RIP1-kinase 选择性抑制剂 | 激活剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S8845 GSK3145095

GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities.

Selective RIP1 kinase, IC50: 6.3 nM
S8484 GSK2982772

GSK2982772是receptor-interacting protein-1 (RIP1) kinase的ATP竞争性抑制剂,IC50为1 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。

Selective human RIP1, IC50: 16 nM
S8642 GSK'963

GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase (RIPK1) with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.

Selective RIP1 kinase, IC50: 29 nM
S8641 Necrostatin 2 racemate (Nec-1s)

Necrostatin 2 racemate (Nec-1s, 7-Cl-O-Nec1, Necrostatin-1 stable, Necrostatin 1S) is a stable variant of Necrostatin-1. It is a more specific RIPK1 inhibitor lacking the IDO-targeting effect, with >1000-fold more selective for RIPK1 than for any other kinase out of 485 human kinases.

S8169 GSK481

GSK481是RIP1(Receptor Interacting Protein Kinase1)抑制剂,抑制RIP1以阻碍细胞坏死。

S6511 RIPA-56

RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor.

Pan RIP1, IC50: 13 nM
S8037 Necrostatin-1

Necrostatin-1是一种特异性RIP1抑制剂,抑制TNF-α诱导的细胞坏死,在293T细胞中EC50为490 nM。

Pan RIP1, EC50: 490 nM
S5584 Citronellol

Citronellol (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.

S8787 GSK'547

GSK'547 is a highly selective and potent inhibitor of RIP1 (RIPK1) exhibiting a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963