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16

抑制剂 & 化合物

14

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T5007	Benproperine phosphate 磷酸苯丙哌林,Blascorid,Pirexyl phosphate	Others; Microtubule Associated	Cytoskeletal Signaling; Others
	Benproperine phosphate (Pirexyl phosphate) 是一种具有口服活性的，肌动蛋白相关蛋白 2/3 复合亚基 2 (ARPC2) 抑制剂。它通过削弱 Arp2/3 功能来减弱肌动蛋白的聚合反应速率。它可抑制癌细胞迁移和肿瘤转移，有用于治疗止咳的潜力。
T28865	STAT3-IN-B9 STAT3 IN B9,B9	STAT	JAK/STAT signaling; Stem Cells
	STAT3-IN-B9 (B9) 是异常 STAT3 激活的抑制剂，可抑制 MDA-MB-468、MDA-MB-231 和 DU145 等肿瘤细胞的增殖。
T67935	Tubulin inhibitor 11	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	Tubulin inhibitor 11 是一种口服活性的有效微管蛋白抑制剂。它通过靶向秋水仙碱结合位点，抑制tubulin聚合，进而促进有丝分裂阻断和apoptosis。
T36969	ARN24139
	ARN24139 is a topoisomerase II poison (IC50= 7.3 μM in a topoisomerase II decatenation assay).1It inhibits proliferation of DU145, HeLa, and A549 cells (IC50s = 4.7, 3.8, and 3.1 μM, respectively). 1.Arencibia, J.M., Brindani, N., Franco-Ulloa, S., et al.Design, synthesis, dynamic docking, biochemical characterization, and in vivo pharmacokinetics studies of novel topoisomerase II poisons with promising antiproliferative activityJ. Med. Chem.63(7)3508-3521(2020)
TP2128	R8-T198wt
	Cell-permeable peptide inhibitor of Pim-1 kinase, derived from p27Kip1. Inhibits Pim-1 phosphorylation of p27Kip1 and Bad; induces cell cycle arrest (at G1) and apoptosis in DU145 prostate cancer cells. Also inhibits Pim-1-dependent growth of DU145 cells
T70962	MHY219
	MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. M...
T35940	Darinaparsin Dimethylarsinic glutathione,Darinaparsin
	Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 &#181M) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 &#181M), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 &#181M, respectively). [1][2] It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase. Darinaparsin decreases transcription of Gli-2,...
T40212	ATR-IN-4
	ATR-IN-4, a potent inhibitor of ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase), restricts the growth of DU145 prostate cancer cells and NCI-H460 lung cancer cells, with IC 50 values of 130.9 nM and 41.33 nM, respectively.
T36905	Nanangenine F
	Nanangenine F is a drimane sesquiterpene fungal metabolite that has been found inA. nanangensis.1It is active againstB. subtilis(IC50= 78 μg/ml) and cytotoxic to NS-1, DU145, and MCF-7 cancer and NFF non-cancerous cells (IC50s = 49, 95, 49, and 84 μg/ml, respectively). 1.Lacey, H.J., Gilchrist, C.L.M., Crombie, A., et al.Nanangenines: Drimane sesquiterpenoids as the dominant metabolite cohort of a novel Australian fungus, Aspergillus nanangensisBeilstein J. Org. Chem.152631-2643(2019)
T79662	STAT3-IN-20	STAT	JAK/STAT signaling; Stem Cells
	STAT3-IN-20（Compound 40）是一种选择性地靶向STAT3的SH2结构域，展现了在DU145和MDA-MB-231癌细胞中的抗增殖效果（IC50分别为2.97 μM和3.26 μM），并诱导细胞周期停滞与细胞凋亡。该抑制剂有效抑制了STAT3的磷酸化、核内易位及其下游基因的转录活性（IC50: 0.65 μM）。
T36968	ARN-21934	Topoisomerase	DNA Damage/DNA Repair
	ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂，具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM，ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。
T15205	EL-102 EL102	Microtubule Associated; HIF	Angiogenesis; Chromatin/Epigenetic; Cytoskeletal Signaling
	EL-102 是一种 HIF1α 抑制剂，具有抗癌活性，可抑制微管蛋白聚合，可用于研究前列腺癌。
T70856	3-Oxobetulin Acetate
	3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor betulin. It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50 = 0.12 µg/ml), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s = 8, 10.6, 5.2, and 12.7 µg/ml, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s = >10 µg/ml for both). 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblasto...
T36195	CAY10744
	CAY10744 is a topoisomerase II-α poison.1 It inhibits topoisomerase II-α by 78.9% when used at a concentration of 20 μM. CAY10744 is selective for topoisomerase II-α over topoisomerase I providing 100 and 0% inhibition, respectively, at 100 μM. It inhibits proliferation of HCT15 colon, T47D breast, DU145 prostate, and HeLa cervical cancer cells (IC50s = 0.014, 0.00267, 0.072, and 2.46 μM, respectively). CAY10744 induces apoptosis in T47D cells when used at concentrations of 10 and 30 μM. CAY1074...
T35437	(-)-Viriditoxin
	(-)-Viriditoxin is a mycotoxin originally isolated from A. viridinutans that has antibacterial and antiproliferative activity. It is active against methicillin-sensitive and -resistant S. aureus (MSSA and MRSA, respectively), tetracycline-sensitive and -resistant Staphylococcus, vancomycin-sensitive and -resistant Enterococcus, and penicillin-sensitive and -resistant S. pneumoniae (MICs = 2-32 μg/ml). (-)-Viriditoxin is also active against fish pathogens, including S. iniae and S. parauberis (MI...
T15362	FX-11 LDHA Inhibitor FX11	Dehydrogenase	Metabolism
	FX-11 (LDHA Inhibitor FX11) 是一种有效的、选择性的和竞争性的乳酸脱氢酶 A (LDHA) 的特异性抑制剂，对LDHA 的Ki 为 8 μM。FX-11 对PKM2 (丙酮酸激酶 M2)具有激活作用。FX-11 可降低 ATP 水平，诱导氧化应激和ROS 生成，可引起细胞死亡。FX-11 在淋巴瘤和胰腺癌异种移植过程中表现出抗肿瘤活性。

化合物

Benproperine phosphate

Cat.No: T5007

Synonym: 磷酸苯丙哌林,Blascorid,Pirexyl phosphate

Target: Others, Microtubule Associated

Cat.No: T28865

Synonym: STAT3 IN B9,B9

Target: STAT

Tubulin inhibitor 11

Cat.No: T67935

Target: Apoptosis, Microtubule Associated

Cat.No: T36969

Cat.No: TP2128

Cat.No: T70962

Cat.No: T35940

Synonym: Dimethylarsinic glutathione,Darinaparsin

Cat.No: T40212

Cat.No: T36905

Cat.No: T79662

Target: STAT

Cat.No: T36968

Target: Topoisomerase

Cat.No: T15205

Synonym: EL102

Target: Microtubule Associated, HIF

3-Oxobetulin Acetate

Cat.No: T70856

Cat.No: T36195

(-)-Viriditoxin

Cat.No: T35437

Cat.No: T15362

Synonym: LDHA Inhibitor FX11

Target: Dehydrogenase

Cat. No.	Product Name	Target	Signaling Pathways
T8188	Podophyllotoxone	Others; Microtubule Associated	Cytoskeletal Signaling; Others
	Podophyllotoxone 是从八角莲根中分离得到的一种天然产物，能抑制微管蛋白聚合，具有抗癌活性。
T3S1416	Decursin Decursinol angelate,前胡素,(+)-Decursin,紫花前胡素	Apoptosis; PKC	Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling
	Decursin (Decursinol angelate) 是一种细胞毒性剂，是一种来自朝鲜当归根的有效蛋白激酶 C 激活剂。它通过 Hippo/YAP 信号通路抑制 HepG2 细胞的生长。它通过下调 CXCR7 表达来抑制胃癌中的肿瘤生长，迁移和侵袭。
T3138	Astaxanthin β-Carotene-4,4'-dione,Ovoester,AstaXin,AstaREAL,trans-Astaxanthin,虾青素	Reactive Oxygen Species; PPAR	DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; NF-κB
	Astaxanthin (trans-Astaxanthin) 是可从雨生红球藻等多种海洋生物中提取得到的红色类胡萝卜素，是过氧化物酶体增殖物活化受体γ 的调节剂，具有抗增殖、神经保护作用和抗炎活性。它是一种抗氧化剂，有用于癌症和心血管疾病的研究潜力，作为颜色添加剂用于动物食品中。
TN3049	4-Methoxycinnamyl alcohol	Others	Others
	4-Methoxycinnamyl alcohol 对MCF-7、HeLa 和DU145癌症细胞系显示出毒性，IC50值分别为14.24、7.82和22.10μg/mL。4-methoxycinnamyl alcohol 是从Foeniculum vulgare 中分离出来的。4-Methoxycinnamyl alcohol 没有显示出凋亡作用，却在10μg/mL DNA 碎片研究显示48小时后发生了坏死。
T2795	Amygdalin 苦杏仁苷,Laetrile	Others	Others
	Amygdalin (Laetrile) 是一种植物葡萄糖苷，分离自蔷薇果实的果核中，如杏，桃，杏仁，樱桃和李子。
T4869	D-Allose 阿洛糖,β-D-Allopyranose,D-(+)-ALLOSE	Others; Endogenous Metabolite	Metabolism; Others
	D-Allose (β-D-Allopyranose) 是内源性代谢产物的一种。
TN2755	2-Desoxy-4-epi-pulchellin	Anti-infection	Microbiology/Virology
	2-Desoxy-4-epi-pulchellin 是分离自 Polygonum hydropiper 的二氯甲烷可溶部分的一种化合物。
T3S0081	Oxypeucedanin (+-)-Oxypeucedanin,氧化前胡素,Oxypeucadanin	Potassium Channel	Membrane transporter/Ion channel
	Oxypeucedanin ((+-)-Oxypeucedanin) 是呋喃香豆素衍生物，分离自Angelica dahurica。它是选择性开放通道阻滞剂，可抑制hKv1.5通道电流，IC50值为 76 nM。它延长心脏动作电位持续时间，是潜在的抗心律失常试剂。它通过抑制癌细胞迁移来诱导细胞凋亡。
TN3528	Bonducellpin D	Antifection	Microbiology/Virology
	Bonducellpin D may show inhibitory activities on the Para3 virus. It also exhibits moderate activity against four tested human cancer cell lines, HepG-2, K562, HeLa, and Du145.
T83578	(19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol
	(19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol 是一种葫芦烷型三萜。该化合物在 MTT 法检测中对癌细胞系 MCF-7、HepG2、Du145、Colon205 以及 HL-60 均未表现出抑制效果。
TN3737	Cycloartane-3,24,25-triol	ATPase	Membrane transporter/Ion channel
	Cycloartane-3,24,25-triol has potential for development as an anti-cancer agent against prostate cancer. It reduces the viability of PC-3 and DU145 cell lines with IC50 values of 2.226 ± 0.28 μM and 1.67 ± 0.18 μM respectively.
TN3920	Effusanin A	Raf; Antifection	MAPK; Microbiology/Virology
	Effusanin A 是一种存在于Isodon rugosus 之中的天然产物。它具有 DNA 损伤和抗菌作用。
TN4263	Isoangustone A	MMP; GSK-3; NF-κB; ROS; Akt; PI3K; CDK; JNK	Cell Cycle/Checkpoint; Cytoskeletal Signaling; Immunology/Inflammation; MAPK; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
	Isoangustone A has antitumor activity, it can induce G1 cycle arrest in DU145 human prostate and 4T1 murine mammary cancer cells, it inhibits cell proliferation by targeting PI3K, MKK4, and MKK7 in human melanoma. Isoangustone A dampens mesangial sclerosis associated with inflammation in response to high glucose through hindering TGF-β and NF-ÎºB signaling. Isoangustone A also shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals.
TN3310	9,9'-Di-O-(E)-feruloylsecoisolariciresinol	mTOR	PI3K/Akt/mTOR signaling
	1,4-O-Diferuloylsecoisolariciresinol(9,9'-Di-O-(E)-feruloylsecoisolariciresinol),and pierreione B, two novel inhibitors of mTOR signaling, have strong anticancer activity. (+)-9,9'-O-Diferuloylsecoisolariciresinol has significant cytotoxic activity agains

天然产物

Podophyllotoxone

Cat.No: T8188

Target: Others, Microtubule Associated

Cat.No: T3S1416

Synonym: Decursinol angelate,前胡素,(+)-Decursin,紫花前胡素

Target: Apoptosis, PKC

Cat.No: T3138

Synonym: β-Carotene-4,4'-dione,Ovoester,AstaXin,AstaREAL,trans-Astaxanthin,虾青素

Target: Reactive Oxygen Species, PPAR

4-Methoxycinnamyl alcohol

Cat.No: TN3049

Target: Others

Cat.No: T2795

Synonym: 苦杏仁苷,Laetrile

Target: Others

Cat.No: T4869

Synonym: 阿洛糖,β-D-Allopyranose,D-(+)-ALLOSE

Target: Others, Endogenous Metabolite

2-Desoxy-4-epi-pulchellin

Cat.No: TN2755

Target: Anti-infection

Cat.No: T3S0081

Synonym: (+-)-Oxypeucedanin,氧化前胡素,Oxypeucadanin

Target: Potassium Channel

Cat.No: TN3528

Target: Antifection

(19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol

Cat.No: T83578

Cycloartane-3,24,25-triol

Cat.No: TN3737

Target: ATPase

Cat.No: TN3920

Target: Raf, Antifection

Cat.No: TN4263

Target: MMP, GSK-3, NF-κB, ROS, Akt, PI3K, CDK, JNK

9,9'-Di-O-(E)-feruloylsecoisolariciresinol

Cat.No: TN3310

Target: mTOR

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