RIP kinase

抑制剂选择性比较

RIP kinase产品

所有产品 RIP kinase抑制剂(13) RIP kinase激活剂(2)

目录号	产品描述	文献引用	实验数据
S8037	Necrostatin-1 Necrostatin-1是一种特异性RIP1 (RIPK1)抑制剂，抑制TNF-α诱导的细胞坏死，在293T细胞中EC50为490 nM。Necrostatin-1也可抑制 IDO、细胞自噬和凋亡。	Sci Adv, 2020, 25;6(13):eaay9789 Cell Death Dis, 2020, 22;11(5):391 Mol Nutr Food Res, 2020, 1;e1901231	Cytosolic extracts or nuclear extracts were examined by Western blot analysis using Abs against p105/p50, p100/p52 and phospho-p65. Solid arrowhead indicates a non-specific band. A nuclear marker, PARP, and cytosolic marker, b-tubulin, were used to assess the purity of each fraction.
S2805	LY364947 LY364947是一种有效的ATP竞争性TGFβR-I抑制剂，无细胞试验中IC50为59 nM，比作用于TGFβR-II选择性高7倍。	Cell Metab, 2020, 31(2):327-338 Nat Commun, 2020, 11(1):3344 Cell Death Dis, 2020, 27;11(1):65	The cytoplasmic and nuclear proteins were separated and the protein expression levels were determined by performing western blotting. LY364947 (1 uM), which is a potent ATP-competitive inhibitor of TGF-βRI, was used as the positive control. GAPDH and PARP were used as cytosolic and nuclear markers, respectively.
S6511	RIPA-56 RIPA-56是一种高效力、代谢稳定的选择性RIP1 (RIPK1)抑制剂。	Cancer Cell Int, 2020, 30;20:36 Biochem Biophys Res Commun, 2020, 10.1016/j.bbrc.2020.02.072
S8641	Nec-1s (7-Cl-O-Nec1) Nec-1s (7-Cl-O-Nec1, Necrostatin-1 stable) 是Necrostatin-1的一种稳态变体（stable variant）,它是一种更为特异的RIPK1抑制剂，没有靶向IDO的效果，对RIPK1的选择性比对其他485种人源激酶高1000倍以上。	Br J Cancer, 2020, 122(2):279-292 Molecules, 2020, 9;25(5):1225 Front Cell Dev Biol, 2020, 8:608
S8845^New	GSK3145095 GSK3145095 是一种有效的口服活性 RIP1 kinase 的抑制剂，IC50值为6.3 nM，具有潜在的抗肿瘤和免疫调节活性。
S8927^New	GSK2983559 (compound 3) GSK2983559是一种有效的receptor interacting protein 2 (RIP2) kinase抑制剂，具有良好的激酶特异性。
S8787	GSK'547 GSK'547是一种高度选择性、有效的RIP1 (RIPK1)抑制剂，在小鼠药代动力学研究中，口服暴露量相比GSK'963提高400倍。
S8484	GSK2982772 GSK2982772是receptor-interacting protein-1 (RIP1) kinase (RIPK1)的ATP竞争性抑制剂，IC50为16 nM。它能够抑制多种TNF依赖性的细胞反应，具有良好的激酶特异性和细胞活性。	Oncotarget, 2019, 10(62):6678-6690
S8642	GSK'963 GSK'963是RIP1 kinase (RIPK1)的手性小分子抑制剂，在FP结合实验中IC50值为29 nM。它对RIP1的选择性是对其他339种激酶的10,000倍以上。
S8261	GSK583 GSK583 是一种高度有效的、选择性的RIP2激酶抑制剂，IC50为5 nM。GSK583 还可抑制 TNF-α 和 IL-6 的生成，对应的IC50值为 200 nM。	Cancer Res, 2020, canres.530.2020
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.
S8775	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。
S8169	GSK481 GSK481是RIP1(Receptor Interacting Protein Kinase1, RIPK1)抑制剂，抑制RIP1以阻碍细胞坏死。
S3238^New	Resibufogenin Resibufogenin (Bufogenin, Recibufogenin) 是huachansu华蟾素中具有抗癌作用的成分，通过上调 receptor-interacting protein kinase 3 (RIP3) 和磷酸化 mixed lineage kinase domain-like protein 的Ser358位点来触发坏死病。Resibufogenin 可通过诱导 reactive oxygen species (ROS) 积累发挥细胞毒性作用。Resibufogenin 可诱导凋亡和 caspase-3 和 caspase-8 活性。Resibufogenin 增加 Bax/Bcl-2 表达，并抑制 cyclin D1、cyclin E、PI3K、p-AKT、p-GSK3β 和 β-catenin 的蛋白表达。
S5584	Citronellol Citronellol, a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.

目录号	产品描述	文献引用	实验数据
S8037	Necrostatin-1 Necrostatin-1是一种特异性RIP1 (RIPK1)抑制剂，抑制TNF-α诱导的细胞坏死，在293T细胞中EC50为490 nM。Necrostatin-1也可抑制 IDO、细胞自噬和凋亡。	Sci Adv,2020, 25;6(13):eaay9789 Cell Death Dis,2020, 22;11(5):391 Mol Nutr Food Res,2020, 1;e1901231	Cytosolic extracts or nuclear extracts were examined by Western blot analysis using Abs against p105/p50, p100/p52 and phospho-p65. Solid arrowhead indicates a non-specific band. A nuclear marker, PARP, and cytosolic marker, b-tubulin, were used to assess the purity of each fraction.
S2805	LY364947 LY364947是一种有效的ATP竞争性TGFβR-I抑制剂，无细胞试验中IC50为59 nM，比作用于TGFβR-II选择性高7倍。	Cell Metab,2020, 31(2):327-338 Nat Commun,2020, 11(1):3344 Cell Death Dis,2020, 27;11(1):65	The cytoplasmic and nuclear proteins were separated and the protein expression levels were determined by performing western blotting. LY364947 (1 uM), which is a potent ATP-competitive inhibitor of TGF-βRI, was used as the positive control. GAPDH and PARP were used as cytosolic and nuclear markers, respectively.
S6511	RIPA-56 RIPA-56是一种高效力、代谢稳定的选择性RIP1 (RIPK1)抑制剂。	Cancer Cell Int,2020, 30;20:36 Biochem Biophys Res Commun,2020, 10.1016/j.bbrc.2020.02.072
S8641	Nec-1s (7-Cl-O-Nec1) Nec-1s (7-Cl-O-Nec1, Necrostatin-1 stable) 是Necrostatin-1的一种稳态变体（stable variant）,它是一种更为特异的RIPK1抑制剂，没有靶向IDO的效果，对RIPK1的选择性比对其他485种人源激酶高1000倍以上。	Br J Cancer,2020, 122(2):279-292 Molecules,2020, 9;25(5):1225 Front Cell Dev Biol,2020, 8:608
S8845^New	GSK3145095 GSK3145095 是一种有效的口服活性 RIP1 kinase 的抑制剂，IC50值为6.3 nM，具有潜在的抗肿瘤和免疫调节活性。
S8927^New	GSK2983559 (compound 3) GSK2983559是一种有效的receptor interacting protein 2 (RIP2) kinase抑制剂，具有良好的激酶特异性。
S8787	GSK'547 GSK'547是一种高度选择性、有效的RIP1 (RIPK1)抑制剂，在小鼠药代动力学研究中，口服暴露量相比GSK'963提高400倍。
S8484	GSK2982772 GSK2982772是receptor-interacting protein-1 (RIP1) kinase (RIPK1)的ATP竞争性抑制剂，IC50为16 nM。它能够抑制多种TNF依赖性的细胞反应，具有良好的激酶特异性和细胞活性。	Oncotarget,2019, 10(62):6678-6690
S8642	GSK'963 GSK'963是RIP1 kinase (RIPK1)的手性小分子抑制剂，在FP结合实验中IC50值为29 nM。它对RIP1的选择性是对其他339种激酶的10,000倍以上。
S8261	GSK583 GSK583 是一种高度有效的、选择性的RIP2激酶抑制剂，IC50为5 nM。GSK583 还可抑制 TNF-α 和 IL-6 的生成，对应的IC50值为 200 nM。	Cancer Res,2020, canres.530.2020
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.
S8775	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。
S8169	GSK481 GSK481是RIP1(Receptor Interacting Protein Kinase1, RIPK1)抑制剂，抑制RIP1以阻碍细胞坏死。

目录号	产品描述	文献引用	实验数据
S3238^New	Resibufogenin Resibufogenin (Bufogenin, Recibufogenin) 是huachansu华蟾素中具有抗癌作用的成分，通过上调 receptor-interacting protein kinase 3 (RIP3) 和磷酸化 mixed lineage kinase domain-like protein 的Ser358位点来触发坏死病。Resibufogenin 可通过诱导 reactive oxygen species (ROS) 积累发挥细胞毒性作用。Resibufogenin 可诱导凋亡和 caspase-3 和 caspase-8 活性。Resibufogenin 增加 Bax/Bcl-2 表达，并抑制 cyclin D1、cyclin E、PI3K、p-AKT、p-GSK3β 和 β-catenin 的蛋白表达。
S5584	Citronellol Citronellol, a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.

目录号

产品描述

文献引用

实验数据

S3238^New

Resibufogenin

Resibufogenin (Bufogenin, Recibufogenin) 是huachansu华蟾素中具有抗癌作用的成分，通过上调 receptor-interacting protein kinase 3 (RIP3) 和磷酸化 mixed lineage kinase domain-like protein 的Ser358位点来触发坏死病。Resibufogenin 可通过诱导 reactive oxygen species (ROS) 积累发挥细胞毒性作用。Resibufogenin 可诱导凋亡和 caspase-3 和 caspase-8 活性。Resibufogenin 增加 Bax/Bcl-2 表达，并抑制 cyclin D1、cyclin E、PI3K、p-AKT、p-GSK3β 和 β-catenin 的蛋白表达。

S5584

Citronellol

Citronellol, a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.

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RIP kinase

抑制剂选择性比较

RIP kinase产品

Necrostatin-1

LY364947

RIPA-56

Nec-1s (7-Cl-O-Nec1)

GSK3145095

GSK2983559 (compound 3)

GSK'547

GSK2982772

GSK'963

GSK583

GSK'872 (GSK2399872A)

HS-1371

GSK481

Resibufogenin

Citronellol

Necrostatin-1

LY364947

RIPA-56

Nec-1s (7-Cl-O-Nec1)

GSK3145095

GSK2983559 (compound 3)

GSK'547

GSK2982772

GSK'963

GSK583

GSK'872 (GSK2399872A)

HS-1371

GSK481

Resibufogenin

Citronellol