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SU6656 {[allProObj[0].p_purity_real_show]}

货号:A742025

SU6656是一种Src家族激酶的抑制剂,对SrcYesLynFynIC50值分别为280、20、130和170 nM。它抑制FAK在Y576/577、Y925和Y861位点的磷酸化以及p-AKT

SU6656 化学结构 CAS号:330161-87-0
SU6656 化学结构
CAS号:330161-87-0
SU6656 3D分子结构
CAS号:330161-87-0
SU6656 化学结构 CAS号:330161-87-0
SU6656 3D分子结构 CAS号:330161-87-0
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SU6656 纯度/质量文件 产品仅供科研

货号:A742025 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 FAK 其他靶点 纯度
Defactinib 99%+
NVP-TAE 226 ++

PYK2, IC50: 3.5 nM

FAK, IC50: 5.5 nM

Insulin Receptor,IGF-1R 98+%
PF-573228 +

FAK, IC50: 4 nM

99% (HPLC)
Solanesol 90% +(HPLC)
PF-431396 ++

PYK2, IC50: 11 nM

FAK, IC50: 2 nM

99%+
PND-1186 ++++

FAK, IC50: 1.5 nM

99%+
PF-562271 ++++

PYK2, IC50: 13 nM

FAK, IC50: 1.5 nM

99%+
GSK2256098 ++++

FAK, Ki: 0.4 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Akt Akt1 Akt2 Akt3 其他靶点 纯度
Honokiol MEK 98%
PF-04691502 ++++

P-Akt (T308), IC50: 7.5 nM

P-Akt (S473), IC50: 3.8 nM

98+%
PHT-427 +

Akt, Ki: 2.7 μM

99%+
Deguelin PI3K 99%+
TIC10 isomer ERK 98+%
Perifosine +

Akt, IC50: 4.7 μM

98%
Miltefosine PKC,PI3K 98%
Triciribine +

Akt, IC50: 130 nM

99%+
Uprosertib +

Akt1, IC50: 180 nM

+

Akt2, IC50: 328 nM

++

Akt3, IC50: 38 nM

99%+
Afuresertib ++++

Akt1, Ki: 0.08 nM

++++

Akt2, Ki: 2 nM

++++

Akt3, Ki: 2.6 nM

99%+
Miransertib ++++

Akt1, IC50: 5 nM

++++

Akt2, IC50: 4.5 nM

++

Akt3, IC50: 16 nM

98+%
GSK-690693 ++++

Akt1, IC50: 2 nM

+++

Akt2, IC50: 13 nM

+++

Akt3, IC50: 9 nM

99%+
AT7867 ++

Akt1, IC50: 32 nM

++

Akt2, IC50: 17 nM

++

Akt3, IC50: 47 nM

PKA 99%+
AKT inhibitor VIII ++

Akt1, IC50: 58 nM

+

Akt2, IC50: 210 nM

+

Akt3, IC50: 2119 nM

97%
MK-2206 2HCl +++

Akt1, IC50: 8 nM

+++

Akt2, IC50: 12 nM

+

Akt3, IC50: 65 nM

99%+
Ipatasertib ++++

Akt1, IC50: 5 nM

++

Akt2, IC50: 18 nM

+++

Akt3, IC50: 8 nM

99%+
AT13148 ++

Akt1, IC50: 38 nM

+

Akt2, IC50: 402 nM

++

Akt3, IC50: 50 nM

PKA 95%
Capivasertib ++++

Akt1, IC50: 3 nM

+++

Akt2, IC50: 8 nM

+++

Akt3, IC50: 8 nM

99%+
A-674563 HCl +++

Akt1, Ki: 11 nM

PKA 99%
CCT128930 +++

Akt2, IC50: 6 nM

PKA 95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Fyn Lck Lyn Src Yes 其他靶点 纯度
Saracatinib ++

Fyn, IC50: 10 nM

++++

LCK, IC50: <4 nM

+++

Lyn, IC50: 5 nM

++++

c-Src, IC50: 2.7 nM

99%+
SU6656 +

Fyn, IC50: 170 nM

+

Lyn, IC50: 130 nM

+

Src, IC50: 280 nM

++

YES, IC50: 20 nM

98%
PP1 +++

Fyn, IC50: 6 nM

+++

LCK, IC50: 5 nM

EGFR 99%+
PP2 +++

Fyn, IC50: 5 nM

++++

LCK, IC50: 4 nM

98%
WH-4-023 ++++

Lck, IC50: 2 nM

+++

Src, IC50: 6 nM

99%+
NVP-BHG 712 +

c-Src, IC50: 1.266 μM

99%+
CCT196969 ++

LCK, IC50: 0.02 μM

+

Src, IC50: 0.03 μM

98%
MNS +

Src, IC50: 29.3 μM

p97,Syk 98%
Tirbanibulin ++

Src (Hep 3B), GI50: 26 nM

Src (HuH7), GI50: 13 nM

99%+
PP121 ++

Src, IC50: 14 nM

VEGFR,PDGFR 99%+
Bosutinib ++++

Src, IC50: 1.2 nM

99%
Dasatinib monohydrate ++++

Src, IC50: 0.8 nM

98%
Quercetin Sirtuin,PKC 97%
Dasatinib ++++

Src, IC50: 0.8 nM

98%
Repotrectinib +++

Src, IC50: 5.3 nM

99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

SU6656 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].

SU6656 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

SU6656 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.

SU6656 实验方案

计算器
存储液制备 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

SU6656 技术信息

CAS号330161-87-0
分子式C19H21N3O3S
分子量 371.45
SMILES Code O=S(C1=CC2=C(NC(/C2=C\C(N3)=CC4=C3CCCC4)=O)C=C1)(N(C)C)=O
MDL No. MFCD10565928
别名
运输蓝冰
InChI Key LOGJQOUIVKBFGH-YBEGLDIGSA-N
Pubchem ID 5312137
存储条件

In solvent -20°C:3-6个月-80°C:12个月

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

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
动物实验配方

10% DMSO+dd water 16 mg/mL

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