“Ligand-gated Ion Channels”的搜索结果
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RIPK2 inhibitor
WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation.
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RET inhibitor
cis-Pralsetinib (cis-BLU-667) is a highly potent and selective inhibitor of rearranged during transfection (RET), with IC50s ranging from 0.3 to 0.4 nM for WT RET and four enzyme variants (V804L, V804M, M918T, CCDC6-RET), and with broad, robust and anti-tumor activity against multiple RET-driven solid tumor types.
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MDM2 inhibitor
RO8994 is a highly potent and selective series of spiroindolinone small-molecule MDM2 inhibitor, with IC50 of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays).
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MDM2 inhibitor
MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53, induces apoptosis, and has anti-tumor activity.
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RIPK1 inhibitor
PK68 is a potent and selective type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90?nM, displays inhibition of RIPK1-dependent necroptosis.
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MDM2/MDMX inhibitor
RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53 with IC50s of ~17 nM and ~24 nM, respectively.
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Mcl-1/Bim interaction 抑制剂
ML311 is a potent and selective inhibitor of the Mcl-1/Bim interaction
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p53-MDM2 interaction 抑制剂
p53和MDM2蛋白相互作用抑制剂消旋体是p53和MDM2蛋白之间相互作用的抑制剂。
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p53-MDM2 interaction 抑制剂
p53和MDM2蛋白相互作用抑制剂手性是p53和MDM2蛋白之间相互作用的抑制剂。
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eIF2α dephosphorylation 抑制剂
Salubrinal是细胞磷酸酶复合物的可渗透细胞的选择性抑制剂,可将真核翻译起始因子2亚基α(eIF2α)磷酸化。保护细胞免受内质网应激诱导的细胞凋亡(EC50?15 μM)。
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- Gregory R. Kardos, .et al. Salubrinal in Combination With 4E1RCat Synergistically Impairs Melanoma Development by Disrupting the Protein Synthetic Machinery, Front Oncol, 2020, 10: 834 PMID: 32637352