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18

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T3162	IDE1	Others	Others
	IDE1 是定形内胚层诱导物，有用于器官移植等方面的潜力。
T4425	JK-P3	VEGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	JK-P3 是广谱 VEGFR2抑制剂。它能够抑制 VEGF-A 刺激的 VEGFR2 激活和细胞内信号转导，也可阻碍内皮单层细胞迁移和血管生成，影响成纤维细胞生长因子受体激酶在体外的活性。它具有抗血管生成的作用。
T67836	AT-533	HSP; HSV	Cytoskeletal Signaling; Metabolism; Microbiology/Virology
	AT-533 是有效的 HSV 和 Hsp90 抑制剂。AT-533 可以阻断 HIF-1α/VEGF/VEGFR-2 信号通路，从而抑制血管生成和肿瘤生长。AT-533 也抑制下游通路的激活，包括 Erk1/2, FAK, Akt/mTOR/p70S6K。AT-533 抑制人脐静脉内皮细胞 (HUVEC) 的细胞迁移、侵袭和管形成。
T71488	Cremastranone
	Cremastranone is a natural antiangiogenic homoisoflavanone. Cremastranone inhibits the proliferation, migration, and tube formation ability of human retinal microvascular endothelial cells.
T28788	SK-216 SK216.Plasminogen activator inhibitor-1 (PAI-1) inhibitor
	SK-216 is a specific PAI-1 inhibitor. SK-216 reduced the extent of angiogenesis in the tumors and inhibited VEGF-induced migration and tube formation by human umbilical vein endothelial cells in vitro. SK-216 reduced the degree of bleomycin-induced pulmon
T36718	Tie2 Inhibitor 7
	Tie2 Inhibitor 7 blocks Tie2 kinase activity with a Ki value of 1.3 μM.. It has been shown to inhibit angiopoietin 1-induced Tie2 autophosphorylation and downstream signaling with an IC50 value of 0.3 μM. This compound can prevent endothelial cell tube formation and aberrant vessel growth in a rat model of Matrigel-induced choroidal neovascularization.
T61532	Tubulin polymerization-IN-6
	Tubulin polymerization-IN-6 (compound 5f) is a potent inhibitor of tubulin polymerization, with an IC50 of 1.09 μM. It not only inhibits cell migration and tube formation but also has anti-angiogenic properties. Additionally, Tubulin polymerization-IN-6 has been found to effectively hinder tumor growth in HT29 xenograft Balb/c nude mice [1].
TP1631L	Competence-Stimulating Peptide-12261 acetate Competence-Stimulating Peptide-12261 acetate (1235882-91-3 free base)	Others	Others
	Competence-Stimulating Peptide-12261 acetate (1235882-91-3 free base) 是感觉刺激肽的片段，是一种抑制胚管 (GT) 形成的群体感应分子。
T41145	TASP 0277308
	TASP 0277308 is a potent and selective sphingosine 1-phosphate 1 (S1P1) receptor antagonist (IC50 = 7.8 nM). TASP 0277308 inhibits S1P-induced chemotaxis (IC50 = 1.1-1.6 nM), HUVEC cell proliferation (IC50 = 3-3.6 nM) and suppresses angiogenesisin vivo. TASP 0277308 also blocks VEGF-induced tube-formation of HUVECsin vitroand reverses or impairs the development of arthritis or mechano-allodynia.
T70903	KRH102053
	KRH102053 is a HIF-1alpha inhibitor. KRH102053 decreased the protein level of HIF-1alpha and the mRNA levels of HIF-regulated downstream target genes, such as vascular endothelial growth factor, aldolase A, enolase 1 and monocarboxylate transporter 4. Consistent with these results, KRH102053 also inhibited the rates of HIF-related migration and invasion of HOS cells as well as the degree of tube formation in human umbilical vein endothelium cells.
T62267	18-Deoxyherboxidiene
	18-Deoxyherboxidiene (RQN-18690A) 是一种有效的血管生成抑制剂。18-Deoxyherboxidiene 能够选择性作用于 SF3b，其中 SF3b 是剪接体中 U2 小核核糖核蛋白 (snRNP) 的亚复合体。18-Deoxyherboxidiene 对人脐静脉内皮细胞 (HUVEC) 的迁移和管形成具有抑制作用，且无明显的细胞毒性。18-Deoxyherboxidiene 具有潜力进行癌症的研究。
T68511	KRH102140
	KRH102140 is a potent activator of PHD2. KRH102140, which has a structure similar to KRH102053. KRH102140 more efficiently suppressed HIF-1α than KRH102053 in human osteosarcoma cells under hypoxia. Furthermore, KRH102140 decreased the mRNA levels of HIF-regulated downstream target genes associated with angiogenesis and energy metabolism such as vascular endothelial growth factor, adrenomedullin, Glut1, aldolase A, enolase 1 and monocarboxylate transporter 4. KRH102140 also inhibited tube format...
T35408	(±)10(11)-EDP Ethanolamide
	(±)10(11)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 0.43 and 22.5 nM for CB1 and CB2 receptors, respectively). It is produced though direct epoxygenation of docosahexaenoyl ethanolamide by cytochrome P450 (CYP) epoxygenases. 10,11-EDP epoxide (12.5 and 25 μM) reduces the viability of 143B metastatic osteosarcoma cells. It induces apoptosis and inhibits cell migration in a wound-healing assay in 143B, MG63, and HOS osteosarcoma cells. (±)10(...
T70906	EHT-6706
	EHT-6706 is a novel microtubule-disrupting agent that targets the colchicine-binding site to inhibit tubulin polymerization. At low nM concentrations, EHT 6706 exhibits highly potent antiproliferative activity on more than 60 human tumor cell lines, even those described as being drug resistant. EHT 6706 also shows strong efficacy as a vascular-disrupting agent, since it prevents endothelial cell tube formation and disrupts pre-established vessels, changes the permeability of endothelial cell mon...
T71116	MPT0B098
	MPT0B098 is a potent microtubule inhibitor through binding to the colchicine-binding site of tubulin. MPT0B098 is active against the growth of various human cancer cells, including chemoresistant cells with IC50 values ranging from 70 to 150 nmol/L. MPT0B098 arrests cells in the G2Â–M phase and subsequently induces cell apoptosis. In addition, MPT0B098 effectively suppresses VEGF-induced cell migration and capillary-like tube formation of HUVECs. Distinguished from other microtubule inhibitors, ...
T35406	α-MSH TFA
	α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube fo...
T35468	(±)19(20)-EDP Ethanolamide
	(±)19(20)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 108 and 280 nM for CB1 and CB2, respectively). It is produced through direct epoxygenation of docosahexaenoyl ethanolamide by cytochrome P450 (CYP) epoxygenases. (±)19(20)-EDP ethanolamide (25 μM) reduces the viability of 143B metastatic osteosarcoma cells. It decreases the production of IL-6 and increases the production of IL-10 when used at concentrations ranging from 2.5 to 10 μM in BV-...
T83680	Azurin (50-77) (P. aeruginosa) TFA Azurin p28,p28
	Azurin (50-77)是一种含铜细菌蛋白azurin的肽段，存在于P. aeruginosa中，具有细胞周期停滞、抑制癌细胞增殖和调节血管生成活性。作为VEGFR2的抑制剂（IC20约为10.7 µM），Azurin (50-77)（20 µM）能在MCF-7乳腺癌细胞中诱导G2/M期的细胞周期停滞。在50 µM的浓度下，减少MCF-7和ZR-75-1乳腺癌细胞的增殖。Azurin (50-77)以25 µM的浓度减少VEGF-A诱导的毛细管管腔形成（IC50 = 12 µM），降低人脐静脉内皮细胞（HUVECs）中与细胞膜相关的F-actin、焦点粘附激酶（FAK）和paxillin的水平，并增加胞外的血小板内皮细胞粘附分子-1（PECAM-1）的水平。在体内，Azurin (50-77)（每日10 mg/kg）在MCF-7小鼠异种移植模型中减少肿瘤体积。

化合物

Cat.No: T3162

Target: Others

Cat.No: T4425

Target: VEGFR

Cat.No: T67836

Target: HSP, HSV

Cat.No: T71488

Cat.No: T28788

Synonym: SK216.Plasminogen activator inhibitor-1 (PAI-1) inhibitor

Tie2 Inhibitor 7

Cat.No: T36718

Tubulin polymerization-IN-6

Cat.No: T61532

Competence-Stimulating Peptide-12261 acetate

Cat.No: TP1631L

Synonym: Competence-Stimulating Peptide-12261 acetate (1235882-91-3 free base)

Target: Others

Cat.No: T41145

Cat.No: T70903

18-Deoxyherboxidiene

Cat.No: T62267

Cat.No: T68511

(±)10(11)-EDP Ethanolamide

Cat.No: T35408

Cat.No: T70906

Cat.No: T71116

Cat.No: T35406

(±)19(20)-EDP Ethanolamide

Cat.No: T35468

Azurin (50-77) (P. aeruginosa) TFA

Cat.No: T83680

Synonym: Azurin p28,p28

Cat. No.	Product Name	Target	Signaling Pathways
T8846	beta-Escin B-escin,AESCINE,beta-七叶素	Immunology/Inflammation related	Immunology/Inflammation
	beta-Escin 是七叶树种子的主要活性成分。它可抑制碱性成纤维细胞生长因子所诱导的增殖、迁移、管形成以及体内 CAM 血管生成。它具有研究抗血管生成作用的分子机制的潜力。
TN3706	Coronarin A
	Coronarin, A, B, C, and D are cytotoxic prinicples from the rhizomes of Hedychium coronarium, Zingiberaceae. Coronarin A exhibits good growth inhibition activities on HUVEC proliferation, it effectively suppresses the growth factor induced tube formation
T36749	Herboxidiene
	Herboxidiene is a polyketide originally isolated from S. chromofuscus that has diverse biological activities.[1],[2,][3],[4],[5] It inhibits growth of HeLa S3, SK-MEL-2, PC3, A549, and EBC-1 cells with GI50 values ranging from 7.4 to 62 nM.3 Herboxidiene is cytostatic against human umbilical vein endothelial cells (HUVECs; (IC50 = 26 nM)) and inhibits VEGF-induced invasion and tube formation of serum-starved HUVECs in a concentration-dependent manner, indicating antiangiogenic activity.[4] Herbo...

天然产物

Cat.No: T8846

Synonym: B-escin,AESCINE,beta-七叶素

Target: Immunology/Inflammation related

Cat.No: TN3706

Cat.No: T36749

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