“Ligand-gated Ion Channels”的搜索结果
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HDAC6 抑制剂
Tubacin (tubulin acetylation inducer)是一种高效且选择性强,可逆,可透过细胞的HDAC6抑制剂,IC50为4 nM。
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menin-MLL interaction 抑制剂
MI-3是一种有效的Menin-MLL相互作用抑制剂,IC50为648 nM。
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Calcineurin-NFAT 抑制剂
INCA-6是钙调神经磷酸酶-NFAT(活化T细胞的核因子)信号传导的有效和选择性抑制剂。
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Menin-MLL interaction 抑制剂
MI-2 (Menin-MLL inhibitor 2)特异性结合menin并抑制menin与细胞中mll融合蛋白的相互作用。它能有效逆转mll融合蛋白通过下调mll融合蛋白致癌活性下游靶基因的表达来介导白血病转化。mi-2是更好地理解mll介导的白血病发生的新工具,代表了研究menin作为mll融合蛋白致癌辅助因子的作用的新方法。
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5-HT1A receptor antagonist/COMT inhibitor
Flopropione是5-HT1A受体拮抗剂,也是儿茶酚-邻甲基转移酶(COMT)抑制剂。
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HDAC inhibitor
Valproic acid is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2; Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
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- Dan Zhao, .et al. From crypts to enteroids: establishment and characterization of avian intestinal organoids, Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
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JAK3 抑制剂
JAK3-IN-2 is a potent and highly selective JAK3 inhibitor with IC50 of 0.15 nM. dispalys >4,300-fold selectivity over JAK1, JAK2 and TYK2, and other kinases BMX, EGFR, ITK and BTK; blocks cytokine signaling through JAK3, but not through other JAK family enzymes; inhibits IL-7 induced pSTAT5 in CD3+, CD8+ T cells with IC50 of 280 nM; sufficiently blocks the development of inflammation in a rat model of rheumatoid arthritis, while sparing hematopoiesis.
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JAK1 抑制剂
Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease.
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HDAC 11 inhibitor
SIS17 is a potent and selective HDAC 11 inhibitor with an IC50 value of 0.83 μM. SIS17, is active in cells and inhibited the demyristoylation of a known HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
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BET inhibitor
ZEN-3219 is a BET inhibitor with IC50s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4.
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Aurora/PLK dual 抑制剂
AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis.
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BRD inhibitor
BETd-246 is a second-generation BET bromodomain (BRD) inhibitor, exhibiting superior selectivity, potency and antitumor activity.
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JAK1 抑制剂
JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM).
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KDM4A inhibitor
Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity.
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HDAC inhibitor
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2.
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HDAC/ER stress inhibitor
Sodium phenylbutyrate is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
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WDR5 and MLL protein-protein interaction inhibitor
MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction.
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WDR5/MLL interaction inhibitor
MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
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menin-mLL interaction inhibitor
MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
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