RIP2-kinase 选择性抑制剂 | 激活剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S9786 BDTX-189

BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity.

Selective RIPK2, Kd: 1.2 nM
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。

Selective RIPK2, IC50: 0.11 μM
S8927 GSK2983559 (compound 3)

GSK2983559 (compound 3, RIP2 kinase inhibitor 1, RIPK2-IN-1) is a potent inhibitor of receptor interacting protein 2 (RIP2) kinase with good kinase specificity.

S8169 GSK481

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

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。

Pan RIP2, IC50: 5 nM
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
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

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.