|N,N-二甲基-2-氧代-3-[(4,5,6,7-四氢-1H-吲哚-2-基)亚甲基]-1H-吲哚-5-磺酰胺|CsnPharm

CAS No.: 330161-87-0

SU6656/2,3-二氢-N，N-二甲基-2-氧代-3-[(4,5,6,7-四氢-1H-吲哚-2-基)亚甲基] -1H-吲哚-5-磺酰胺 Catalog No. CSN18218

SU 6656 is an inhibitor of Src kinases and can target Src, Yes, Lyn, and Fyn with IC50 of 280 nM, 20 nM, 130 nM, 170 nM, respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Lyn

IC50:130nM Fyn

IC50:170nM Yes

IC50:20nM Src

IC50:280nM
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
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
Sf9 insect cells - Function assay - Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells, IC50=0.77 μM 20117004
参考文献

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6921 mL
- 13.4606 mL
- 26.9213 mL
- 5 mM
- 0.5384 mL
- 2.6921 mL
- 5.3843 mL
- 10 mM
- 0.2692 mL
- 1.3461 mL
- 2.6921 mL

技术信息

CAS号

330161-87-0

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H21N3O3S

运输

蓝冰

分子量

371.45

别名

溶解度

DMSO	72.0 mg/mL (193.8 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

10% DMSO+dd water

16 mg/mL

大规格询价

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靶点	Description	IC50
Lyn		IC50:130nM
Fyn		IC50:170nM
Yes		IC50:20nM
Src		IC50:280nM

SU6656/2,3-二氢-N，N-二甲基-2-氧代-3-[(4,5,6,7-四氢-1H-吲哚-2-基)亚甲基] -1H-吲哚-5-磺酰胺 Catalog No. CSN18218

靶点选择性

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