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9

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2679	BMS-265246 BMS265246	CDK	Cell Cycle/Checkpoint
	BMS-265246 是一种有效的选择性 CDK1/2 抑制剂，对 CDK1/cyclin B 和 CDK2/cyclin E 的 IC50分别为6 nM 和9 nM。
T63354	Anticancer agent 17
	Anticancer agent 17 对 HeLa 细胞 (IC50: 0.19 μM) 和 A2780 细胞 (IC50: 0.09 μM) 具有有效抗癌作用。
T79437	NAMPT degrader-3	NAMPT	Metabolism
	NAMPTdegrader-3 (compound C5)，是一种依赖VHL和蛋白酶体途径降解NAMPT的化合物。该化合物展现出对A2780细胞的细胞毒性作用，并能抑制其增殖。
T63110	CBP/p300-IN-15
	CBP/p300-IN-15 (compound 13a) 是一种有效的 p300 (IC50: 2.5 nM) 和 CBP (IC50: 28.0 nM) 抑制剂。CBP/p300-IN-15 能够较好的抑制 OVCAR-3 细胞 (EC50: 0.865 μM) 和 A2780 细胞 (EC50: 2.71 μM)。 CBP/p300-IN-15 能够用于研究卵巢癌。
T78974	P-gp inhibitor 13
	P-gp inhibitor 13为P-gp抑制剂，能够逆转A2780/T细胞中P-糖蛋白介导的紫杉醇耐药。该抑制剂主要用于研究晚期急性髓性白血病。
T35607	10'-Desmethoxystreptonigrin
	10'-Desmethoxystreptonigrin is an antibiotic originally isolated from Streptomyces and a derivative of the antibiotic streptonigrin. It is active against a variety of bacteria, including S. aureus, S. faecalis, E. coli, K. pneumoniae, and P. vulgaris (MICs = 0.4, 1.6, 3.1, 3.1 and 0.4 μg/ml, respectively). 10'-Desmethoxystreptonigrin is cytotoxic to HCT116 colon and A2780 ovarian cancer cells (IC50s = 0.004 and 0.001 μg/ml, respectively), as well as HCT116 cells resistant to etoposide and tenipo...
T71401	Oxaliplatin-d10
	Oxaliplatin-d10 is intended for use as an internal standard for the quantification of oxaliplatin by GC- or LC-MS. Oxaliplatin is a platinum-containing DNA-crosslinking agent. It induces the formation of DNA inter- and intrastrand crosslinks and DNA-protein adducts, inhibits DNA and RNA synthesis, and induces apoptosis in cancer cells. Oxaliplatin is cytotoxic to cisplatin-sensitive A2780(1A9) and KB-3-1 cells and cisplatin-resistant A2780-E(80) and KB-CP20 cells (IC50s = 0.12, 0.39, 4.7, and 2....
T74530	GEM-5
	GEM-5为基于吉西他滨且含HIF-1α抑制剂(YC-1)的偶联物，IC50值为30 nM。此化合物能有效降低HIF-1α表达，并提高肿瘤抑制因子p53的表达量。GEM-5可诱导A2780细胞的凋亡(apoptosis)，进而抑制肿瘤生长。
T71287	CDKI-83
	CDKI-83 is a potent CDK9 inhibitor. The compound shows effective anti-proliferative activity in human tumour cell lines with GI50 <1 μM, and is capable of inducing apoptosis in A2780 human ovarian cancer cells as determined by the activated caspase-3, Annexin V/PI double staining and accumulated cells at the sub-G1 phase of cellcycle. The research results suggest that combined inhibition of CDK9 and CDK1 may result in the effective induction of apoptosis and CDKI-83 has the potential to be devel...

化合物

Cat.No: T2679

Synonym: BMS265246

Target: CDK

Anticancer agent 17

Cat.No: T63354

NAMPT degrader-3

Cat.No: T79437

Target: NAMPT

Cat.No: T63110

P-gp inhibitor 13

Cat.No: T78974

10'-Desmethoxystreptonigrin

Cat.No: T35607

Oxaliplatin-d10

Cat.No: T71401

Cat.No: T74530

Cat.No: T71287

Cat. No.	Product Name	Target	Signaling Pathways
T2851	Daphnetin 7,8-Dihydroxycoumarin,Daphnetol,瑞香素	EGFR; PKA; PKC; Parasite; Autophagy	Angiogenesis; Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors
	Daphnetin (7,8-Dihydroxycoumarin) 是从 Genus Daphne 中分离得到的香豆素衍生物，有抗氧化、抗炎、抗疟疾和解热作用，可用于凝血功能障碍、类风湿性关节炎等疾病的相关研究。
T35749	Thymohydroquinone Thymoquinol	Antioxidant; Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB; oxidation-reduction
	Thymohydroquinone (Thymoquinol) 是中药材百里香、牛至和其他唇形科植物中含有的单萜酚类化合物。 Thymohydroquinone 抑制癌细胞生长、减少氧化应激和调节炎症反应，在无细胞实验中清除2,2-二苯基-1-picrylhydrazyl 自由基(IC50 = 2.4 μg/ml)，在浓度为1.6至6.4 μg/ml 的氧自由基吸收能力(ORAC)实验中，它的Trolox 当量值为2.6胸腺对苯二酚对A2780、OVCAR-8和CIS-A2780卵巢癌细胞(IC50分别为3.1、8.9和9.8 μM)和人卵巢永生化上皮细胞(IC50 = 14 μM)的生长有抑制作用，体外对恶性疟原虫也有抑制作用(IC50 = 15.9 μM)。
T3S1265	Liriopesides B 山麦冬皂苷B,Nolinospiroside F	Others	Others
	Liriopesides B (Nolinospiroside F) 是一种甾体皂苷，分离自 Ophiopogon japonicas 中，具有抗氧化和抗衰老活性。
T4S0998	Trifolirhizin 红车轴草根甙/三叶豆紫檀苷,三叶豆紫檀苷	TNF; Tyrosinase	Apoptosis; Proteases/Proteasome
	Trifolirhizin 是一种从苦参根中分离出的 pterocarpan 黄酮类化合物。它具有酪氨酸酶高抑制活性，IC50=506 μM。它具有抗炎和抗癌的潜能。
T35647	4-oxo-27-TBDMS Withaferin A
	4-oxo-27-TBDMS Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.1 It is cytotoxic to A2780 ovarian cancer cells (IC50 = 17 μM) but not to carboplatin-resistant A2780 (A2780/CP70) cells (IC50 = >100 μM). It is selective for A2780 cells over non-cancerous ARPE19 cells (IC50 = 1,660 μM). 4-oxo-27-TBDMS Withaferin A induces DNA fragmentation in A2780 cells.References1. Perestelo, N.R., Llanos, G.G., Reyes, C.P., et al. Expanding the chemical space of wi...
T36893	4-oxo Withaferin A
	4-oxo Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.1 It is cytotoxic to A2780 ovarian cancer cells and carboplatin-resistant A2780 (A2780/CP70) cells (IC50s = 7.3 and <1 μM, respectively) and is 4.4-fold selective for A2780 cells over non-cancerous ARPE19 cells.References1. Perestelo, N.R., Llanos, G.G., Reyes, C.P., et al. Expanding the chemical space of withaferin A by incorporating silicon to improve its clinical potential on human ovarian ca...
TN4168	Grifolin	Others	Others
	Grifolin has anti-cancer effects, it induces apoptosis and promotes cell cycle arrest in the A2780 human ovarian cancer cell line via inactivation of the ERK1/2 and Akt pathways; it enhances the differentiation and proliferation of oligodendrocyte precurs
TN3364	Agrimonolide	Apoptosis; Dehydrogenase; p38 MAPK; ROS; JAK	Angiogenesis; Apoptosis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; MAPK; Metabolism; Stem Cells
	Agrimonolide 是一种来自异香豆素的化合物，主要存在于草药Agrimonia pilosa Ledeb 中，具有显著的生物活性。Agrimonolide 通过抑制脂多糖（LPS）诱导的JAK-STATs 和p38 MAPKs 信号通路的激活而发挥抗炎作用。Agrimonolide 及其衍生物去甲阿戈莫内德已显示出能够有效提高肝细胞中胰岛素介导的糖原水平，可能在调节胰岛素抵抗的HepG2细胞中发挥关键作用。Agrimonolide 通过靶向卵巢癌细胞中的SCD1，对癌症的进展和诱导细胞死亡和凋亡表现出抑制作用。特别是，Agrimonolide 对A2780和SKOV-3细胞的增殖、迁移和侵袭表现出剂量依赖性的抑制，同时促进细胞凋亡。该化合物还被发现能诱导铁介导的细胞死亡，同时增加活性氧（ROS）和总铁的水平。Agrimonolide 很容易穿过血脑屏障，表明其在神经系统疾病的治疗应用方面具有潜力。

天然产物

Cat.No: T2851

Synonym: 7,8-Dihydroxycoumarin,Daphnetol,瑞香素

Target: EGFR, PKA, PKC, Parasite, Autophagy

Thymohydroquinone

Cat.No: T35749

Synonym: Thymoquinol

Target: Antioxidant, Reactive Oxygen Species

Cat.No: T3S1265

Synonym: 山麦冬皂苷B,Nolinospiroside F

Target: Others

Cat.No: T4S0998

Synonym: 红车轴草根甙/三叶豆紫檀苷,三叶豆紫檀苷

Target: TNF, Tyrosinase

4-oxo-27-TBDMS Withaferin A

Cat.No: T35647

4-oxo Withaferin A

Cat.No: T36893

Cat.No: TN4168

Target: Others

Cat.No: TN3364

Target: Apoptosis, Dehydrogenase, p38 MAPK, ROS, JAK

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