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Cat. No. | Product Name | Target | Signaling Pathways |
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T23027 |
MRT-10
|
Hedgehog/Smoothened | GPCR/G Protein; Stem Cells |
MRT 10 是一种七跨膜平滑受体 (Smo) 拮抗剂,通过多种 Hedgehog (Hh) 测定,其IC50=0.65 μM。它与Smo 受体结合的位点是 Bodipycyclopamine。它可用于研究癌症。 | |||
T68594 | NFAT:AP-1 inhibitor-10 | ||
NFAT:AP-1 inhibitor-10 is a novel inhibitor of the NFAT:AP-1:DNA interaction on the ARRE-2 element, binding to DNA in a sequence-selective manner and inhibiting the transcription of the Il2 gene and several other cyclosporin A-sensitive cytokine genes important for the effector immune response. | |||
T8425 |
Linoleoyl Ethanolamide
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
Linoleoyl ethanolamide 是脂肪酸乙醇酰胺。它可弱结合 CB1 和 CB2 受体,并分别抑制[3H]CP-55,940的结合,Ki 分别为 10 和 25μM。它在引起小鼠过氧化氢酶方面的效力是 anandamide 的4倍,且对睡眠时间无延长效果。 | |||
T4567 |
Sulfaphenazole
Plisulfan,Raziosulfa,Depocid,磺胺苯吡唑,Depotsulfonamide |
P450; Antibacterial | Metabolism; Microbiology/Virology |
Sulfaphenazole (Plisulfan) 是一种 CYP2C9的特异性抑制剂,抑制 CYP2C9介导的亚油酸动脉粥样硬化和促炎症效应,增加 AP-1的氧化应激和激活。 | |||
T25573 |
Ketomethylenebestatin
|
||
Ketomethylenebestatin is a carba-analog of bestatin,the aminopeptidase (AP) inhibitor. Ketomethylenebestatin is 10 fold less effective as an inhibitor of aminopeptidases than bestatin. | |||
T83856 |
AP-1
|
||
AP-1是一种微型化的蛋白质水解靶向嵌合体(PROTAC),由吲哚美辛(±)连接的间变性淋巴瘤激酶(ALK)配体和E3泛素连接酶配体通过超短连接器相连。在10至300 nM浓度范围内使用时,AP-1能高效降解Karpas-299细胞中高表达的ALK融合蛋白NPM-ALK,此效应可被蛋白酶体抑制剂MG-132阻断。它还能降解在SN-N-SH和NCI H3122细胞中表达的ALK融合蛋白EML4-ALK及含有苯丙氨酸至亮氨酸替换突变(ALKF1174L)的ALK。AP-1对依赖ALK的Karpas-299细胞具有细胞毒性(IC50 = 0.1265 nM),但对非ALK依赖的THP-1细胞无细胞毒性(IC50 = 2,704 nM)。在给药剂量为25, 50, 和100 mg/kg时,能减小NCI H3122小鼠移植瘤模型中的肿瘤体积。 | |||
T70063 |
GYKI 52466 HCl
|
||
GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of general... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TQ0185 |
14-Deoxy-11,12-didehydroandrographolide
AP10,14-脱氧-11,12-二去氢穿心莲内酯,14-dehydro Andrographolide |
NF-κB | NF-κB |
14-Deoxy-11,12-didehydroandrographolide (AP10) 是一种 Andrographolide 的类似物,能够抑制 NF-κB 活性。 | |||
TN5639 |
Rocaglaol
Ferrugin,Aglaiastatin A |
||
Rocaglaol is a potent anticancer drug that induces apoptosis of LNCaP cells through the mitochondrial pathway and its G2/M-phase cell cycle arrest is associated with the down-regulation of Cdc25C and the dephosphorylation of Cdc2. Rocaglaol can reduce tis |