SU6656是一种Src家族激酶的抑制剂,对Src、Yes、Lyn和Fyn的IC50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。
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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。 |
靶点 |
|
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 |
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 |
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 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
|
动物实验配方 |
10% DMSO+dd water 16 mg/mL |