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19

抑制剂 & 化合物

24

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T22223	3PO	Glucokinase; Autophagy	Autophagy; Metabolism
	3PO 是一种 PFKFB3 的小分子抑制剂，IC50值为22.9 μM。它抑制几种人类恶性造血和腺癌细胞系的增殖，IC50在1.4到24 μM 之间。它抑制葡萄糖摄取，并降低 Fru-2,6-BP、乳酸、ATP、NAD+ 和 NADH 的细胞内浓度。
T12854	SBI-797812	NAMPT	Metabolism
	SBI-797812 是在结构上类似于活性位点定向的 NAMPT 抑制剂的化合物，能够阻断这些抑制剂与 NAMPT 的结合。它将 NAMPT 反应平衡转向 NMN 形成，提高 NAMPT 对 ATP 的亲和力，稳定 His247 处的磷酸化 NAMPT，增加焦磷酸盐副产物的消耗，并通过 NAD+钝化反馈抑制。
TNU0031	5-Hydroxyuridine OHUrd	Nucleoside Antimetabolite/Analog	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	5-Hydroxyuridine (OHUrd) 是一种嘌呤核苷类似物，具有潜在的抗肿瘤活性，对人结肠腺癌细胞系显示出细胞毒。
T62281	PARP-1-IN-2	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	PARP-1-IN-2 是一种有效且可透过血脑屏障的 PARP1 抑制剂（IC50： 149 nM）。PARP-1-IN-2 在细胞实验中对人肺腺癌上皮细胞系 A549 显示出显著的抗增殖活性。PARP-1-IN-2 可诱导 A549 细胞凋亡。
T76873	Nidanilimab CAN04	IL Receptor	Immunology/Inflammation
	Nidanilimab (CAN04) 是一种完全人源化的 IL1RAP 单克隆抗体，其 Kd 值为 1.10 pM。Nidanilimab 具有抗肿瘤活性，切断 IL1α 和 IL1β 信号通路，并诱导免疫系统破坏肿瘤细胞。Nidanilimab 可用于研究非小细胞肺癌 (NSCLC) 和胰腺导管腺癌 (PDAC) 等实体癌。
T36083	DS-7423	PI3K; mTOR	PI3K/Akt/mTOR signaling
	DS-7423 是PI3K 和mTOR 的有效抑制剂，抑制PI3Kα 和 mTOR 的IC50分别为15.6 nM 和 34.9 nM。DS-7423表现出抗癌活性。
T71060	IST-622
	IST-622 is a unique topoisomerase inhibitor, showing significant growth-inhibitory effects against large-cell lung cancer (Lu-116) and gastric adenocarcinoma (St-4).
T61806	Antitumor agent-44
	Antitumor agent-44 (Compound 5n) elicits potent antitumor effects by inducing disruption of mitochondrial homeostasis, cell cycle arrest, and apoptosis in human adenocarcinoma cells. Moreover, Antitumor agent-44 demonstrates significant anti-tumor activity in a lung cancer cell xenograft mice model [1].
T10588	BPI-9016M	Others	Others
	BPI-9016M is an effective, orally active, and selective dual inhibitor of c-Met and AXL tyrosine kinases. It suppresses tumor cell growth, invasion, and migration of lung adenocarcinoma.
T70646	Deltarasin HCl
	Deltarasin is a high affinity PDEδ-KRAS interaction inhibitor. Deltarasin can inhibit KRAS-PDEδ interactions by binding to a hydrophobic pocket on PDEδ, resulting in the impairment of cell growth, KRAS activity, and RAS/RAF signaling in human pancreatic ductal adenocarcinoma cell lines. The anti-cancer cell activity of deltarasin can be enhanced by simultaneously blocking tumor protective" autophagy
T77180	Retifanlimab
	Retifanlimab为一种抗程序性细胞死亡蛋白1(anti-PD-1)单克隆抗体(mAb)，主要用于胃食道腺癌(GEA)的研究。
T76855	Gresonitamab
	Gresonitamab (AMG 910) 是一种半衰期延长 (HLE) 双特异性 T 细胞接合物 (BiTE) 抗体，靶向 CD3阳性 T 细胞和表达 CLDN18.2的肿瘤细胞。Gresonitamab 可用于腺癌的研究。
T38302	Chrysomycin B
	Chrysomycin B 是分离自链霉菌的一种抗生素。Chrysomycin B 能引起人肺腺癌 A549 细胞系的 DNA 损伤，并抑制拓扑异构酶 II。
T82605	DB21, Galectin-1 Antagonist	Galectin	Immunology/Inflammation
	DB21, Galectin-1 Antagonist 是一种用于抑制galectin-1 (GAL1)与细胞表面聚糖结合的二苯并呋喃缀合肽模拟物。在黑色素瘤、肺腺癌和卵巢癌模型中，该化合物能增强血管生成和肿瘤生长的抑制效果。
T9660	Bexlosteride
	Bexlosteride (LY300502) 是一种苯并喹啉酮类人 I 型 5α-还原酶抑制剂。Bexlosteride 在 LNCaP 细胞培养物中显示出代谢抑制、抗增殖和抗分泌作用。Bexlosteride 可用于前列腺癌的研究。
T62510	Antitumor agent-75
	Antitumor agent-75 是一种新型的、有效的抗肿瘤剂。Antitumor agent-75 对癌症和正常人类细胞系具有细胞毒性作用。Antitumor agent-75 结合使用 Antitumor agent-74 时对人肺腺癌（细胞系 A549 ）表现出高度选择性的细胞毒作用 (IC50: 2.8 μM)。Antitumor agent-75 能够用于研究癌症。
T71783	Oxythiamine chloride HCl
	Oxythiamine chloride HCl is a thiamine antimetabolite that has anticancer activities. It is converted by thiamine pyrophosphokinase to oxythiamine pyrophosphate, a transketolase inhibitor. Oxythiamine decreases transketolase activity in breast cancer. It inhibits the nonoxidative synthesis of ribose and decreases RNA and DNA synthesis in pancreatic cancer. In vivo, oxythiamine induces cell cycle arrest at the G1 phase and apoptosis in an adenocarcinoma model. Oxythiamine, in combination with sor...
T79353	P-gp/BCRP-IN-2
	P-gp/BCRP-IN-2（化合物15）为恶二唑衍生物，作为ABC转运蛋白P-glycoprotein（IC50：1.6 nM）及BCRP（IC50：600 nM）的双重抑制剂。该化合物增强了Doxorubicin针对耐药型人腺癌结肠癌细胞系HT29/DX及MDCK-MDR1细胞的抗增殖效果。
T36846	Chromomycin A2
	Chromomycin A2 is an aureolic acid that has been found in several marine actinomycetes and has antibacterial and anticancer activities. Chromomycin A2 inhibits the growth of B. subtilis in an agar diffusion assay. It also inhibits the growth of human SGC7901 gastric cancer, HepG2 hepatocellular carcinoma, A549 lung epithelial adenocarcinoma, HCT116 colon cancer, and COC1 ovarian cancer cells, as well as human umbilical vein endothelial cells (HUVECs; IC50s = 4, 0.5, 3, 5, 5, and 8 nM, respective...

化合物

Cat.No: T22223

Target: Glucokinase, Autophagy

Cat.No: T12854

Target: NAMPT

5-Hydroxyuridine

Cat.No: TNU0031

Synonym: OHUrd

Target: Nucleoside Antimetabolite/Analog

Cat.No: T62281

Target: PARP

Cat.No: T76873

Synonym: CAN04

Target: IL Receptor

Cat.No: T36083

Target: PI3K, mTOR

Cat.No: T71060

Antitumor agent-44

Cat.No: T61806

Cat.No: T10588

Target: Others

Cat.No: T70646

Cat.No: T77180

Cat.No: T76855

Cat.No: T38302

DB21, Galectin-1 Antagonist

Cat.No: T82605

Target: Galectin

Cat.No: T9660

Antitumor agent-75

Cat.No: T62510

Oxythiamine chloride HCl

Cat.No: T71783

Cat.No: T79353

Cat.No: T36846

Cat. No.	Product Name	Target	Signaling Pathways
T1166	Ellipticine 玫瑰树碱,NSC 71795,Elliptisine	Topoisomerase	DNA Damage/DNA Repair
	Ellipticine (Elliptisine) 是一种有效的抗肿瘤剂，抑制 DNA 拓扑异构酶 II 活性，对白血病、神经母细胞瘤和胶质母细胞瘤有部分活性。
TN1620	Eriocalyxin B 毛萼乙素	Apoptosis; cAMP; NF-κB; STAT	Apoptosis; GPCR/G Protein; JAK/STAT signaling; NF-κB; Stem Cells
	Eriocalyxin B 是从中草药枇杷素中分离得到的一种二萜类天然产物，可诱导细胞凋亡，具有抗癌和抗炎作用。
T4672	Brevilin A	Apoptosis; Anti-infection; JAK; STAT; Autophagy	Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; JAK/STAT signaling; Microbiology/Virology; Stem Cells
	Brevilin A 是从Centipeda minima 中分离的倍半萜内酯，具有抗癌活性。它通过线粒体途径和 PI3K/AKT/mTOR 失活诱导结肠腺癌细胞 CT26 的凋亡和自噬。它是一种选择性JAK-STAT 信号通路抑制剂，通过减弱 JAK 信号和阻塞 STAT3 信号起作用。
TMA1841	Dihydrodaidzin	Others	Others
	Dihydrodaidzin shows cytotoxic activities against human stomach carcinoma (Hs 740.T, Hs 756 T), breast adenocarcinoma (Hs 578 T, Hs 742.T), and prostate carcinoma (DU 145, LNCaP-FGC) cell lines.
T70955	Vinaxanthone SM-345431	Phospholipase; Antibacterial	Metabolism; Microbiology/Virology
	Vinaxanthone (SM-345431) 是一种从青霉菌中提取的小分子化合物，是一种具有选择性和有效性的 semaphorin3A、phospholipase C (PLC) 和 FabI 抑制剂，抑制semaphorin3A 和 FabI。Vinaxanthone 具有抗菌活性，阻止细胞内脂肪酸合成，抑制金黄色葡萄球菌的生长。
TN1872	Linderone	Others	Others
	Linderone A shows anticancer activity against A549 non-small cell lung cancer cells and PC-3 prostate adenocarcinoma cell line.
TN1464	Camellianin A	RAAS	Endocrinology/Hormones
	Camellianin A has anticancer activity, it can inhibit the proliferation of the human hepatocellular liver carcinoma Hep G2 and human breast adenocarcinoma MCF-7 cell lines in a dose-dependent manner and induce the significant increase of the G0/G1 cell po
TN1523	Conicasterol	Others	Others
	Conicasterol displays marked cytotoxic activity against human breast adenocarcinoma cell line (MCF-7) with the IC50 value of 6.23 ug/mL.
TN3465	Atalantoflavone	Antifection	Microbiology/Virology
	Atalantoflavone shows urease inhibitory potential. It displays weak cytotoxic activity against the human Caucasian prostate adenocarcinoma cell line PC-3.
TN4355	Jolkinol A	Others	Others
	Jolkinol A can inhibit both MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) cell lines, with GI50 values ranging between 40.9 microM and 95.3 microM.
TN4352	Jatamanvaltrate B	Others	Others
	Jatamanvaltrate B shows cytotoxicity against lung adenocarcinoma (A549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8),and hepatoma (Bel7402) cell lines.
TN2529	1-Decarboxy-3-oxo-ceanothic acid	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	1-Decarboxy-3-oxo-ceanothic acid shows in vitro cytotoxic activity in a human ovarian adenocarcinoma cell line, the cytotoxic effect is mediated, at least in part, by the induction of apoptosis. It shows cytotoxic against OVCAR-3 and HeLa cancer cell line
TN2493	1,4,5,6-Tetrahydroxy-7-prenylxanthone	Others	Others
	1,4,5,6-Tetrahydroxy-7-prenylxanthone has anti-cancer activity, it shows moderate cytotoxicities against breast cancer (MDA-MB-435S) and lung adenocarcinoma (A549) cell lines; it also exhibits moderate activities with GI50 (Growth inhibitory) values of 2.
TN2492	1,4,5,6-Tetrahydroxy-7,8-diprenylxanthone	Others	Others
	1,4,5,6-Tetrahydroxy-7,8-diprenylxanthone has moderate cytotoxicities against breast cancer (MDA-MB-435S) and lung adenocarcinoma (A549) cell lines, but lacks antifungal activity against Candida albicans.
TN3646	Chlorovaltrate K	Others	Others
	Chlorovaltrate K shows moderate cytotoxicity against lung adenocarcinoma (A 549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8) and hepatoma (Bel 7402) cell lines with IC50 values of 0.89-9.76 uM.
TN5249	Volvaltrate B	Others	Others
	Volvaltrate B shows cytotoxic activity against the lung adenocarcinoma (A549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8), and hepatoma (Bel7402) cell lines, with IC50 values of 8.5, 2.0, 3.2, and 6.1 uM, respectively.
T81452	Pixinol
	Pixinol，天然糖苷，对GLC4人肺癌细胞株和COLO 320腺癌细胞株显示出细胞毒性，IC50值分别为71 µM与43 µM。
TN2945	3-Hydroxybakuchiol	ATPase; Caspase	Apoptosis; Membrane transporter/Ion channel; Proteases/Proteasome
	3-Hydroxybakuchiol exerts cytotoxic and anti-proliferative effects on the TA3/Ha mouse mammary adenocarcinoma cell line and induces a decrease in the mitochondrial transmembrane potential, the activation of caspase-3, the opening of the mitochondrial perm
TN2684	2,3,23-Trihydroxy-12-oleanen-28-oic acid	Others	Others
	2β,3β,23α-Trihydroxy-12-oleanen-28-oic acid shows cytotoxic activities to human lung adenocarcinoma(A-549)cell lines. 2α,3β,23-Trihydroxyolean-12-en-28-oic acid and 2α,3β,23-trihydroxyurs-12-en-28-oic acid exhibit cytotoxicity in vitro against the growth of human cancer cells lines HepG-2,with IC50 values of 16.13 ± 3.83, 15.97 ± 2.47 uM, respectively.
TN1646	Flemiphilippinin A	Others	Others
	Flemiphilippin A has antioxidant activity, it shows DPPH radical scavenging activity with effective half maximal concentration (EC50) of 18.36 ug/mL. Flemiphilippinin A (5 ug/mL) exhibits some level of antitumor activity against human hepatocellular carci
TN3009	4',5,7-Trihydroxy-6-prenylflavone	Others	Others
	6-Prenylapigenin(4',5,7-Trihydroxy-6-prenylflavone) shows potent inhibitory activity on melanin formation, it may be potential sources for skin whitening agents. It also shows moderate cytotoxicities against breast cancer (MDA-MB-435S) and lung adenocarci
TN5264	Xanthoxyletin	TNF; NOS; ROS; COX; Antifection	Apoptosis; Immunology/Inflammation; Microbiology/Virology; Neuroscience
	Xanthoxyletin shows potent antibacterial, fungicidal, and algicidal properties, it also has anticancer, and anti-inflammatory activities. It shows an inhibitory effect on iNOS protein expression at 10 microM, it also can inhibit the synthesis of nitric oxide and the protein expression of tumor necrosis factor-alpha and cyclooxygenase-2. Xanthoxyletin induces S phase arrest and apoptosis in human gastric adenocarcinoma SGC-7901 cells, the effects are associated with the DNA damage, apoptosis thro...
T81201	Sartorypyrone B
	Sartorypyrone B为Chevalone C的2β-乙酰氧基衍生物，由海绵源真菌Neosartorya tsunodae(KUFC 9213)的培养物中乙酸乙酯提取得到。该化合物对MCF-7、NCI-H460和A375-C5细胞系展示出较强的生长抑制活性，GI50s值分别为17.8、20.5和25.0 μM，显示其在乳腺癌、非小细胞肺癌和黑色素瘤研究中的应用潜力。
T36179	Aspulvinone O
	Aspulvinone O is a fungal metabolite that has been found in P. variotti and has antioxidant and anticancer activities.1,2 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 11.6 μM).1 Aspulvinone O inhibits aspartate transaminase 1 (GOT1; Kd = 3.32 μM) and is cytotoxic to PANC-1, AsPC-1, and SW1990 pancreatic cancer cells (IC50s = 20.54-26.8 μM).2 It reduces the oxygen consumption rate (OCR) and induces apoptosis in SW1990 cells. Aspulvinone O (2.5 and 5 mg/kg) redu...

天然产物

Cat.No: T1166

Synonym: 玫瑰树碱,NSC 71795,Elliptisine

Target: Topoisomerase

Cat.No: TN1620

Synonym: 毛萼乙素

Target: Apoptosis, cAMP, NF-κB, STAT

Cat.No: T4672

Target: Apoptosis, Anti-infection, JAK, STAT, Autophagy

Cat.No: TMA1841

Target: Others

Cat.No: T70955

Synonym: SM-345431

Target: Phospholipase, Antibacterial

Cat.No: TN1872

Target: Others

Cat.No: TN1464

Target: RAAS

Cat.No: TN1523

Target: Others

Atalantoflavone

Cat.No: TN3465

Target: Antifection

Cat.No: TN4355

Target: Others

Jatamanvaltrate B

Cat.No: TN4352

Target: Others

1-Decarboxy-3-oxo-ceanothic acid

Cat.No: TN2529

Target: DNA/RNA Synthesis

1,4,5,6-Tetrahydroxy-7-prenylxanthone

Cat.No: TN2493

Target: Others

1,4,5,6-Tetrahydroxy-7,8-diprenylxanthone

Cat.No: TN2492

Target: Others

Chlorovaltrate K

Cat.No: TN3646

Target: Others

Cat.No: TN5249

Target: Others

Cat.No: T81452

3-Hydroxybakuchiol

Cat.No: TN2945

Target: ATPase, Caspase

2,3,23-Trihydroxy-12-oleanen-28-oic acid

Cat.No: TN2684

Target: Others

Flemiphilippinin A

Cat.No: TN1646

Target: Others

4',5,7-Trihydroxy-6-prenylflavone

Cat.No: TN3009

Target: Others

Cat.No: TN5264

Target: TNF, NOS, ROS, COX, Antifection

Sartorypyrone B

Cat.No: T81201

Cat.No: T36179

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