Serine/threonin kinase

抑制剂选择性比较

Serine/threonin kinase产品

所有产品 Serine/threonin kinase抑制剂(16) 新Serine/threonin kinase产品

产品目录	产品描述	文献引用	实验数据
S7270	SRPIN340 SRPIN340是选择性SRPK抑制剂，作用于SRPK1, K_i为0.89 μM ，对其他140多种激酶没有显著的抑制活性。	Cell, 2017, 171(7):1545-1558	Crystal violet staining of the indicated cell lines treated with SRPIN340 at the indicated concentrations.
S7209	GSK650394 GSK650394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。	J Immunother Cancer, 2019, 7(1):33 J Mol Med (Berl), 2019, 10.1007/s00109-019-01807-8 Front Physiol, 2019, 10:167	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.
S6499^New	PF-6260933 PF-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 HCl ML-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。	Exp Cell Res, 2018, 363(2):321-331 FASEB J, 2018, 10.1096/fj.201800343R Biomed Pharmacother, 2017, 92:810-818	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。	Cell, 2019, 177(2):384-398 Oxid Med Cell Longev, 2019, 2019:2301903 Exp Mol Med, 2018, 50(9):125	(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.
S8864^New	ZT-12-037-01 ZT-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。
S8872^New	GSK8612 GSK8612是高效选择性TBK1抑制剂，pKd为8。
S8810^New	SPHINX31 SPHINX31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。
S6088^New	6-(Dimethylamino)purine 6-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。
S8775^New	HS-1371 HS-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。
S4956^New	Benzamidine HCl Benzamidine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。
S5792^New	CID 2011756 CID 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。
S8215	BAY 1217389 BAY 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。
S8366	CRT0066101 CRT0066101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。
S8358	WNK463 WNK463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	CID755673 CID755673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。	Mol Cell Biochem, 2018, 446(1-2):199-207 J Mol Med (Berl), 2017, 95(7):739-751

产品目录	产品描述	文献引用	实验数据
S7270	SRPIN340 SRPIN340是选择性SRPK抑制剂，作用于SRPK1, K_i为0.89 μM ，对其他140多种激酶没有显著的抑制活性。	Cell,2017, 171(7):1545-1558	Crystal violet staining of the indicated cell lines treated with SRPIN340 at the indicated concentrations.
S7209	GSK650394 GSK650394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。	J Immunother Cancer,2019, 7(1):33 J Mol Med (Berl),2019, 10.1007/s00109-019-01807-8 Front Physiol,2019, 10:167	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.
S6499^New	PF-6260933 PF-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 HCl ML-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。	Exp Cell Res,2018, 363(2):321-331 FASEB J,2018, 10.1096/fj.201800343R Biomed Pharmacother,2017, 92:810-818	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。	Cell,2019, 177(2):384-398 Oxid Med Cell Longev,2019, 2019:2301903 Exp Mol Med,2018, 50(9):125	(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.
S8864^New	ZT-12-037-01 ZT-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。
S8872^New	GSK8612 GSK8612是高效选择性TBK1抑制剂，pKd为8。
S8810^New	SPHINX31 SPHINX31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。
S6088^New	6-(Dimethylamino)purine 6-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。
S8775^New	HS-1371 HS-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。
S4956^New	Benzamidine HCl Benzamidine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。
S5792^New	CID 2011756 CID 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。
S8215	BAY 1217389 BAY 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。
S8366	CRT0066101 CRT0066101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。
S8358	WNK463 WNK463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	CID755673 CID755673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。	Mol Cell Biochem,2018, 446(1-2):199-207 J Mol Med (Berl),2017, 95(7):739-751

Tags: STK activation | STK kinase family | STK family kinases | STK activity | STK cancer | Serine/threonine kinase | STK phosphorylation | STK inhibition | STK inhibitors cancer | STK inhibitor review