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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T5858	Sertindole Lu 23-174,舍吲哚	Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Autophagy	Autophagy; GPCR/G Protein; Neuroscience
	Sertindole (Lu 23-174) 是一种非典型抗精神病药，可与多巴胺 D2 受体和血清素受体亚型 5-HT1D、5-HT2A 和 5-HT2C 结合，Kd 值分别为 2.7、20、0.14 和 6 nM。
T83469	10m/ZS44
	10m/ZS44是一种能够穿透血脑屏障的Glioblastoma (GBM) 抑制剂，在小鼠异种移植模型中有效抑制了GBM肿瘤生长，并通过激活SIRT1/p53介导的细胞凋亡途径来抑制U251细胞增殖。
T36407	Pyrrolidine Ricinoleamide
	Ricinoleic acid is a naturally occurring 12-hydroxy fatty acid. It constitutes about 90% of the fatty acids in castor oil. Pyrrolidine Ricinoleamide is a derivative of the amide of ricinoleic acid that shows potent antiproliferative activity against an array of cancer cell lines, including human glioma U251 cells.
T36406	Pyrrolidine Linoleamide
	Linoleic acid is an essential fatty acid and one of the most abundant polyunsaturated fatty acids in the western diet. Pyrrolidine Linoleamide is a derivative of the amide of linoleic acid that shows potent antiproliferative activity against an array of cancer cell lines, including human glioma U251 cells. It is greater than 4-fold more effective against cancer cells than non-cancer cells.
T81967	KY386
	KY386为选择性DHX33 helicase抑制剂，IC50仅19 nM。针对U251-MG细胞（DHX33过表达癌细胞株）的抑制作用表现出相似效力，IC50为20 nM。该化合物展现出显著的抗癌活性及中等的代谢稳定性。
T36449	(S)-α-Methylbenzyl Ricinoleamide
	(S)-α-Methylbenzyl ricinoleamide is a fatty acid amide derived from ricinoleic acid and methyl benzylamine. It demonstrates potent growth inhibition of glioma (U251), breast (MCF-7), ovarian (NCI-ADR/RES and OVCAR-3), kidney (786-0), non-small cell lung (NCI-H460), and prostate (PC-3) cancer cells with a mean GI50 value of 6.9 μM.
T35558	KAAD-Cyclopamine
	Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated onco...
T83741	S7 TFA Leu-Ser-Leu-Iso-Thr-Arg-Leu-OH
	S7是一种IL-6受体的肽类拮抗剂，能够浓度依赖性地抑制IL-6与IL-6受体的结合。在C-33 A宫颈癌细胞和RPMI-8226 B细胞淋巴细胞中，S7 (50 µM) 能抑制IL-6诱导的VEGF水平增加。在每两天给药一次，剂量为50 mg/kg的条件下，S7能减少IL-6过表达的C-33 A宫颈癌小鼠异种移植模型中的肿瘤体积。当S7与半胱氨酸结合，并连接到包裹多柔比星的脂质纳米粒子(LNPs)表面时，能增强LNPs对胶质瘤的靶向性，并在U251胶质母细胞瘤小鼠异种移植模型中提高生存率。
T36241	Arecaidine propargyl ester (hydrobromide)
	Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecai...

化合物

Sertindole

Cat.No: T5858

Synonym: Lu 23-174,舍吲哚

Target: Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, Autophagy

Pyrrolidine Ricinoleamide

Cat.No: T36407

Synonym:

Target:

Pyrrolidine Linoleamide

(S)-α-Methylbenzyl Ricinoleamide

Synonym: Leu-Ser-Leu-Iso-Thr-Arg-Leu-OH

Target:

Arecaidine propargyl ester (hydrobromide)

Cat.No: T36241

Synonym:

Target:

Cat. No.	Product Name	Target	Signaling Pathways
T5784	Topotecan NSC 609669,拓扑替康,SKF 104864A	Topoisomerase; Autophagy	Autophagy; DNA Damage/DNA Repair
	Topotecan (NSC-609669) 是一种拓扑异构酶 I 抑制剂，通过抑制 DNA 拓扑异构酶起抗肿瘤作用，可用于治疗卵巢癌。
T32567	Lanuginosine Oxoxylopin,NSC-137553,Oxoxylopine,NSC137553,NSC 137553
	Lanuginosine, an aporphine alkaloid, exhibits cytotoxicity against U251.

天然产物

Topotecan

Cat.No: T5784

Synonym: NSC 609669,拓扑替康,SKF 104864A

Target: Topoisomerase, Autophagy

Lanuginosine

Cat.No: T32567

Synonym: Oxoxylopin,NSC-137553,Oxoxylopine,NSC137553,NSC 137553

Target:

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