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19

抑制剂 & 化合物

17

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12171	Nampt-IN-5	P450; NAMPT	Metabolism
	Nampt-IN-5 是烟酰胺磷酸核糖基转移酶抑制剂。它可抑制 A2780 和 COR-L23 细胞，IC50值分别为 0.7 nM 和 3.9 nM。它还抑制 CYP3A4 活性。
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。
T2617	SNS-314 Mesylate SNS-314	Aurora Kinase	Cell Cycle/Checkpoint; Chromatin/Epigenetic
	SNS-314 Mesylate (SNS-314) 是一种有效且特异性的极光激酶抑制剂，对极光激酶 A、B、C 的 IC50值分别为 9，31 和 3 nM。
T6690	T0901317 N-(2,2,2-三氟乙基)-N-[4-[2,2,2-三氟-1-羟基-1-(三氟甲基)乙基]苯基]苯磺酰胺	Apoptosis; FXR; Liver X Receptor; ROR	Apoptosis; Metabolism
	T0901317 是一种口服有效且高度选择性的LXR 激动剂，对 LXRα 的EC50为 20 nM。它激活FXR，EC50为 5 μM。它是RORα和RORγ双重反向激动剂，Ki 值分别为 132 nM 和 51 nM。它诱导细胞凋亡，并抑制低密度脂蛋白受体缺失小鼠动脉粥样硬化的发展。
T3102	NS-1619	Apoptosis; Potassium Channel	Apoptosis; Membrane transporter/Ion channel
	NS 1619 是 Ca2+激活的 K+(BK) 通道的激活剂，是一种高效的松弛剂，在血管和其他组织的几个平滑肌中的 EC50约为 10 – 30 μM。它抑制A2780卵巢癌细胞增殖并诱导细胞凋亡。
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。
T64273	Nampt-IN-10 TFA
	Nampt-IN-10 TFA (compound 4) 是一种磷酸核糖转移酶 (NAMPT) 抑制剂。Nampt-IN-10 TFA 对 A2780 (IC50: 5 nM) 和 CORL23 (IC50: 19 nM) 具有细胞效能。Nampt-IN-10 TFA 能够用做 ADCs 的非抗有丝分裂有效载荷。
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。
T70792	SPR519
	SPR519 is a potent dual inhibitor of PI3Kα and mTOR kinases with IC50 (PI3Kalpha) = 30 nM and IC50 (mTOR) = 10 nM. SPR519 exhibits an EC50 of low sub-micromolar range among various tested cancer cell lines such as A2780 (0.23 μM), PC3 (0.48 μM), and SKOV3 (0.50 μM).
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。
T74562	Nampt-IN-10 trihydrochloride
	Nampt-IN-10 trihydrochloride (compound 4) 为磷酸核糖转移酶 (NAMPT) 抑制剂。在A2780与CORL23细胞中展现出活性，IC50值依次为5和19 nM。Nampt-IN-10 trihydrochloride 同时作为抗体偶联活性分子 (ADC) 的非限制性有效载荷。
T74340	DNA crosslinker 4 dihydrochloride
	DNA crosslinker 4 (dihydrochloride) 作为高效的DNA小沟结合剂，对NCI-H460、A2780和MCF-7癌细胞表现出显著抑制活性，适用于抗癌研究。
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。
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...
T74338	DNA crosslinker 2 dihydrochloride
	DNA crosslinker 2 (dihydrochloride)为一种高效DNA小沟结合剂，其结合亲和力(ΔTm)达1.2°C。该化合物对NCI-H460、A2780及MCF-7癌细胞展示出抑制活性，适用于抗癌研究。
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....
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...
T80615	Enoticumab REGN421
	Enoticumab（REGN421，SAR153192）是一种针对人类Dll4的IgG1κ类型抗体。DLL4为Notch信号通路中的关键配体，其功能通过巨胞饮作用依赖的非转录调控机制影响长链脂肪酸的摄取。该抗体在卵巢癌异种移植模型中展示出明确的体内活性，其中EGN421（2.5mg/kg，周剂量）在小鼠皮下TOV-112D及腹膜内A2780人类肿瘤异种移植模型中实现了分别达到86%和83%的肿瘤生长抑制效果。

化合物

Cat.No: T12171

Target: P450, NAMPT

Cat.No: T2679

Synonym: BMS265246

Target: CDK

SNS-314 Mesylate

Cat.No: T2617

Synonym: SNS-314

Target: Aurora Kinase

Cat.No: T6690

Synonym: N-(2,2,2-三氟乙基)-N-[4-[2,2,2-三氟-1-羟基-1-(三氟甲基)乙基]苯基]苯磺酰胺

Target: Apoptosis, FXR, Liver X Receptor, ROR

Cat.No: T3102

Target: Apoptosis, Potassium Channel

Anticancer agent 17

Cat.No: T63354

NAMPT degrader-3

Cat.No: T79437

Target: NAMPT

Nampt-IN-10 TFA

Cat.No: T64273

Cat.No: T63110

Cat.No: T70792

P-gp inhibitor 13

Cat.No: T78974

Nampt-IN-10 trihydrochloride

Cat.No: T74562

DNA crosslinker 4 dihydrochloride

Cat.No: T74340

Cat.No: T74530

10'-Desmethoxystreptonigrin

Cat.No: T35607

DNA crosslinker 2 dihydrochloride

Cat.No: T74338

Oxaliplatin-d10

Cat.No: T71401

Cat.No: T71287

Cat.No: T80615

Synonym: REGN421

Cat. No.	Product Name	Target	Signaling Pathways
T5S0106	Peimisine 贝母辛,Ebeiensine	RAAS; AChR	Endocrinology/Hormones; Neuroscience
	Peimisine (Ebeiensine) 非竞争性拮抗气管平滑肌 M 受体，抑制 Ach 引起的平滑肌收缩。它兴奋 β 受体和拮抗内钙释放，促进一氧化氮释放，可舒张气管平滑肌，有平喘作用。
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。
TN5156	Totaradiol	NADPH-oxidase	Immunology/Inflammation
	Totaradiol shows antioxidant activity, it can inhibit linoleic acid autoxidation but not generation of superoxide anion. Totaradiol exhibits cytotoxic activity against the A2780 ovarian cancer cell line.
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...
TN2590	11alpha,12alpha-Oxidotaraxerol palmitate	Others	Others
	11alpha,12alpha-Oxidotaraxerol palmitate shows selective cytotoxicity against HCT-8, Bel-7402, BGC-823, A549 and A2780.
TN3383	α-Amyrin palmitate alpha-Amyrin palmitate	PKA	Tyrosine Kinase/Adaptors
	alpha-Amyrin palmitate is antiarthritic in the adjuvant model of arthritis in rats. alpha-Amyrin palmitate is a potent non-competitive inhibitor of chymotrypsin (Ki=6 microM), it also shows weak cytotoxicity against the A2780 human ovarian cancer cell line.
TN2913	3-Acetoxy-11-ursen-28,13-olide	Phosphatase	Metabolism
	3β-Acetoxy-urs-11-en-28,13-olide exhibits significant protein tyrosine phosphatase 1B (PTP1B) inhibitory activity, it is a mixed-type PTP1B inhibitor. It exhibits weak-moderate antiproliferative activity against the A2780 human ovarian cancer cell line.
TN3447	Arjunglucoside I
	Arjunglucoside I has anti-inflammatory activity, it exhibits significant activity against carrageenan-induced paw edema in rat. It also shows antiproliferative activity against the A2780 human ovarian cancer cell line with an IC(50) value of 1.2 microM.
T81686	Neotriptonoterpene
	Neotriptonoterpene 是一种从 T. regelii 分离得到的化合物，在 A2780、HepG2 和 MCF-7 细胞上具有较弱的细胞毒活性，其 IC50 值分别为 65.80 µM、35.45 µM 和 64.80 µM。
TN2936	3-Hydroxy-11-ursen-28,13-olide	Others	Others
	3β-Hydroxy-urs-11-en-28,13β-olide shows a potent concentration-independent cytoprotective effect against CCl4-induced injury on human hepatoma cell line relative to silymarin as a reference standard. It exhibits weak-moderate antiproliferative activity ag
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
TN5474	Bonducellin
	Bonducellin has anti-inflammatory activities, it can significantly and dose-dependently inhibit the inflammatory mediators; nitric oxide (NO), and cytokines [tumor necrosis factor (TNF)-alpha and interleukin (IL)-12. Bonducellin shows weak antimalarial ac
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: T5S0106

Synonym: 贝母辛,Ebeiensine

Target: RAAS, AChR

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

Cat.No: TN5156

Target: NADPH-oxidase

4-oxo-27-TBDMS Withaferin A

Cat.No: T35647

4-oxo Withaferin A

Cat.No: T36893

11alpha,12alpha-Oxidotaraxerol palmitate

Cat.No: TN2590

Target: Others

α-Amyrin palmitate

Cat.No: TN3383

Synonym: alpha-Amyrin palmitate

Target: PKA

3-Acetoxy-11-ursen-28,13-olide

Cat.No: TN2913

Target: Phosphatase

Arjunglucoside I

Cat.No: TN3447

Neotriptonoterpene

Cat.No: T81686

3-Hydroxy-11-ursen-28,13-olide

Cat.No: TN2936

Target: Others

Cat.No: TN4168

Target: Others

Cat.No: TN5474

Cat.No: TN3364

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

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