RIP kinase
抑制剂选择性比较
RIP kinase产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S8037 |
Necrostatin-1Necrostatin-1 (Nec-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。 |
![]() ![]() 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.
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S2805 |
LY364947LY364947 (HTS 466284)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。 |
![]() ![]() 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. |
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S6511 |
RIPA-56RIPA-56是一种高效力、代谢稳定的选择性RIP1 (RIPK1)抑制剂。 |
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S8641 |
Necrostatin 2 racemate (Nec-1s)Necrostatin 2 racemate (Nec-1s, 7-Cl-O-Nec1, Necrostatin-1 stable, Necrostatin 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。 |
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E0301New |
Necrostatin-34 (Nec-34)Necrostatin-34 (Nec-34) 是 RIPK1激酶 的小分子抑制剂,在 L929 细胞中的 IC50 为 0.13 μM。 |
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S9733New |
Mito-TEMPOMito-TEMPO (MT) 是一种线粒体靶向超氧化物歧化酶模拟物,通过抑制过氧亚硝酸盐的形成,保护对乙酰氨基酚(APAP)肝毒性的早期阶段。Mito-TEMPO 处理可抑制 APAP 诱导的 RIP3 kinase 表达。 |
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S8787 |
GSK'547GSK'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。 |
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S8484 |
GSK2982772GSK2982772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。 |
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S8642 |
GSK'963GSK'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。 |
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S8261 |
GSK583GSK583 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,在外植体培养中的IC50值约为 200 nM。 |
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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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S8845 |
GSK3145095GSK3145095 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。 |
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S9786 |
BDTX-189BDTX-189 是一种有效的 EGFR 和 HER2 致癌突变的变构性抑制剂,对EGFR、HER2、BLK 和 RIPK2的Kd值分别为0.2 nM、0.76 nM、13 nM和1.2 nM。BDTX-189 具有抗癌活性。 |
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S6078 |
ICCB-19 hydrochlorideICCB-19 hydrochloride 是 TNFRSF1A Associated Via Death Domain (TRADD) 的抑制剂,可保护 Velcade 诱导的 Jurkat细胞凋亡,对应的IC50值为 1.12 μM,保护MEF中的RDA的IC50值为2.01 μM。ICCB-19 可间接地抑制 Receptor-interacting serine/threonine-protein kinase 1 (RIPK1)。ICCB-19 可有效地诱导自噬。 |
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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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S8927 |
GSK2983559 (compound 3)GSK2983559 (compound 3, RIP2 kinase inhibitor 1, RIPK2-IN-1)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。 |
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S8169 |
GSK481GSK481是RIP1(Receptor Interacting Protein Kinase1, RIPK1)抑制剂,抑制RIP1以阻碍细胞坏死。 |
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S3238 |
ResibufogeninResibufogenin (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。 |
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S5584 |
CitronellolCitronellol (Dihydrogeraniol, (±)-β-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-1Necrostatin-1 (Nec-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。 |
![]() ![]() 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 |
LY364947LY364947 (HTS 466284)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。 |
![]() ![]() 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-56RIPA-56是一种高效力、代谢稳定的选择性RIP1 (RIPK1)抑制剂。 |
||
S8641 |
Necrostatin 2 racemate (Nec-1s)Necrostatin 2 racemate (Nec-1s, 7-Cl-O-Nec1, Necrostatin-1 stable, Necrostatin 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。 |
||
E0301New |
Necrostatin-34 (Nec-34)Necrostatin-34 (Nec-34) 是 RIPK1激酶 的小分子抑制剂,在 L929 细胞中的 IC50 为 0.13 μM。 |
||
S9733New |
Mito-TEMPOMito-TEMPO (MT) 是一种线粒体靶向超氧化物歧化酶模拟物,通过抑制过氧亚硝酸盐的形成,保护对乙酰氨基酚(APAP)肝毒性的早期阶段。Mito-TEMPO 处理可抑制 APAP 诱导的 RIP3 kinase 表达。 |
||
S8787 |
GSK'547GSK'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 |
GSK2982772GSK2982772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。 |
||
S8642 |
GSK'963GSK'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 |
GSK583GSK583 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,在外植体培养中的IC50值约为 200 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。 |
![]() ![]() (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.
|
|
S8845 |
GSK3145095GSK3145095 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。 |
||
S9786 |
BDTX-189BDTX-189 是一种有效的 EGFR 和 HER2 致癌突变的变构性抑制剂,对EGFR、HER2、BLK 和 RIPK2的Kd值分别为0.2 nM、0.76 nM、13 nM和1.2 nM。BDTX-189 具有抗癌活性。 |
||
S6078 |
ICCB-19 hydrochlorideICCB-19 hydrochloride 是 TNFRSF1A Associated Via Death Domain (TRADD) 的抑制剂,可保护 Velcade 诱导的 Jurkat细胞凋亡,对应的IC50值为 1.12 μM,保护MEF中的RDA的IC50值为2.01 μM。ICCB-19 可间接地抑制 Receptor-interacting serine/threonine-protein kinase 1 (RIPK1)。ICCB-19 可有效地诱导自噬。 |
||
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。 |
||
S8927 |
GSK2983559 (compound 3)GSK2983559 (compound 3, RIP2 kinase inhibitor 1, RIPK2-IN-1)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。 |
||
S8169 |
GSK481GSK481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 |
ResibufogeninResibufogenin (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 |
CitronellolCitronellol (Dihydrogeraniol, (±)-β-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. |