SU6656 |
Catalog No.GC17500
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Chemical Name | (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 | ||
| Formula | C19H21N3O3S | M.Wt | 371.45 |
| Solubility | ≥ 18.55mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)