 408-414.
[6] Dussault N, Simard C, Néron S, et al. Human B lymphocytes and non-Hodgkin's lymphoma cells become polyploid in response to the protein kinase inhibitor SU6656[J]. Blood Cells, Molecules, and Diseases, 2007, 39(1): 130-134.
[7] Thouverey C, Ferrari S, Caverzasio J. Selective inhibition of Src family kinases by SU6656 increases bone mass by uncoupling bone formation from resorption in mice[J]. Bone, 2018, 113: 95-104.
[8] Hao X, Jin Y, Zhang Y, et al. Inhibition of oncogenic src ameliorates silica-induced pulmonary fibrosis via PI3K/AKT pathway[J]. International Journal of Molecular Sciences, 2023, 24(1): 774.
SU6656是一种小分子吲哚酮类化合物，可选择性抑制Src、Yes和Fyn激酶活性，IC50值分别为0.28μM、0.02μM和0.17μM[1]。SU6656能激活AMPK并促进Thr172位点磷酸化，同时抑制Erk1/2的磷酸化[2]。SU6656已广泛应用于不同物种的胰岛素分泌调控研究[3]。
在体外，SU6656处理72小时可显著抑制BaF3细胞增殖，IC50值为0.18µM[4]。使用100μM的SU6656处理FRO细胞72小时，能显著抑制细胞活力并提高细胞内p21蛋白水平[5]。用5μM的SU6656处理B淋巴瘤细胞72小时，可显著增加细胞核与细胞质体积 [6]。
在体内，隔天腹腔注射25mg/kg剂量的SU6656连续12周，能显著增加骨骼成熟小鼠的全身、胫骨和腰椎骨密度(BMD)，且不影响体重[7]。连续20天每日腹腔注射3mg/kg/day剂量的SU6656，可减轻硅肺病小鼠模型的纤维化程度并改善肺功能[8]。
| Cell experiment [1]: | |
Cell lines | FRO cells |
Preparation Method | FRO cells were cultured in RPMI 1640 medium supplemented with 10% heat-inactivated fetal bovine serum (FBS) and 1% streptomycin/penicillin at 37°C and 5% CO2. Cells (5×103 cells /100μl) were seeded in 96-well plates and, after overnight culture, treated with 10, 20, 50, and 100μM SU6656 for 24, 48, and 72 hours. CCK-8 reagent was added, and the cells were cultured at 37°C for 4 hours, and the absorbance was measured at a wavelength of 450nm. |
Reaction Conditions | 10, 20, 50, and 100μM; 24, 48, and 72h |
Applications | SU6656 treatment significantly inhibited the cell viability of FRO cells in a concentration- and time-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female C57BL/6J mice |
Preparation Method | Twelve 4-month-old female C57BL/6J mice were randomly divided into two groups and received intraperitoneal injections of SU6656 (25mg/kg) or an equal volume of control solution (20% dimethyl sulfoxide-DMSO, 20% polyethylene glycol 400, 60% sodium chloride) every other day for 12 weeks (6 mice per group). During the adaptation period (6 weeks) and the duration of the experiment, mice were housed under standard non-barrier conditions with a 12h/12h light/dark cycle and had AD libitum access to RM3 mouse diet and water containing 1.24% Ca and 0.56% available phosphorus. Bone mineral density (BMD) of the whole body, tibia, and lumbar spine was analyzed. |
Dosage form | 25mg/kg; every other day for 12 weeks; i.p. |
Applications | SU6656 treatment significantly increased total body, tibial, and lumbar BMD in skeletally mature mice, without affecting body weight. |
References: | |
| Cas No. | 330161-87-0 | SDF | |
| 化学名 | (Z)-2-hydroxy-N,N-dimethyl-3-((4,5,6,7-tetrahydro-1H-indol-2-yl)methylene)-3H-indole-5-sulfonamide | ||
| Canonical SMILES | CN(S(C1=CC(/C(C(O)=N2)=C([H])/C(N3)=CC4=C3CCCC4)=C2C=C1)(=O)=O)C | ||
| 分子式 | C19H21N3O3S | 分子量 | 371.45 |
| 溶解度 | ≥ 18.55mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6922 mL | 13.4608 mL | 26.9215 mL |
| 5 mM | 538.4 μL | 2.6922 mL | 5.3843 mL |
| 10 mM | 269.2 μL | 1.3461 mL | 2.6922 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet