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9

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T62807	AKT-IN-7
	AKT-IN-7 (compound 1-P1) 是一种 AKT 的有效抑制剂。AKT-IN-7 具有潜力进行癌症的研究。
T63455	PI3K/Akt/mTOR-IN-3
	PI3K/Akt/mTOR-IN-3 是 PI3K/Akt/mTOR 的有效抑制剂。PI3K/Akt/mTOR-IN-3 能够抑制 MCF-7 细胞 (IC50: 0.77 μM)、HeLa 细胞 (IC50: 1.23 μM) 和 HepG2 细胞(IC50: 4.57 μM)。PI3K/Akt/mTOR-IN-3 在 4 μM 浓度下可抑制 MCF-7 和 HeLa 细胞的迁移。PI3K/Akt/mTOR-IN-3 能够将细胞周期阻滞在 S 期，并诱导细胞凋亡 (apoptosis)。
T64041	PI3K/mTOR Inhibitor-7
	PI3K/mTOR Inhibitor-7 是有效的 PI3K/mTOR 双重抑制剂。PI3K/mTOR Inhibitor-7 的作用比 gedatolisib 高 4.7 倍，他们的 IC50 值分别为 1.4 μM 和 0.3 μM。10 μM 的 PI3K/mTOR Inhibitor-7 能够明显抑制 PI3K/Akt/mTOR 信号通路。PI3K/mTOR Inhibitor-7 对癌症疾病表现出研究潜力。
T69589	PX-316
	PX-316 is a AKT inhibior. PX-316, when administered intraperitoneally to mice at 150 mg/kg, inhibits Akt activation in HT-29 human tumor xenografts up to 78% at 10 h with recovery to 34% at 48 h. PX-316 has antitumor activity against early human MCF-7 breast cancer and HT-29 colon cancer xenografts in mice. PX-316 formulated in 20% hydroxypropyl-beta-cyclodextrin for intravenous administration is well tolerated in mice and rats with no hemolysis and no hematological toxicity. Thus, PX-316 is the...
T61990	Topoisomerase I/II inhibitor 3
	Topoisomerase I/II inhibitor 3 (化合物7) 是拓扑异构酶 I (Topo I)和 II (Topo II)的有效双抑制剂。通过抑制 PI3K/Akt/mTOR 信号通路，Topoisomerase I/II inhibitor 3抑制细胞增殖、侵袭和迁移，诱导细胞凋亡(apoptosis)。Topoisomerase I/II inhibitor 3 在肝癌中具有研究价值。
T78608	Anticancer agent 164	Apoptosis	Apoptosis
	CML-IN-1（compound 7）是一种高效抗癌药物，针对人类慢性粒细胞白血病（CML）细胞系K562，能有效诱导凋亡（apoptosis）。该化合物主要通过显著抑制PI3K/Akt信号通路的蛋白磷酸化来发挥作用，同时CML-IN-1（compound 4）也能通过抑制结直肠癌的MEK/ERK信号通路来阻止细胞增殖。
T36197	CAY10747
	CAY10747 is an inhibitor of the protein-protein interaction between heat shock protein 90 (Hsp90) and cell division cycle 37 (Cdc37) and a derivative of celastrol .1It decreases protein levels of the Hsp90-Cdc37 complex and the Hsp90-Cdc37 clients phosphorylated Akt and Cdk4 in A549 cells when used at a concentration of 5 μM. CAY10747 inhibits proliferation of A549, MCF-7, HOS, and HepG2 cells (IC50s = 0.41, 0.64, 0.9, and 0.94 μM, respectively) and induces apoptosis in A549 cells. 1.Li, N., Xu,...
T36991	Monascuspiloin
	Monascuspiloin is a fungal metabolite that has been found inM. pilosusM93-fermented rice.1It induces endoplasmic reticulum stress and autophagy in PC3 prostate cancer cells. Monascuspiloin (15-45 μM) decreases viability of PC3 cells and has an additive effect on the reduction in viability of PC3 cells induced by irradiation when used at a concentration of 25 μM. It induces intratumor apoptosis and autophagy and reduces tumor growth in a PC3 mouse xenograft model when administered at doses of 40 ...
T35527	PI3Kα-IN-4 PI3Kα-IN-4
	PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity[1]. PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ, with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively in kinase assays[1].PI3Kα-IN-4 inhibits PI3Kα, β, δ, and γ, with IC50s of 12.1,1393, 183, and >10000 nM, respectively in cell based assays[1]. PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit t...

化合物

Cat.No: T62807

PI3K/Akt/mTOR-IN-3

Cat.No: T63455

PI3K/mTOR Inhibitor-7

Cat.No: T64041

Cat.No: T69589

Topoisomerase I/II inhibitor 3

Cat.No: T61990

Anticancer agent 164

Cat.No: T78608

Target: Apoptosis

Cat.No: T36197

Cat.No: T36991

Cat.No: T35527

Synonym: PI3Kα-IN-4

Cat. No.	Product Name	Target	Signaling Pathways
T2789	Scutellarin 黄岑素,野黄芩苷,Breviscapin,Breviscapinun,Breviscapine,Scutellarein-7-glucuronide	Akt; HIV Protease; STAT	Cytoskeletal Signaling; JAK/STAT signaling; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
	Scutellarin (Scutellarein-7-glucuronide) 是从黄芩中分离的黄酮，可抑制破骨细胞中 RANKL 介导的 MAPK 和 NF-κB 信号通路，并下调 HCC 细胞中的 STAT3/Girdin/Akt 信号通路。
T6S0653	Linarin Buddleoflavonoloside,Buddleoside,Acacetin-7-O-rutinoside,Acaciin,Linarine,蒙花苷	TNF; AChE	Apoptosis; Neuroscience
	Linarin (Acacetin-7-O-rutinoside) 是一种选择性的乙酰胆碱酯酶 (AChE) 抑制剂，从薄荷花提取物中分离得到。
T3729	Ethyl gallate Nipagallin A,Phyllemblin,gallic acid ethyl ester,没食子酸乙酯	MMP; NF-κB; Akt; Antibacterial	Cytoskeletal Signaling; Microbiology/Virology; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Ethyl gallate (gallic acid ethyl ester) 是一种非类黄酮酚过氧化氢清除剂。
T6S1315	Oroxylin A 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether	Virus Protease; HIF/HIF Prolyl-Hydroxylase; Autophagy	Autophagy; Chromatin/Epigenetic; Metabolism; Microbiology/Virology
	Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮，具有较强的抗癌作用。

天然产物

Cat.No: T2789

Synonym: 黄岑素,野黄芩苷,Breviscapin,Breviscapinun,Breviscapine,Scutellarein-7-glucuronide

Target: Akt, HIV Protease, STAT

Cat.No: T6S0653

Synonym: Buddleoflavonoloside,Buddleoside,Acacetin-7-O-rutinoside,Acaciin,Linarine,蒙花苷

Target: TNF, AChE

Cat.No: T3729

Synonym: Nipagallin A,Phyllemblin,gallic acid ethyl ester,没食子酸乙酯

Target: MMP, NF-κB, Akt, Antibacterial

Cat.No: T6S1315

Synonym: 千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether

Target: Virus Protease, HIF/HIF Prolyl-Hydroxylase, Autophagy

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