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17

抑制剂 & 化合物

5

天然产物

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Cat. No. Product Name Target Signaling Pathways
T9928 Ranibizumab

VEGFR Angiogenesis; Tyrosine Kinase/Adaptors
Ranibizumab 是一种人源化单克隆抗体片段,旨在靶向和抑制血管内皮生长因子 (VEGF),包括 VEGF110、VEGF121 和 VEGF165。 Ranibizumab 选择性靶向和中和 VEGF-A 同工型的能力使其成为湿性年龄相关性黄斑变性 (AMD) 研究和治疗策略的重要组成部分。
T33701 NM-3

NM-3,isocoumarin,NM 3,Isocoumarin NM-3,NM3

Apoptosis; Reactive Oxygen Species Apoptosis; Immunology/Inflammation; Metabolism; NF-κB
NM-3 是一种可口服的抗血管生成的抑制剂,具有抗肿瘤活性。NM-3在体外和体内可当作辐射调节剂使用。NM-3抑制血管内皮生长因子(VEGF),从而抑制内皮细胞的增殖。NM-3与活性氧的机制诱导细胞凋亡有关。
T27028 CJ-3-60

CJ 3-60,CJ3-60,CJ-360,CJ360,CJ 360

CJ-3-60, an anti-HIF-1alpha agent, inhibits HIF-1alpha and cellular VEGF proteins.
T12650 R916562

TAM Receptor Tyrosine Kinase/Adaptors
R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC50s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.
T35492 (±)10(11)-DiHDPA

(±)10(11)-DiHDPA is produced from cytochrome P450 epoxygenase action on docosahexaenoic acid . It has been shown to inhibit VEGF-induced angiogenesis in mice and may have additional anti-inflammatory and anti-tumor effects.
T80593 Brolucizumab

DLX1008,ESBA 1008,RTH258

VEGFR Angiogenesis; Tyrosine Kinase/Adaptors
Brolucizumab(DLX1008)是一种具有高亲和力(KD=1.05 pM)的单链抗VEGF-A抗体片段,适用于癌症研究。
T10273 AhR modulator-1

Others Others
AhR modulator-1 is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. It inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. It also possesses anti-estrogenic properties in rat uterus.
T68935 BMS-645737

BMS-645737 is an inhibitor of vascular endothelial growth factor (VEGF) receptor-2 and fibroblast growth factor (FGF) receptor-1. BMS-646737 has anti-angiogenic activity and was evaluated in nonclinical studies as a treatment for cancer.
T78064 Synstatin (92-119)

SSTN92-119

Integrin Cytoskeletal Signaling
Synstatin (92-119)为一种抗肿瘤化合物,它能够抑制血管生成与癌细胞侵袭,通过下调整合素αvβ3,降低VEGF与FGF-2的活化。
T76871 Navicixizumab

Navicixizumab (OMP-305B83) 是一种双特异性抗 VEGF 和抗 DLL4抑制抗体。Navicixizumab 可以与紫杉醇结合用于癌症研究。Navicixizumab 可用于卵巢癌、原发性腹膜癌或输卵管癌的研究。
T74118 Roxatidine

Roxatidine 是 Roxatidine acetate 的活性代谢产物,是组胺 H2受体拮抗剂。Roxatidine 是抗溃疡药,抑制组胺释放(从而抑制质子分泌)并抑制炎症和血管生成的重要标志物 VEGF-1 的产生。具有抗过敏性炎症作用。
T69599 ABT-510

ABT-510 is synthetic peptide that mimics the anti-angiogenic activity of the endogenous protein thrombospondin-1 (TSP-1). ABT-510 inhibits the actions of several pro-angiogenic growth factors important to tumor neovascularization; these pro-angiogenic growth factors include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF)), hepatocyte growth factor (HGF), and interleukin 8 (IL-8).
T71176 Atiprimod (free base)

Atiprimod is an orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, ind...
T77108 Olinvacimab

Olinvacimab (TTAC-0001) 是一种人抗 VEGFR2单克隆抗体。Olinvacimab 抑制 VEGF 与 KDR 结合,Kd 值为 0.23 nM。Olinvacimab 具有抗血管生成活性。Olinvacimab 可用于复发性胶质母细胞瘤和乳腺癌的研究。
T68324 KCN1

KCN1, a novel synthetic sulfonamide, is a HIF pathway inhibitor with potential anticancer activity in vitro and in vivo anti-pancreatic cancer activities and preclinical pharmacology. KCN1 specifically inhibited HIF reporter gene activity in several glioma cell lines at the nanomolar level. KCN1 also downregulated transcription of endogenous HIF-1 target genes, such as VEGF, Glut-1, and carbonic anhydrase 9, in a hypoxia-responsive element (HRE)-dependent manner. KCN1 potently inhibited the grow...
T76895 Abicipar pegol

Abicipar pegol (AGN-150998, MP0112) 是一种抗VEGFDARPin 分子,DARPin 分子是一类新型的小蛋白,含有工程化的 ankyrin 重复结构域,以高特异性和亲和力与靶蛋白结合。Abicipar pegol 可有效抑制血管生成和血管通透性,通过玻璃体内注射,降低平均视网膜厚度和渗漏面积,用于眼部炎症等相关疾病研究。
T68389 LY2457546

LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 (KDR), PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. In vivo, LY2457546 inhibited VEGF-driven autophosphorylation of lung KDR in the mouse and rat in a dose and concentration dependent manner. LY2457546 was well tolerated and exhibited efficacy in a 13762 synge...

化合物

Ranibizumab
Cat.No: T9928
Synonym:
Target: VEGFR
NM-3
Cat.No: T33701
Synonym: NM-3,isocoumarin,NM 3,Isocoumarin NM-3,NM3
Target: Apoptosis, Reactive Oxygen Species
CJ-3-60
Cat.No: T27028
Synonym: CJ 3-60,CJ3-60,CJ-360,CJ360,CJ 360
Target:
R916562
Cat.No: T12650
Synonym:
Target: TAM Receptor
(±)10(11)-DiHDPA
Cat.No: T35492
Synonym:
Target:
Brolucizumab
Cat.No: T80593
Synonym: DLX1008,ESBA 1008,RTH258
Target: VEGFR
AhR modulator-1
Cat.No: T10273
Synonym:
Target: Others
BMS-645737
Cat.No: T68935
Synonym:
Target:
Synstatin (92-119)
Cat.No: T78064
Synonym: SSTN92-119
Target: Integrin
Navicixizumab
Cat.No: T76871
Synonym:
Target:
Roxatidine
Cat.No: T74118
Synonym:
Target:
ABT-510
Cat.No: T69599
Synonym:
Target:
Atiprimod (free base)
Cat.No: T71176
Synonym:
Target:
Olinvacimab
Cat.No: T77108
Synonym:
Target:
KCN1
Cat.No: T68324
Synonym:
Target:
Abicipar pegol
Cat.No: T76895
Synonym:
Target:
LY2457546
Cat.No: T68389
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN1557 Decursinol angelate

ERK; VEGFR; PKC; JNK Angiogenesis; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; Tyrosine Kinase/Adaptors
Decursinol angelate 是从朝鲜当归根部分离得到的一种天然产物,是 PKC 激酶的激活剂,有细胞毒性,抗肿瘤和抗炎活性。
T5429 Theaflavin 3,3'-digallate

茶黄素-3,3'-双没食子酸,8-Gingerol,TFDG

Virus Protease; Antioxidant; HIV Protease; HSV Microbiology/Virology; oxidation-reduction; Proteases/Proteasome
Theaflavin 3,3'-digallate (8-Gingerol) 是一种寨卡病毒蛋白酶抑制剂,IC50为 2.3 μM。它直接与 ZIKVpro 结合并抑制 ZIKV 复制,可抑制 gp41 和 NS2B-3 蛋白酶的活性,并具有抗 HSV 和 HIV-1病毒活性。它是红茶中的主要多酚,有抗肿瘤作用。
TN3139 5α-Hydroxycostic acid

5alpha-Hydroxycostic acid

ERK; FAK; Phospholipase; NOS; Akt; Src Angiogenesis; Cytoskeletal Signaling; Immunology/Inflammation; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
5alpha-Hydroxycostic acid possesses anti-angiogenic ability by interfering the VEGF- and Ang2-related pathways, and it may be a good drug candidate.
TN1874 Liriodendrin

鹅掌楸苦素

ATPase; Potassium Channel; Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel
Liriodendrin 调节肺部炎症、NF-kB (p65) 的磷酸化和血管内皮生长因子 (VEGF) 的表达。Liriodendrin 具有抗炎、镇痛、降血糖活性,在脓毒症引起的急性肺损伤中起保护作用。
TN4356 Jolkinolide A

Akt; STAT; mTOR Cytoskeletal Signaling; JAK/STAT signaling; PI3K/Akt/mTOR signaling; Stem Cells
Jolkinolide A has anti-tumor activity. It inhibited VEGF expression in A549 cells through the inhibition of the Akt-STAT3-mTOR signaling pathway, and directly inhibited the proliferation and migration of HUVECs.

天然产物

Decursinol angelate
Cat.No: TN1557
Synonym:
Target: ERK, VEGFR, PKC, JNK
Theaflavin 3,3'-digallate
Cat.No: T5429
Synonym: 茶黄素-3,3'-双没食子酸,8-Gingerol,TFDG
Target: Virus Protease, Antioxidant, HIV Protease, HSV
5α-Hydroxycostic acid
Cat.No: TN3139
Synonym: 5alpha-Hydroxycostic acid
Target: ERK, FAK, Phospholipase, NOS, Akt, Src
Liriodendrin
Cat.No: TN1874
Synonym: 鹅掌楸苦素
Target: ATPase, Potassium Channel, Prostaglandin Receptor
Jolkinolide A
Cat.No: TN4356
Synonym:
Target: Akt, STAT, mTOR
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