“Ligand-gated Ion Channel”的搜索结果
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TRPV4 antagonist
RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM).
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TRPM8 inhibitor
BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
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5-HT1A agonist
Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K+ channel blocker, with IC50 of 3800 nM.
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IP3R inhibitor
2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca2+ (SOC) channel and activates some TRP channels (V1, V2 and V3).
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potassium current activator
NS5806, a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2.
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inhibitor of KCNJ1
KCNJ1 (Kir1.1, or renal outer medullary potassium channel) and KCNJ13 (Kir7.1) are inwardly rectifying two-transmembrane K+ channels. KCNJ1 has critical roles in kidney function, while KCNJ13 is important in the eye, kidney, and small intestine. VU590 is a small molecule inhibitor of KCNJ1 (IC50 = 294 nM) which also causes 70% inhibition of KCNJ13 at 10 ?M. It has no effect on the related channels KCNJ2 (Kir2.1) and KCNJ10 (Kir4.1) at a concentration of 10 ?M.
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Violanthrone-79 is an n-channel organic semiconductor
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HCN4 CLP ligand
BPU-11 is a HCN4 CLP ligand. It acts by modulating channel function and completely abolishing the cAMP-induced shift in V1/2.
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HIV-1 production 抑制剂
Baicalin是已知的脯氨酰内肽酶抑制剂,并且影响GABA受体。
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- Shoichi Ozawa, .et al. Uremic serum residue decreases SN-38 sensitivity through suppression of organic anion transporter polypeptide 2B1 in LS-180 colon cancer cells, Sci Rep, 2019, 9: 15464
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Dienogest是一种口服抗孕激素,具有抗雄激素活性,因此可以改善雄激素症状。
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Protein translocation 抑制剂
Brefeldin A阻断ADP-核糖基化因子与高尔基体的结合并抑制GDP-GTP交换。
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Rheochrysidin (Physcione)是大成气汤治疗炎症的主要成分之一。
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osteoclastic bone resorption 抑制剂
Zoledronic acid, 破骨细胞抑制剂,通过抑制甲羟戊酸途径诱导破骨细胞凋亡。
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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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Protective agent
Dimesna (BNP7787)是一种用于减少尿毒症的尿道保护剂。
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HCV replication 抑制剂
Anguizole是一种抑制HCV复制并改变NS4B亚细胞分布的小分子。
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- Choi M, .et al. A hepatitis C virus NS4B inhibitor suppresses viral genome replication by disrupting NS4B-s dimerization/multimerization as well as its interaction with NS5A, Virus Genes., 2013, Dec;47(3):395-407 PMID: 23868571
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Amfebutamone (Bupropion)是一种非典型的抗抑郁药和戒烟助剂。
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Glucocorticoid Receptor 激动剂
Betamethasone Dipropionate是糖皮质激素类固醇,具有抗炎和免疫抑制特性。
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Protein Synthesis 抑制剂
Cycloheximide (Actidione)用作选择性抗生素。它抑制腐菌真菌真核生物的蛋白质合成(DNA依赖性RNA)。通过与80S核糖体结合而对皮肤真菌和系统性真菌无效。
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- Ke Chen, .et al. Junction plakoglobin regulates and destabilizes HIF2α to inhibit tumorigenesis of renal cell carcinoma, Cancer Commun (Lond), 2021, Apr; 41(4): 316-332 PMID: 33591636
- Zhiyuan Qin, .et al. miR-224-5p Contained in Urinary Extracellular Vesicles Regulates PD-L1 Expression by Inhibiting Cyclin D1 in Renal Cell Carcinoma Cells, Cancers (Basel), 2021, Feb 4;13(4):618 PMID: 33557163
- Hua Xu, .et al. Preclinical Study Using ABT263 to Increase Enzalutamide Sensitivity to Suppress Prostate Cancer Progression Via Targeting BCL2/ROS/USP26 Axis Through Altering ARv7 Protein Degradation, Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
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Androgen 拮抗剂
17 alpha-propionate是一种新型的局部和外周选择性雄激素拮抗剂。
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Voltage-gated sodium channels 拮抗剂
Proparacaine HCl是一种电压门控钠通道拮抗剂,ED50为3.4 mM。
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Doxazosin mesylate是一种喹唑啉化合物,是一种α1选择性α受体阻滞剂,用于治疗与良性前列腺增生(BPH)相关的高血压和尿retention留。
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Fluticasone propionate是一种高亲和力的选择性糖皮质激素受体激动剂(Kd = 0.5 nM)。
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- Abhinav Kumar, .et al. A Biocompatible Synthetic Lung Fluid Based on Human Respiratory Tract Lining Fluid Composition, Pharm Res, 2017, 34(12): 2454-2465 PMID: 28560698
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gap-junction modulator
Tonabersat (SB-220453)是一种新颖的苯并吡喃衍生物,是一种gap-junction调节剂。
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Rac1 activation 抑制剂
SC 23766是Rac1-GEF相互作用的选择性抑制剂。通过Rac特异性鸟嘌呤核苷酸交换因子(GEF)TrioN和Tiam1(IC50为50 μM)阻止Rac1激活,而不影响Cdc42或RhoA激活。
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RSV fusion 抑制剂
TMC353121是一种有效的体外RSV融合抑制剂,pEC50 为 9.9。抗病毒药,也是治疗RSV疾病的新型候选药物。
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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
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Palifosfamide是具有潜在抗肿瘤活性的合成芥末化合物。
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TEMPOL是一种超氧化物歧化酶类似物,属于一类不含硫醇的辐射保护剂,并具有渗透膜的能力。
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HIV maturation 抑制剂
GSK2838232是一种新型的人类免疫病毒(HIV)成熟抑制剂,正在开发用于治疗慢性HIV感染。
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EGFR 抑制剂
AZD-9291 (Osimertinib)是第三代EGFR抑制剂,在临床前研究中显示出希望,并为已对现有EGFR抑制剂产生耐药性的晚期肺癌患者提供了希望。
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- Liu YN, .et al. Acquired resistance to EGFR tyrosine kinase inhibitors is mediated by the reactivation of STC2/JUN/AXL signaling in lung cancer, Int J Cancer, 2019, Jun 4 PMID: 31162839
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Hyperforin (solution in Ethanol)是一种植物化学物质,由金丝桃属植物的一些成员产生,特别是贯叶金丝桃(圣约翰草)。它抑制几种cyp450酶的活性,其中cyp2d6最敏感,ic50约为10微克/毫升。贯叶金丝桃素也是类固醇x受体(sxr)的配体。
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Ras-Raf interaction 抑制剂
Kobe0065抑制锚定依赖性和非依赖性生长,阻断MEK / ERK活性并诱导H-rasG12V转化的NIH3T3细胞凋亡。
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Rac GTPase Inhibitor
EHop-016 is a potent and specific inhibitor of Rac1 and Rac3 GTPase activity that inhibits Vav2 interaction with Rac, Rac-activated PAK1, lamellipodia formation, and cell migration.
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BMPS是一种短的巯基和氨基反应性异双功能交联剂。
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HIV-1 maturation 抑制剂
Bevirimat (PA-457,MPC-4326,YK FH312) 是HIV-1病毒颗粒成熟抑制剂。
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- Mingzhang Wang, .et al. Quenching protein dynamics interferes with HIV capsid maturation, Nat Commun, 2017, 8: 1779 PMID: 29176596
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NF-κB 抑制剂
JSH 23是NF-kB的抑制剂,可阻止其转运入细胞核(IC50 = 7.1 uM)。
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- Yu N, .et al. Low-Dose Radiation Promotes Dendritic Cell Migration and IL-12 Production via the ATM/NF-KappaB Pathway, Radiat Res, 2018, Apr;189(4):409-417 PMID: 29420126
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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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aspartic protease 抑制剂
Pepstatin A是一种有效的天冬氨酸蛋白酶抑制剂,还可以抑制HIV复制。
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eIF4F subunit interaction 抑制剂
4E1RCat是eIF4E:eIF4G和eIF4E:4E-BP1相互作用的双重抑制剂。
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NF-κB activation 抑制剂
Caffeic Acid Phenethyl Ester是一种有效且特异性的NF-κB活化抑制剂。
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Rac GTPase 抑制剂
NSC 23766是Rac特异性GEF TrioN和Tiam 1(IC50 = 50 uM)引起的Rac1激活的细胞可渗透性可逆抑制剂。
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KCa2.1 channels activator
GW 542573X是小电导Ca2+激活的K+通道(KCa2)的激活剂。
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neuronal differentiation inducer
Neuropathiazol是一种合成的小分子,可诱导成年海马神经祖细胞的神经元分化。
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IL-12/IL-23 inhibitor
Apilimod is a potent IL-12/IL-23 inhibitor, IL-12 production in cultures of IFN-r/LPS?Cstimulated human PBMCs is strongly inhibited by STA-5326 with an IC50 of 10 nM.
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CDK4/6 抑制剂
PD 0332991 Isethionate是CDK4/6的高选择性抑制剂,IC50分别为11 nM/16 nM。
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AMPA desensitization 抑制剂
Cyclothiazide是苯并噻二叠氮,可作为AMPA受体的增效剂,正向调节其对谷氨酸的响应(EC50 = 3.8 M)。
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NaV1.3 and NaV1.1 channels 抑制剂
ICA-121431是人NaV1.3和NaV1.1通道的有效和选择性抑制剂(IC50值分别为13和23 nM)。
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STAT 抑制剂
STAT5抑制剂是一种细胞可渗透的非肽烟酰yl,可通过靶向其SH2结构域(针对STAT5βSH2结构域EPO肽结合活性的IC50 = 47μM)来抑制STAT5。
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MIF Antagonist是MIF体外(IC50 = 7 μM)和细胞(IC50 = 25 μM)的多巴色素互变异构酶活性的抑制剂。
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