Serine/threonin kinase
抑制剂选择性比较
Serine/threonin kinase产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7270 |
SRPIN340SRPIN340是选择性SRPK抑制剂，作用于SRPK1, Ki为0.89 μM ，对其他140多种激酶没有显著的抑制活性。 |
Crystal violet staining of the indicated cell lines treated with SRPIN340 at the indicated concentrations.
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| S7209 |
GSK650394GSK650394是一种血清和糖皮质激素调节的激酶-1抑制剂,对SGK1和SGK2的 IC50分别为62 nM和103 nM。 |
BV-2 cells were incubated in the absence or presence of gsk650394 (1 μM) for 30 min, followed by LPS (500 ng/ml) administration for 30 min, and then fixed. NF-κB p65 protein was visualized by indirect immunofluorescence staining using an antibody for NF-κB p65. For nuclear staining, the cells were stained with DAPI. Bar = 20 μm.
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| S6499New |
PF-6260933PF-6260933是MAP4K4抑制剂，IC50为3.7 nM，具有良好的激酶组选择性。 |
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| S8388 |
ML-7 HClML-7是平滑肌肌球蛋白轻链激酶MLCK抑制剂，Ki值为0.3 μM。对钙离子-钙调蛋白依赖性或非依赖性的平滑肌MLCKs具有可逆的、ATP竞争性抑制作用。 |
Platelets (3 × 108/mL) were treated with ML-7 (5 µM) for 20 minutes, followed by stimulation with oxLDL (50 µg/mL) for 15 seconds. Samples were then lysed, separated by SDS-PAGE, and immunoblotted for phospho-MLCSer19 followed by reprobing for β-tubulin. (Ai) Representative blots. (Aii) Densitometric analysis of 5 independent experiments. *P < .05.
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| S8465 |
GSK'872 (GSK2399872A)GSK'872 (GSK2399872A)是一种有效的、特异性的RIP3 kinase抑制剂，与RIP3激酶区域以高亲和力结合（IC50为1.8 nM），抑制酶活性的IC50为1.3 nM。仅具微弱交叉反应。 |
(H-K) Cells incubated in the absence or presence of GSK’872, and treated with PM (100 μg/ml) for 24 h. The relative levels of IL6 (H), and IL8 (J) mRNA transcripts were measured by quantitative RT-PCR, and the protein levels of IL6 (I) and IL8 (K) in the culture supernatants, which are in turn were measured by ELISA.
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| S8257New |
CFI-402257CFI-402257 is a potent highly selective, and orally active small-molecule inhibitor of Mps1 with Ki value of 0.09 ± 0.02 nM. |
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| S2642New |
1-Naphthyl PP1(1-NA-PP1)1-Naphthyl PP1 (1-NA-PP 1)是一种高度选择性的、有效的 pan-PKD 抑制剂，对于PKD1、PKD2和PKD3的IC50值分别为154.6 nM、133.4 nM和109.4 nM。1-Naphthyl PP1是 Src family kinases (v-Src, c-Fyn) 和 the tyrosine kinase c-Abl 的选择性抑制剂， 对于v-Src、c-Fyn、c-Abl、CDK2和CAMK II的IC50值分别为1.0 μM、 0.6 μM、0.6 μM、18 μM 和 22 μM。 |
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| S6710New |
SGC-GAK-1SGC-GAK-1是一种有效的、具有细胞活性的cyclin G-associated kinase (GAK)抑制剂，Ki值为3.1 nM。对GAK的选择性比对其他相近激酶的选择性高50倍以上。 |
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| S8864New |
ZT-12-037-01ZT-12-037-01是ATP竞争性STK19抑制剂，对STK19 (WT)和STK19 (D89N)的IC50值分别为23.96 nM和27.94 nM。浓度为1 μM时，在包含468种激酶的激酶库中具有高选择性。 |
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| S8872New |
GSK8612GSK8612是高效选择性TBK1抑制剂，pKd为8。 |
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| S8215 |
BAY 1217389BAY 1217389一种具有生物口服活性的、选择性丝氨酸/苏氨酸激酶monopolar spindle 1 (Mps1)抑制剂，IC50低于10 nM，具有良好的选择性。 |
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| S5792 |
CID 2011756CID 2011756是protein kinase D (PKD)的抑制剂，对PKD1、PKD2、PKD3的IC50值分别为3.2、0.6和0.7 μM。 |
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| S4956 |
Benzamidine HClBenzamidine是丝氨酸蛋白酶（serine proteases）抑制剂，对胰蛋白酶（trypsin）、胞浆素（plasmin）和凝血酶（thrombin）的IC50分别为35 μM、350 μM和220 μM。 |
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| S8810 |
SPHINX31SPHINX31是SRPK1抑制剂，IC50为5.9 nM。它对SRPK1的选择性是对SRPK2的50倍，CLK1的100倍。 |
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| S8775 |
HS-1371HS-1371是有效的RIP3 kinase抑制剂，IC50为20.8 nM。它结合到RIP3的ATP结合区域，因而阻止了ATP的结合、在体外抑制了RIP3的酶活性。 |
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| S8366 |
CRT0066101CRT0066101是PKD (Protein Kinase D)家族的特异性小分子抑制剂，在杜仲癌细胞类型中（包括A549h和MiaPaCa-2细胞），特异地抑制PKD1/2/3的活性，而不影响PKCα/PKCβ/PKCε活性。对PKD1/2/3的IC50分别为1, 2.5, 2 nM。 |
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| S6088 |
6-(Dimethylamino)purine6-Dimethylaminopurine是一种丝氨酸苏氨酸蛋白激酶（serine threonine protein kinase）抑制剂。它能抑制胚泡破裂以及卵母细胞的减数分裂成熟。 |
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| S8358 |
WNK463WNK463是一种WNK激酶的泛抑制剂。在体外实验中，它能有效地抑制WNK激酶家族中4个成员的活性（WNK1, WNK2, WNK3和WNK4） |
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| S7188 |
CID755673CID755673是一种具有细胞活性的泛PKD1/2/3抑制剂，IC50值分别为180 nM, 280nM,以及227 nM，选择性比其它CAMKs高大约200倍。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7270 |
SRPIN340SRPIN340是选择性SRPK抑制剂，作用于SRPK1, Ki为0.89 μM ，对其他140多种激酶没有显著的抑制活性。 |
Crystal violet staining of the indicated cell lines treated with SRPIN340 at the indicated concentrations.
|
|
| S7209 |
GSK650394GSK650394是一种血清和糖皮质激素调节的激酶-1抑制剂,对SGK1和SGK2的 IC50分别为62 nM和103 nM。 |
BV-2 cells were incubated in the absence or presence of gsk650394 (1 μM) for 30 min, followed by LPS (500 ng/ml) administration for 30 min, and then fixed. NF-κB p65 protein was visualized by indirect immunofluorescence staining using an antibody for NF-κB p65. For nuclear staining, the cells were stained with DAPI. Bar = 20 μm.
|
|
| S6499New |
PF-6260933PF-6260933是MAP4K4抑制剂，IC50为3.7 nM，具有良好的激酶组选择性。 |
||
| S8388 |
ML-7 HClML-7是平滑肌肌球蛋白轻链激酶MLCK抑制剂，Ki值为0.3 μM。对钙离子-钙调蛋白依赖性或非依赖性的平滑肌MLCKs具有可逆的、ATP竞争性抑制作用。 |
Platelets (3 × 108/mL) were treated with ML-7 (5 µM) for 20 minutes, followed by stimulation with oxLDL (50 µg/mL) for 15 seconds. Samples were then lysed, separated by SDS-PAGE, and immunoblotted for phospho-MLCSer19 followed by reprobing for β-tubulin. (Ai) Representative blots. (Aii) Densitometric analysis of 5 independent experiments. *P < .05.
|
|
| S8465 |
GSK'872 (GSK2399872A)GSK'872 (GSK2399872A)是一种有效的、特异性的RIP3 kinase抑制剂，与RIP3激酶区域以高亲和力结合（IC50为1.8 nM），抑制酶活性的IC50为1.3 nM。仅具微弱交叉反应。 |
(H-K) Cells incubated in the absence or presence of GSK’872, and treated with PM (100 μg/ml) for 24 h. The relative levels of IL6 (H), and IL8 (J) mRNA transcripts were measured by quantitative RT-PCR, and the protein levels of IL6 (I) and IL8 (K) in the culture supernatants, which are in turn were measured by ELISA.
|
|
| S8257New |
CFI-402257CFI-402257 is a potent highly selective, and orally active small-molecule inhibitor of Mps1 with Ki value of 0.09 ± 0.02 nM. |
||
| S2642New |
1-Naphthyl PP1(1-NA-PP1)1-Naphthyl PP1 (1-NA-PP 1)是一种高度选择性的、有效的 pan-PKD 抑制剂，对于PKD1、PKD2和PKD3的IC50值分别为154.6 nM、133.4 nM和109.4 nM。1-Naphthyl PP1是 Src family kinases (v-Src, c-Fyn) 和 the tyrosine kinase c-Abl 的选择性抑制剂， 对于v-Src、c-Fyn、c-Abl、CDK2和CAMK II的IC50值分别为1.0 μM、 0.6 μM、0.6 μM、18 μM 和 22 μM。 |
||
| S6710New |
SGC-GAK-1SGC-GAK-1是一种有效的、具有细胞活性的cyclin G-associated kinase (GAK)抑制剂，Ki值为3.1 nM。对GAK的选择性比对其他相近激酶的选择性高50倍以上。 |
||
| S8864New |
ZT-12-037-01ZT-12-037-01是ATP竞争性STK19抑制剂，对STK19 (WT)和STK19 (D89N)的IC50值分别为23.96 nM和27.94 nM。浓度为1 μM时，在包含468种激酶的激酶库中具有高选择性。 |
||
| S8872New |
GSK8612GSK8612是高效选择性TBK1抑制剂，pKd为8。 |
||
| S8215 |
BAY 1217389BAY 1217389一种具有生物口服活性的、选择性丝氨酸/苏氨酸激酶monopolar spindle 1 (Mps1)抑制剂，IC50低于10 nM，具有良好的选择性。 |
||
| S5792 |
CID 2011756CID 2011756是protein kinase D (PKD)的抑制剂，对PKD1、PKD2、PKD3的IC50值分别为3.2、0.6和0.7 μM。 |
||
| S4956 |
Benzamidine HClBenzamidine是丝氨酸蛋白酶（serine proteases）抑制剂，对胰蛋白酶（trypsin）、胞浆素（plasmin）和凝血酶（thrombin）的IC50分别为35 μM、350 μM和220 μM。 |
||
| S8810 |
SPHINX31SPHINX31是SRPK1抑制剂，IC50为5.9 nM。它对SRPK1的选择性是对SRPK2的50倍，CLK1的100倍。 |
||
| S8775 |
HS-1371HS-1371是有效的RIP3 kinase抑制剂，IC50为20.8 nM。它结合到RIP3的ATP结合区域，因而阻止了ATP的结合、在体外抑制了RIP3的酶活性。 |
||
| S8366 |
CRT0066101CRT0066101是PKD (Protein Kinase D)家族的特异性小分子抑制剂，在杜仲癌细胞类型中（包括A549h和MiaPaCa-2细胞），特异地抑制PKD1/2/3的活性，而不影响PKCα/PKCβ/PKCε活性。对PKD1/2/3的IC50分别为1, 2.5, 2 nM。 |
||
| S6088 |
6-(Dimethylamino)purine6-Dimethylaminopurine是一种丝氨酸苏氨酸蛋白激酶（serine threonine protein kinase）抑制剂。它能抑制胚泡破裂以及卵母细胞的减数分裂成熟。 |
||
| S8358 |
WNK463WNK463是一种WNK激酶的泛抑制剂。在体外实验中，它能有效地抑制WNK激酶家族中4个成员的活性（WNK1, WNK2, WNK3和WNK4） |
||
| S7188 |
CID755673CID755673是一种具有细胞活性的泛PKD1/2/3抑制剂，IC50值分别为180 nM, 280nM,以及227 nM，选择性比其它CAMKs高大约200倍。 |
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