Serine/threonin kinase

Serine/threonin kinase产品

目录号	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, Ki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 Nucleic Acids Res, 2017, 45(16):9654-9678	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。	Nat Cell Biol, 2019, 21(6):778-790 J Immunother Cancer, 2019, 7(1):33 J Mol Med (Berl), 2019, 10.1007/s00109-019-01807-8	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.
S8824New	EMD638683 EMD638683 是一种 serum- and glucocorticoid-inducible kinase 1 (SGK1) 的高度选择性抑制剂，其IC50值为3 μM。EMD638683 具有降压药效和抗肿瘤活性。
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。	Antioxid Redox Signal, 2020, 23 Cell Death Dis, 2020, 22;11(5):391 Biochem Pharmacol, 2020, 12:114023	(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	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。
S8976New	DCLK1-IN-1 DCLK1-IN-1 是一种选择性的 doublecortin like kinase 1 (DCLK1) domain 的体内相容性化学探针，可与DCLK1和DCLK2结合，对应的IC50分别为9.5 nM和31 nM。在激酶活性测定中，DCLK1-IN-1抑制DCLK1和DCLK2激酶的IC50分别为57.2 nM和103 nM。
S8929New	GCN2iB GCN2iB is an ATP-competitive serine/threonine-protein kinase general control nonderepressible 2 (GCN2) inhibitor with IC50 of 2.4 nM.
S6710New	SGC-GAK-1 SGC-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。
S4956	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。	Sci Rep, 2019, 9(1):382 Nature, 2015, 519(7542):247-50 Nature, 2015, 12;519(7542):247-50.
S8810	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	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。
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）	BMC Cancer, 2020, 20(1):4 Nat Cell Biol, 2019, 21(12):1532-1543
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。	Nat Cell Biol, 2019, 21(6):778-790 Cancer Res, 2018, 78(18):5274-5286 Aging (Albany NY), 2018, 10(12):3736-3744

目录号	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, Ki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 Nucleic Acids Res,2017, 45(16):9654-9678	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。	Nat Cell Biol,2019, 21(6):778-790 J Immunother Cancer,2019, 7(1):33 J Mol Med (Berl),2019, 10.1007/s00109-019-01807-8	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.
S8824New	EMD638683 EMD638683 是一种 serum- and glucocorticoid-inducible kinase 1 (SGK1) 的高度选择性抑制剂，其IC50值为3 μM。EMD638683 具有降压药效和抗肿瘤活性。
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。	Antioxid Redox Signal,2020, 23 Cell Death Dis,2020, 22;11(5):391 Biochem Pharmacol,2020, 12:114023	(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	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。
S8976New	DCLK1-IN-1 DCLK1-IN-1 是一种选择性的 doublecortin like kinase 1 (DCLK1) domain 的体内相容性化学探针，可与DCLK1和DCLK2结合，对应的IC50分别为9.5 nM和31 nM。在激酶活性测定中，DCLK1-IN-1抑制DCLK1和DCLK2激酶的IC50分别为57.2 nM和103 nM。
S8929New	GCN2iB GCN2iB is an ATP-competitive serine/threonine-protein kinase general control nonderepressible 2 (GCN2) inhibitor with IC50 of 2.4 nM.
S6710New	SGC-GAK-1 SGC-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。
S4956	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。	Sci Rep,2019, 9(1):382 Nature,2015, 519(7542):247-50 Nature,2015, 12;519(7542):247-50.
S8810	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	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。
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）	BMC Cancer,2020, 20(1):4 Nat Cell Biol,2019, 21(12):1532-1543
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。	Nat Cell Biol,2019, 21(6):778-790 Cancer Res,2018, 78(18):5274-5286 Aging (Albany NY),2018, 10(12):3736-3744