RIP kinase

抑制剂选择性比较

RIP kinase产品

所有产品 RIP kinase抑制剂(10)

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.
S6511^New	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 J Exp Clin Cancer Res, 2019, 38(1):461
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
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。
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。
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.

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.
S6511^New	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 J Exp Clin Cancer Res,2019, 38(1):461
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
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。
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。
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.