SU6656

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Chemical Structure| 330161-87-0 同义名 : -
CAS号 : 330161-87-0
货号 : A742025
分子式 : C19H21N3O3S
纯度 : 98%
分子量 : 371.453
MDL号 : MFCD10565928
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(48.46 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

10% DMSO+dd water 16 mg/mL

生物活性
靶点

  • Fyn

    Fyn, IC50:170 nM

  • Src

    Src, IC50:280 nM

  • Yes

    YES, IC50:20 nM

  • Lyn

    Lyn, IC50:130 nM
描述 Src kinases are regulators of the expression of connective tissue growth factor (CTGF/CCN2), which plays a role in fibrotic injuries[3]. SU6656 is a small-molecule indolinone that selectively inhibits Src family kinase and induces death of cancer cells[4]. Src family protein tyrosine kinases (SFKs) inhibitor SU6656 caused proliferation abrogation as a result of the formation of cells with single multilobed nuclei and several mitotic spindle poles, features similar to polyploid megakaryocytes[5]. Four-month-old female C57Bl/6J mice received intraperitoneal injections of either 25 mg/kg SU6656 or its vehicle every other day for 12 weeks. SU6656-treated mice exhibited increased bone mineral density, cortical thickness, cancellous bone volume and trabecular thickness. SU6656 inhibited bone resorption in mice as shown by reduced osteoclast number, and diminished expressions of Oscar, Trap5b and CtsK. SU6656 did not affect Rankl or Opg expressions[6]. SU6656 reduced TNF-α-mediated paracellular permeability changes, restored occludin, p120, and E-cadherin and lowered autocrine TNF-α release. SU6656 improved the barrier properties of severe asthmatic air-liquid interface cultures[7]. Ischemic postconditioning induced neuroprotective effects were significantly attenuated by pre-treatment of selective Src Kinase inhibitors SU-6656 (4 mg/kg i.p.) and PP1 (0.2 mg/kg i.p.)[8].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
Sf9 insect cells Function assay Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells, IC50=0.77 μM 20117004
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.92mL

5.38mL

2.69mL
参考文献

[1]McCarthy SD, Jung D, et al. c-Src and Pyk2 protein tyrosine kinases play protective roles in early HIV-1 infection of CD4+ T-cell lines. J Acquir Immune Defic Syndr. 2014 Jun 1;66(2):118-26.

[2]Blake RA, Broome MA, et al. SU6656, a selective src family kinase inhibitor, used to probe growth factor signaling. Mol Cell Biol. 2000 Dec;20(23):9018-27.

[3]Iwona Cicha,et al. Dual inhibition of Src family kinases and Aurora kinases by SU6656 modulates CTGF (connective tissue growth factor) expression in an ERK-dependent manner. Int J Biochem Cell Biol. 2014 Jan;46:39-48.

[4] S H Kim,et al. Inhibition of p21 and Akt potentiates SU6656-induced caspase-independent cell death in FRO anaplastic thyroid carcinoma cells. Horm Metab Res. 2013 Jun;45(6):408-14.

[5]Nathalie Dussault,et al. Human B lymphocytes and non-Hodgkin's lymphoma cells become polyploid in response to the protein kinase inhibitor SU6656. Blood Cells Mol Dis. Jul-Aug 2007;39(1):130-4.

[6]Cyril Thouverey,et al. Selective inhibition of Src family kinases by SU6656 increases bone mass by uncoupling bone formation from resorption in mice. Bone. 2018 Aug;113:95-104.

[7]Michelle A Hardyman,et al. TNF-α-mediated bronchial barrier disruption and regulation by src-family kinase activation. J Allergy Clin Immunol.2013 Sep;132(3):665-675.e8.

[8]Kumar A, et al. Pharmacological investigations on possible role of Src kinases in neuroprotective mechanism of ischemic postconditioning in mice. Int J Neurosci. 2014 Oct;124(10):777-86.