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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
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...

化合物

MRT-10

Cat.No: T23027

Synonym:

Target: Hedgehog/Smoothened

Linoleoyl Ethanolamide

Cat.No: T8425

Synonym:

Target: TRP/TRPV Channel

Sulfaphenazole

Cat.No: T4567

Synonym: Plisulfan,Raziosulfa,Depocid,磺胺苯吡唑,Depotsulfonamide

Target: P450, Antibacterial

Ketomethylenebestatin

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