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19

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8496	MAZ51	Apoptosis; VEGFR	Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors
	MAZ51 是一种 VEGFR-3酪氨酸激酶的选择性抑制剂。它抑制 VEGF-C 诱导的 VEGFR-3 激活，而没有阻断 VEGF-C 介导的 VEGFR2 刺激。它阻止增殖并诱导多种肿瘤细胞凋亡，具有抗肿瘤活性。
T9929	Ramucirumab	VEGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	Ramucirumab 是一种人 VEGFR-2 拮抗剂，具有抗实体瘤活性。它是人源化单克隆抗体，能够与 VEGFR-2 结合，阻碍 VEGFR 配体 VEGF-A，VEGF-C 和 VEGF-D 结合。
T72924	VEGFR-3-IN-1	VEGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	VEGFR-3-IN-1 是一种新型有效且具有选择性的 VEGFR3 抑制剂，其 IC50 为 110.4 nM。VEGFR-3-IN-1 具有抗肿瘤活性，可使 VEGFR3 信号通路失活，可抑制 VEGF-C 诱导人真皮淋巴管内皮细胞 (HDLEC)、MDA-MB-231 和 MDA-MB-436 细胞的增殖和迁移，并且能有效抑制乳腺癌的生长。
T3708	BP-1-102	STAT	JAK/STAT signaling; Stem Cells
	BP-1-102 是可口服的转录因子Stat3小分子抑制剂，IC50值为 6.8 μM。
T28899	T-1840383
	T-1840383 is an inhibitor of VEGF-induced VEGFR-2 phosphorylation and HGF-induced c-Met phosphorylation in vascular endothelial cells and cancer epithelial cells.
T71930	aPKC-I
	aPKC-I is an inhibitor of atypical protein kinase C (aPKC ) which inhibits both PKCζ and PKCι with high specificity and prevents VEGF-induced endothelial permeability in cell culture and in vivo, thereby blocking ischemia-reperfusion (IR)-induced permeability.
T80595	Conbercept KH902	VEGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	Conbercept (KH902) 是一种针对 VEGFRA 的融合蛋白，由 FLT1 第二个 C-LIKE 结构域与 KDR 第三和第四个 C-LIKE 结构域结合而成，并与 IGHG1 Fc 片段融合。该化合物设计用于中和 VEGF家族因子，具有重要的生物医学应用。
T21387	Nafoxidine HCl（1845-11-0 Free base） PNU-0011100,PNU0011100,CP5600,CP 5600,CP-5600,PNU 0011100,Nafoxidine HCl
	Nafoxidine is a partial estrogen antagonist. It inhibits angiogenesis in some tissues by blocking the effects of VEGF and FGF; paradoxically, it may enhance angiogenesis in uterine tissue. Nafoxidine also induces calcium signaling, oxidative stress, and p
T74422	Sozinibercept
	Sozinibercept (OPT 302; VGX-300) 是VEGFR-3的可溶性形式，能有效抑制血管生成原因子VEGF-C/D 的活性，抑制血管生成和血管渗漏。Sozinibercept 对大鼠糖尿病视网膜水肿也有抑制作用。
T71204	Apatinib HC Rivoceranib HCl,YN-968D1 HCl
	Apatinib, also known as Rivoceranib and YN-968D1, is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. The free-base form is also known as Rivoceranib. Apatinib selectively binds to and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated endothelial cell migration and proliferation and decrease tumor microvessel density. In addition, this agent mildly inhibits c-Kit and c-SR...
T71853	Enzastaurin HCl
	Enzastaurin HCl, also known as DB-102 and LY317615, is a synthetic macrocyclic bisindolemaleimide with potential antineoplastic activity. Binding to the ATP-binding site, Enzastaurin HCl selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply and so tumor burden.
T69354	Enzastaurin 2HCl
	Enzastaurin 2HCl, also known as DB-102 and LY317615, is a synthetic macrocyclic bisindolemaleimide with potential antineoplastic activity. Binding to the ATP-binding site, Enzastaurin 2HCl selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply and so tumor burden.
T37079	VEGFR2 Kinase Inhibitor II
	Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitor II is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. V...
T61604	PKC-IN-4
	PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), exhibiting an IC 50 value of 0.52 μM. In vitro studies have demonstrated that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α. Moreover, this compound effectively impedes the permeability of the retinal vasculature, induced by both VEGF and TNFα. [1]
T71180	Oglufanide disodium
	Oglufanide disodium is t he disodium salt of a synthetic form of a naturally-occurring dipeptide consisting of L-glutamic acid and L-tryptophan with potential antiangiogenic and potential immunomodulating activities. Oglufanide inhibits vascular endothelial growth factor (VEGF), which may inhibit angiogenesis. This agent has also been reported to stimulate the immune response to hepatitic C virus and intracellular bacterial infections. Check for active clinical trials or closed clinical trials u...
T27033	CKD-712 CKD 712,CKD712
	CKD-712 is a nuclear factor NF-kappa B inhibitor. CKD-712 suppressed MMP-9, but not MMP-2 and other NF-κB-regulated proteins involved in cancer metastasis such as VEGF. CKD-712 induced cell cycle arrest at G2M phase by suppressing cyclin A, cyclin B and C
T73516	EVT801
	EVT801 是一种口服有效、选择性的 VEGFR-3抑制剂 (IC50=11 nM)，具有抗肿瘤作用。EVT801 不仅抑制VEGF-C 诱导的人内皮细胞增殖，还抑制肿瘤小鼠模型中的肿瘤 (淋巴) 血管生成。EVT801 能够减少肿瘤缺氧，减少免疫抑制细胞因子 (CCL4、CCL5) 和髓系衍生抑制细胞 (MDSC) 产生。EVT801 与免疫检查点疗法 (ICT) 组有协同作用，它提高 ICT 应答率，对癌小鼠模型的抑制效果更好。
T83741	S7 TFA Leu-Ser-Leu-Iso-Thr-Arg-Leu-OH
	S7是一种IL-6受体的肽类拮抗剂，能够浓度依赖性地抑制IL-6与IL-6受体的结合。在C-33 A宫颈癌细胞和RPMI-8226 B细胞淋巴细胞中，S7 (50 µM) 能抑制IL-6诱导的VEGF水平增加。在每两天给药一次，剂量为50 mg/kg的条件下，S7能减少IL-6过表达的C-33 A宫颈癌小鼠异种移植模型中的肿瘤体积。当S7与半胱氨酸结合，并连接到包裹多柔比星的脂质纳米粒子(LNPs)表面时，能增强LNPs对胶质瘤的靶向性，并在U251胶质母细胞瘤小鼠异种移植模型中提高生存率。
T36379	Halometasone
	Halometasone is a synthetic corticosteroid.1,2Formulations containing halometasone have been used in the treatment of psoriasis vulgaris and eczematous dermatoses. 1.de la Brassine, M., Kint, A., Lachapelle, J.M., et al.Halomethasone (C 48.401-Ba) for the topical treatment of common dermatosesJ. Int. Med. Res.12(5)307-309(1984) 2.Zhu, J.-W., Wu, X.-J., Lu, Z.-F., et al.Role of VEGF receptors in normal and psoriatic human keratinocytes: Evidence from irradiation with different UV sourcesPLoS One8...

化合物

Cat.No: T8496

Target: Apoptosis, VEGFR

Cat.No: T9929

Target: VEGFR

Cat.No: T72924

Target: VEGFR

Cat.No: T3708

Target: STAT

Cat.No: T28899

Cat.No: T71930

Cat.No: T80595

Synonym: KH902

Target: VEGFR

Nafoxidine HCl（1845-11-0 Free base）

Cat.No: T21387

Synonym: PNU-0011100,PNU0011100,CP5600,CP 5600,CP-5600,PNU 0011100,Nafoxidine HCl

Cat.No: T74422

Cat.No: T71204

Synonym: Rivoceranib HCl,YN-968D1 HCl

Enzastaurin HCl

Cat.No: T71853

Enzastaurin 2HCl

Cat.No: T69354

VEGFR2 Kinase Inhibitor II

Cat.No: T37079

Cat.No: T61604

Oglufanide disodium

Cat.No: T71180

Cat.No: T27033

Synonym: CKD 712,CKD712

Cat.No: T73516

Cat.No: T83741

Synonym: Leu-Ser-Leu-Iso-Thr-Arg-Leu-OH

Cat.No: T36379

Cat. No.	Product Name	Target	Signaling Pathways
T3S0335	Soyasaponin Bb Soyasaponin I,大豆皂苷Bb	NF-κB; Caspase	Apoptosis; NF-κB; Proteases/Proteasome
	Soyasaponin Bb (Soyasaponin I) 是一种分离自菜豆科中的大豆皂苷，可用作醛糖还原酶差异抑制剂。
T3S2344	β,β-Dimethylacrylshikonin β,β-二甲基丙烯酰紫草素,Dimethylacrylshikonin,β, β-Dimethylacrylshikonin	ERK; HIF/HIF Prolyl-Hydroxylase	Chromatin/Epigenetic; MAPK; Metabolism
	β,β-Dimethylacrylshikonin (Dimethylacrylshikonin) 是一种萘醌衍生物，从 Arnebia nobilis 中提取得到。它利用 PI3K 通路诱导 eNOS、VEGF 和 HIF-1α 的表达，促进血管生成，具有抗肿瘤活性。

天然产物

Cat.No: T3S0335

Synonym: Soyasaponin I,大豆皂苷Bb

Target: NF-κB, Caspase

β,β-Dimethylacrylshikonin

Cat.No: T3S2344

Synonym: β,β-二甲基丙烯酰紫草素,Dimethylacrylshikonin,β, β-Dimethylacrylshikonin

Target: ERK, HIF/HIF Prolyl-Hydroxylase

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