Src
信号通路图
研究领域
抑制剂选择性比较
Src产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1021 |
DasatinibDasatinib是一种新型有效的多靶点抑制剂，作用于Abl，Src和 c-Kit，在无细胞试验中IC50分别为 <1 nM，0.8 nM 和 79 nM。 |
Antitumor activity (A)and body weight (B) relationship for BLU-285 and dasatinib in a P815 KIT D814Y mastocytoma allograft model.
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| S1006 |
Saracatinib (AZD0530)Saracatinib (AZD0530)是一种有效的Src抑制剂，无细胞试验中IC50为2.7 nM，对c-Yes， Fyn， Lyn， Blk， Fgr和Lck也具有活性；但对Abl和EGFR (L858R和L861Q)活性较低。Phase 2/3。 |
Saracatinib (AZD0530) administration alleviates provocative tumor formation conferred by LHBs exp ression. A and B, cell proliferation assay for Huh7 cells (A) and SK-Hep1 cells (B) after stable LHBs expression under treatment with saracatinib(1 μmol/L). *, P < 0.05. |
|
| S1014 |
Bosutinib (SKI-606)Bosutinib (SKI-606)是一种新型的双重Src/Abl抑制剂，在无细胞试验中IC50分别为1.2 nM 和 1 nM。 |
Both parental and HR cell lines were treated with bosutinib (0.01, 0.1, and 1 μmol/L) for 24 hours. Src-related signaling pathway molecules were then analyzed. |
|
| S2700 |
KX2-391KX2-391是第一个临床Src抑制剂(拟肽类)，靶向作用于Src的肽底物位点，在癌细胞系中GI50为9-60 nM。Phase 2。 |
The histogram represents the absolute cell numbers obtained after 15 days of culture, in the presence of KX2-391 inhibitor at different concentrations and Dasatinib, as compared to control, arbitrarily normalized to one. The data are represented as mean±SEM obtained by nine independent experiments and analyzed by Wilcoxon signed-rank test (*p < 0.05; **p < 0.005).
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| S2202 |
NVP-BHG712NVP-BHG712是一种特异性的EphB4抑制剂，ED50为25 nM，区别于对VEGFR和EphB4的抑制，对c-Raf， c-Src和c-Abl也具有抑制活性，IC50分别为0.395 μM， 1.266 μM和1.667 μM。 |
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| S5254New |
Dasatinib hydrochlorideDasatinib hydrochloride is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. |
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| S8706New |
UM-164UM-164是一种高度有效的c-Src/p38双重抑制剂，对c-Src的结合常数Kd值为2.7 nM，也能抑制p38α和p38β。 |
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| S7008 |
PP2PP2是一种Src家族激酶抑制剂，有效抑制Lck/Fyn，无细胞试验中IC50为4 nM/5 nM，作用于EGFR效果低100倍左右，对ZAP-70，JAK2和PKA没有活性。 |
Inhibition of PLCG1 phosphorylation by the silencing of DopEcR, ErGPCR, and Gq and the addition of inhibitors of RTK and Src. 5 µM SU6668 (RTK inhibitor) and 20 µM PP2 (Src inhibitor) were added to the cells for 30 min treatment before the 20E stimulation.
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| S2622 |
PP121PP121是一种作用于PDGFR， Hck， mTOR， VEGFR2， Src和Abl的多靶点抑制剂，IC50分别为2 nM， 8 nM， 10 nM， 12 nM， 14 nM和18 nM，也抑制DNA-PK，IC50为60 nM。 |
After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of PP-121 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF. |
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| S7060 |
PP1PP1是一种有效的Src选择性抑制剂，作用于Lck/Fyn时，IC50为5 nM/6 nM。 |
PP1 attenuated DAVLBH-induced lysosomal degradation of internalized VE-cadherin. HUVECs pretreated with or without PP1 were treated with or without DAVLBH for 4 h. Quantification of BV9/LAMP colocalization is shown (n = 3). The data are presented as mean ± SEM. ***P < 0.001 compared with the control group; #P < 0.05 and ###P < 0.001 compared with the DAVLBH group (one-way ANOVA with Tukey's post hoc comparison). Scale bar, 20 µm.
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| S4921 |
MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN)MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN)是一种酪氨酸激酶抑制剂，抑制Syk， Src和p97， IC50分别为2.5 μM， 29.3 μM和1.7 μM。 |
WT mouse primary macrophages were untreated as control (lane 1) or treated with 0.1μg/ml E. coli LPS (lane 5-8), 10μM E-64 (lane 2 and 6), 250μM PMSF (lane 3 and 7), or 20μM MNS (lane 4 and 8). The cells were continuously cultured for 16 hrs. Extracts from whole cells or nuclei were separately purified and subjected to WB analysis with antibody against pERK2, LITAF, or actin/tubulin as control.
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| S7565 |
WH-4-023WH-4-023是一种有效的，口服具有活性的Lck/Src抑制剂，无细胞试验中IC50分别为2 nM 和 6 nM。对p38α和KDR的选择性低300倍以上，还能有效抑制SIK（对SIK1、2、3的IC50分别为10、22、60 nM）。 |
(G-I) WB analysis of total LCK, LCK Y505, and Src Y416 expression in ALL-SIL, CCRF-CEM, and TALL-1. Cells were treated with DMSO only (Ctrl), dasatinib, bosutinib, nintedanib, or WH-4-023 overnight at the compound concentrations corresponding to the GI50 at 48 hr. Bos, bosutinib; Das, dasatinib; Nint, nintedanib; WH, WH-4-023.
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| S8518 |
AD80AD80，一种多激酶抑制剂，对人源RET、BRAF、S6K和SRC活性较强，但对mTOR的活性比AD57或AD58弱。其对RET的IC50值为4 nM。 |
||
| S7782 |
Dasatinib MonohydrateDasatinib Monohydrate 是一种新型有效的多靶点抑制剂，作用于靶点Abl，Src 和 c-Kit，IC50分别为 <1 nM，0.8 nM 和 79 nM。 |
|
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| S8583 |
Repotrectinib (TPX-0005)TPX-0005是一种新型的ALK/ROS1/TRK抑制剂，对WT ALK、ALK(G1202R)、ALK(L1196M)的IC50分别为1.01 nM、1.26 nM、1.08 nM；同时也是一种有效的SRC抑制剂，IC50为5.3 nM。 |
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| S2391 |
QuercetinQuercetin是蔬菜水果和白酒中的天然黄酮类化合物，是一种体外重组Sirt1蛋白的激活剂同时也是PI3K抑制剂，IC50为2.4 – 5.4 μM。 |
After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF. |
|
| S7774 |
SU6656SU 6656 是一种选择性 Src 家族激酶抑制剂，对Src，Yes，Lyn，和 Fyn 的 IC50 分别为 280 nM，20 nM，130 nM，和 170 nM。 |
Interaction between Src and FAK during ILTV infection in LMH cells. The protein levels of FAK, phosphorylated FAK (p-FAK), Src, and phosphorylated Src (p-SRC) were assayed in LMH cells with or without ILTV infection upon pretreatment with SU6656. β-Tubulin or β-actin was used as a loading control. The intensity ratio between the corresponding bands (upper band/lower band) was determined using ImageJ and normalized to the ratio of DMSO.
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| S7743 |
CCT196969CCT196969是一种新型的、具有口服活性的pan-RAF抑制剂，同时具有抑制SRC的活性。它还能抑制LCK和p38 MAPKs。 |
||
| S8321 |
MLR-1023MLR-1023是Lyn kinase 激活剂，也是一种新型的insulin receptor 增强剂，在具有2型糖尿病的动物模型中使得葡萄糖稳态快速起效、并持久改善。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1021 |
DasatinibDasatinib是一种新型有效的多靶点抑制剂，作用于Abl，Src和 c-Kit，在无细胞试验中IC50分别为 <1 nM，0.8 nM 和 79 nM。 |
Antitumor activity (A)and body weight (B) relationship for BLU-285 and dasatinib in a P815 KIT D814Y mastocytoma allograft model.
|
|
| S1006 |
Saracatinib (AZD0530)Saracatinib (AZD0530)是一种有效的Src抑制剂，无细胞试验中IC50为2.7 nM，对c-Yes， Fyn， Lyn， Blk， Fgr和Lck也具有活性；但对Abl和EGFR (L858R和L861Q)活性较低。Phase 2/3。 |
Saracatinib (AZD0530) administration alleviates provocative tumor formation conferred by LHBs exp ression. A and B, cell proliferation assay for Huh7 cells (A) and SK-Hep1 cells (B) after stable LHBs expression under treatment with saracatinib(1 μmol/L). *, P < 0.05. |
|
| S1014 |
Bosutinib (SKI-606)Bosutinib (SKI-606)是一种新型的双重Src/Abl抑制剂，在无细胞试验中IC50分别为1.2 nM 和 1 nM。 |
Both parental and HR cell lines were treated with bosutinib (0.01, 0.1, and 1 μmol/L) for 24 hours. Src-related signaling pathway molecules were then analyzed. |
|
| S2700 |
KX2-391KX2-391是第一个临床Src抑制剂(拟肽类)，靶向作用于Src的肽底物位点，在癌细胞系中GI50为9-60 nM。Phase 2。 |
The histogram represents the absolute cell numbers obtained after 15 days of culture, in the presence of KX2-391 inhibitor at different concentrations and Dasatinib, as compared to control, arbitrarily normalized to one. The data are represented as mean±SEM obtained by nine independent experiments and analyzed by Wilcoxon signed-rank test (*p < 0.05; **p < 0.005).
|
|
| S2202 |
NVP-BHG712NVP-BHG712是一种特异性的EphB4抑制剂，ED50为25 nM，区别于对VEGFR和EphB4的抑制，对c-Raf， c-Src和c-Abl也具有抑制活性，IC50分别为0.395 μM， 1.266 μM和1.667 μM。 |
|
|
| S5254New |
Dasatinib hydrochlorideDasatinib hydrochloride is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. |
||
| S8706New |
UM-164UM-164是一种高度有效的c-Src/p38双重抑制剂，对c-Src的结合常数Kd值为2.7 nM，也能抑制p38α和p38β。 |
||
| S7008 |
PP2PP2是一种Src家族激酶抑制剂，有效抑制Lck/Fyn，无细胞试验中IC50为4 nM/5 nM，作用于EGFR效果低100倍左右，对ZAP-70，JAK2和PKA没有活性。 |
Inhibition of PLCG1 phosphorylation by the silencing of DopEcR, ErGPCR, and Gq and the addition of inhibitors of RTK and Src. 5 µM SU6668 (RTK inhibitor) and 20 µM PP2 (Src inhibitor) were added to the cells for 30 min treatment before the 20E stimulation.
|
|
| S2622 |
PP121PP121是一种作用于PDGFR， Hck， mTOR， VEGFR2， Src和Abl的多靶点抑制剂，IC50分别为2 nM， 8 nM， 10 nM， 12 nM， 14 nM和18 nM，也抑制DNA-PK，IC50为60 nM。 |
After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of PP-121 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF. |
|
| S7060 |
PP1PP1是一种有效的Src选择性抑制剂，作用于Lck/Fyn时，IC50为5 nM/6 nM。 |
PP1 attenuated DAVLBH-induced lysosomal degradation of internalized VE-cadherin. HUVECs pretreated with or without PP1 were treated with or without DAVLBH for 4 h. Quantification of BV9/LAMP colocalization is shown (n = 3). The data are presented as mean ± SEM. ***P < 0.001 compared with the control group; #P < 0.05 and ###P < 0.001 compared with the DAVLBH group (one-way ANOVA with Tukey's post hoc comparison). Scale bar, 20 µm.
|
|
| S4921 |
MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN)MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN)是一种酪氨酸激酶抑制剂，抑制Syk， Src和p97， IC50分别为2.5 μM， 29.3 μM和1.7 μM。 |
WT mouse primary macrophages were untreated as control (lane 1) or treated with 0.1μg/ml E. coli LPS (lane 5-8), 10μM E-64 (lane 2 and 6), 250μM PMSF (lane 3 and 7), or 20μM MNS (lane 4 and 8). The cells were continuously cultured for 16 hrs. Extracts from whole cells or nuclei were separately purified and subjected to WB analysis with antibody against pERK2, LITAF, or actin/tubulin as control.
|
|
| S7565 |
WH-4-023WH-4-023是一种有效的，口服具有活性的Lck/Src抑制剂，无细胞试验中IC50分别为2 nM 和 6 nM。对p38α和KDR的选择性低300倍以上，还能有效抑制SIK（对SIK1、2、3的IC50分别为10、22、60 nM）。 |
(G-I) WB analysis of total LCK, LCK Y505, and Src Y416 expression in ALL-SIL, CCRF-CEM, and TALL-1. Cells were treated with DMSO only (Ctrl), dasatinib, bosutinib, nintedanib, or WH-4-023 overnight at the compound concentrations corresponding to the GI50 at 48 hr. Bos, bosutinib; Das, dasatinib; Nint, nintedanib; WH, WH-4-023.
|
|
| S8518 |
AD80AD80，一种多激酶抑制剂，对人源RET、BRAF、S6K和SRC活性较强，但对mTOR的活性比AD57或AD58弱。其对RET的IC50值为4 nM。 |
||
| S7782 |
Dasatinib MonohydrateDasatinib Monohydrate 是一种新型有效的多靶点抑制剂，作用于靶点Abl，Src 和 c-Kit，IC50分别为 <1 nM，0.8 nM 和 79 nM。 |
|
|
| S8583 |
Repotrectinib (TPX-0005)TPX-0005是一种新型的ALK/ROS1/TRK抑制剂，对WT ALK、ALK(G1202R)、ALK(L1196M)的IC50分别为1.01 nM、1.26 nM、1.08 nM；同时也是一种有效的SRC抑制剂，IC50为5.3 nM。 |
||
| S2391 |
QuercetinQuercetin是蔬菜水果和白酒中的天然黄酮类化合物，是一种体外重组Sirt1蛋白的激活剂同时也是PI3K抑制剂，IC50为2.4 – 5.4 μM。 |
After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF. |
|
| S7774 |
SU6656SU 6656 是一种选择性 Src 家族激酶抑制剂，对Src，Yes，Lyn，和 Fyn 的 IC50 分别为 280 nM，20 nM，130 nM，和 170 nM。 |
Interaction between Src and FAK during ILTV infection in LMH cells. The protein levels of FAK, phosphorylated FAK (p-FAK), Src, and phosphorylated Src (p-SRC) were assayed in LMH cells with or without ILTV infection upon pretreatment with SU6656. β-Tubulin or β-actin was used as a loading control. The intensity ratio between the corresponding bands (upper band/lower band) was determined using ImageJ and normalized to the ratio of DMSO.
|
|
| S7743 |
CCT196969CCT196969是一种新型的、具有口服活性的pan-RAF抑制剂，同时具有抑制SRC的活性。它还能抑制LCK和p38 MAPKs。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S8321 |
MLR-1023MLR-1023是Lyn kinase 激活剂，也是一种新型的insulin receptor 增强剂，在具有2型糖尿病的动物模型中使得葡萄糖稳态快速起效、并持久改善。 |
