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31

抑制剂 & 化合物

13

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11520	GW806742X	MLK; VEGFR	Angiogenesis; MAPK; Tyrosine Kinase/Adaptors
	GW806742X 是ATP 模拟物，是MLKL 抑制剂，可结合 MLKL 假激酶结构域，Kd 值为 9.3μM。它对VEGFR2的IC50为 2 nM，延缓 MLKL 膜移位并抑制坏死。
T9979	VEGFR-2-IN-29	VEGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	VEGFR-2-IN-29是一种 VEGFR2抑制剂。
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。
T4435	E7820 ER68203-00	Integrin	Cytoskeletal Signaling
	E7820 (ER68203-00) 是具有口服活性芳香族磺酰胺衍生物，是一种血管生成抑制剂，可抑制内皮上整合素 α2 亚基的表达。它调节 α1，α2，α3 和 α5 整联素 mRNA 表达，具有抗血管生成和抗肿瘤活性。它抑制大鼠主动脉血管生成，IC50为 0.11 μg/ml。
T7611	ODM-203	VEGFR; FGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	ODM-203 是 FGFR 和 VEGFR 家族的抑制剂，具有显著的抗肿瘤活性，能够诱导抗肿瘤免疫。
T0692	Allopurinol Zyloric,别嘌醇,Zyloprim,Lopurin,别嘌呤醇	ROS; Xanthine Oxidase	Immunology/Inflammation; Metabolism
	Allopurinol (Zyloric) 是一种黄嘌呤氧化酶(XO)抑制剂，IC50=7.82±0.12 μM。
T6182	Tirofiban L700462,Aggrastat,替罗非班,MK383	Integrin	Cytoskeletal Signaling
	Tirofiban (L700462) 是一种非肽类选择性 GPIIb/IIIa 拮抗剂，IC50 为 9 nM，可抑制血小板聚集。
T22436	Takeda-6d	VEGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	Takeda-6d 是一种新型、有效的 DFG-out RAF/血管内皮生长因子受体 2 (VEGFR2) 抑制剂，IC50 分别为 7.0 nM 和 2.2 nM。
T6376	Allopurinol Sodium 1H-吡唑并[3,4-D]嘧啶-4-醇单钠盐,Allopurinol sodium salt,Sodium allopurinol	ROS	Immunology/Inflammation
	Allopurinol Sodium 是黄嘌呤氧化酶抑制剂，其IC50= 0.2~50 μM。它能够抗利什曼原虫，也可用于研究痛风以及高尿酸血症。
T2537	Tirofiban hydrochloride monohydrate Tirofiban Hydrochloride,盐酸替罗非班水合物,MK-383 Hydrochloride,盐酸替罗非班	ATPase; Integrin	Cytoskeletal Signaling; Membrane transporter/Ion channel
	Tirofiban hydrochloride monohydrate (MK-383 Hydrochloride) 是一种非肽类糖蛋白IIb/IIIa 的拮抗剂。
T11076	Dooku1	Others	Others
	Dooku1 是Yoda1 的类似物，是一种内源性Piezo1通道的选择性拮抗剂，能够抑制Yoda1 诱导的主动脉舒张。它在HEK 293 细胞以及HUVEC 中测得对2 μM Yoda1 诱导的钙离子流的IC50值分别为1.3 μM 和1.5 μM。
T2500	Cediranib AZD2171,NSC-732208,西地尼布	VEGFR; FLT; PDGFR; c-Kit; Autophagy	Angiogenesis; Autophagy; Tyrosine Kinase/Adaptors
	Cediranib (AZD2171) 是一种可口服的高选择性VEGFR2抑制剂，对Flt1、KDR、Flt4、PDGFRα、PDGFRβ和c-Kit 的IC50值分别为小于1、小于3、5、5、36和 2nM。
T0005	Aspirin 阿司匹林,Acetylsalicylate,Acetylsalicylic Acid,邻乙酰水杨酸,ASA	Mitophagy; Virus Protease; COX; Autophagy	Autophagy; Immunology/Inflammation; Microbiology/Virology; Neuroscience
	Aspirin (Acetylsalicylic Acid) 是一种选择性 COX 抑制剂，具有多种药理活性。它是组蛋白去乙酰化酶抑制剂，可上调细胞周期阻滞蛋白 p21，抑制携带 COX-1 的卵巢 Y 细胞。它还抑制 HUVEC 和新生大鼠心室心肌细胞中 COX-2 的表达，分别减少 PG 的产生和 ERK 和 NF-KB 的下调。
T10680	Carebastine	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Carebastine 是 Ebastine 的活性代谢产物，可抑制巨噬细胞移动抑制因子的表达。它是组胺 H1 受体拮抗剂，可抑制 VEGF 诱导的 HUVEC 和 HPAEC 增殖，迁移和血管生成。
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。
T27622	IPS-05002
	IPS-05002 is an integrin a5β1 antagonist. IPS-05002 inhibited VEGF-stimulated human umbilical vein endothelial cell (HUVEC) proliferation, adhesion, and migration in a dose-dependent manner. IPS-05002 is a potent inhibitor for VEGF-mediated angiogenesis.
T79364	Antiangiogenic agent 4	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	Antiangiogenic agent 4（Compound 3b）在HFF和HUVEC细胞中抑制Akt磷酸化，可应用于癌症研究。
T34492	Salinazid Nilazid,Salicylaldehyde isonicotinoyl hydrazone,Salizid,Salizide,Nupasal,SIH1	Others	Others
	Salinazid (Salicylaldehyde isonicotinoyl hydrazone) 是一种有效的抗结核药。
T72449	Tubulin inhibitor 31
	Tubulin inhibitor 31, 以IC50值4 µM的效力，是一种高效的微管蛋白(Tubulin)抑制剂，具有显著的抗增殖活性，并能抑制HUVEC的迁移。
T72363	Antiangiogenic agent 3
	Antiangiogenic agent 3 是一种抗血管生成剂，具有抑制人脐静脉内皮细胞(HUVEC)生长、迁移与趋化运动的作用。此外，该化合物还能降低 Src、cdc42 以及 MAPK 的基因表达。
T79702	Nrf2 activator-9
	Nrf2 activator-9 (compound D-36) 是抑制oxLDL和HG诱导的HUVEC细胞凋亡的Nrf2激活剂，有助于预防动脉粥样硬化。该化合物可防止VEC损伤，展现出对心血管疾病的潜在治疗效果。
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。
T80872	VEGFR-2-IN-37	VEGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	VEGFR-2-IN-37（化合物12）是一种VEGFR-2抑制剂，其在200 μM浓度下的抑制率为56.9%。该化合物也是潜在的HUVEC增殖抑制剂。
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.
T74627	Angiogenesis inhibitor 3
	Angiogenesis inhibitor 3 (compound 8) 是一种有效的血管生成(angiogenesis)抑制剂，能够抑制HUVEC和HCT-15细胞增殖，其IC50值分别为1.00和0.71 μM。此外，此化合物还能诱导这两种细胞的凋亡(apoptosis)并具有抑制癌细胞侵袭的抗癌活性。Angiogenesis inhibitor 3还能够抑制斑马鱼胚胎的血管生成。
T79560	22-(4′-py)-JA 22-(4′-Pyridinecarbonyl) jorunnamycin A	Akt	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	22-(4′-py)-JA是久那霉素A的半合成衍生物，源自泰国蓝海绵（Xestospongia sp.）。该化合物显示出抗转移活性，能抑制AKT/mTOR/p70S6K信号通路，并阻断人脐静脉内皮细胞（HUVEC）中肿瘤细胞侵袭及管形成作用。它通过下调金属蛋白酶（MMP-2和MMP-9）、缺氧诱导因子1α（HIF-1α）和血管内皮生长因子（VEGF）来发挥作用。此外，22-(4′-py)-JA对非小细胞肺癌（NSCLC）显示出显著的抗癌效果。
T76052	ELA-32(human) TFA
	ELA-32(human) TFA is a potent, high affinityapelin receptoragonist (IC50=0.27 nM; Kd=0.51 nM). ELA-32(human) TFA exhibits no binding GPR15 and GPR25. ELA-32(human) TFA activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. ELA-32(human) TFA also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. ELA-32(human) TFA stimulates angiogenesis in HUVEC cells.
T36138	BMP-22
	BMP-22 is an inhibitor of autotaxin (IC50 = 170 nM). It is selective for autotaxin over the phosphodiesterases NPP6 and NPP7 at 10 μM. BMP-22 (0.1-1,000 nM) inhibits autotaxin-mediated production of lysophosphatidic acid (LPA) from lysophosphatidylcholine in vitro in a concentration-dependent manner. It inhibits LPC-dependent MM1 cell invasion of a human umbilical vein endothelial cell (HUVEC) monolayer. BMP-22 (0.5 mg/kg per day) decreases the number of lung metastatic foci in a B16/F10 syngene...
T82402	Fibulostatin 6.2
	Fibulostatin 6.2为一种抗血管生成肽，其能够抑制体外环境中人类脐静脉内皮细胞（HUVEC）的迁移现象。
TP2097	ELA-32(human) ELA-32 (human)
	Potent, high affinity apelin receptor agonist (IC50 = 0.27 nM; Kd = 0.51 nM). Exhibits no binding GPR15 and GPR25. Activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. Also potentiates the T
T78548	3-Hydroxyxanthone 3-Hydroxy-xanthen-9-one	Integrin	Cytoskeletal Signaling
	3-Hydroxyxanthone (3-Hydroxy-xanthen-9-one) 是一种具有抗炎活性的氧杂蒽酮化合物。它能抑制人脐静脉内皮细胞（HUVEC）中NADPH催化的脂质过氧化，并且阻止TNF-α所诱导的ICAM-1表达。

化合物

Cat.No: T11520

Target: MLK, VEGFR

Cat.No: T9979

Target: VEGFR

Cat.No: T4425

Target: VEGFR

Cat.No: T4435

Synonym: ER68203-00

Target: Integrin

Cat.No: T7611

Target: VEGFR, FGFR

Cat.No: T0692

Synonym: Zyloric,别嘌醇,Zyloprim,Lopurin,别嘌呤醇

Target: ROS, Xanthine Oxidase

Cat.No: T6182

Synonym: L700462,Aggrastat,替罗非班,MK383

Target: Integrin

Cat.No: T22436

Target: VEGFR

Allopurinol Sodium

Cat.No: T6376

Synonym: 1H-吡唑并[3,4-D]嘧啶-4-醇单钠盐,Allopurinol sodium salt,Sodium allopurinol

Target: ROS

Tirofiban hydrochloride monohydrate

Cat.No: T2537

Synonym: Tirofiban Hydrochloride,盐酸替罗非班水合物,MK-383 Hydrochloride,盐酸替罗非班

Target: ATPase, Integrin

Cat.No: T11076

Target: Others

Cat.No: T2500

Synonym: AZD2171,NSC-732208,西地尼布

Target: VEGFR, FLT, PDGFR, c-Kit, Autophagy

Cat.No: T0005

Synonym: 阿司匹林,Acetylsalicylate,Acetylsalicylic Acid,邻乙酰水杨酸,ASA

Target: Mitophagy, Virus Protease, COX, Autophagy

Cat.No: T10680

Target: Histamine Receptor

Cat.No: T67836

Target: HSP, HSV

Cat.No: T27622

Antiangiogenic agent 4

Cat.No: T79364

Target: Akt

Cat.No: T34492

Synonym: Nilazid,Salicylaldehyde isonicotinoyl hydrazone,Salizid,Salizide,Nupasal,SIH1

Target: Others

Tubulin inhibitor 31

Cat.No: T72449

Antiangiogenic agent 3

Cat.No: T72363

Nrf2 activator-9

Cat.No: T79702

18-Deoxyherboxidiene

Cat.No: T62267

Cat.No: T80872

Target: VEGFR

Cat.No: T41145

Angiogenesis inhibitor 3

Cat.No: T74627

22-(4′-py)-JA

Cat.No: T79560

Synonym: 22-(4′-Pyridinecarbonyl) jorunnamycin A

Target: Akt

ELA-32(human) TFA

Cat.No: T76052

Cat.No: T36138

Fibulostatin 6.2

Cat.No: T82402

Cat.No: TP2097

Synonym: ELA-32 (human)

3-Hydroxyxanthone

Cat.No: T78548

Synonym: 3-Hydroxy-xanthen-9-one

Target: Integrin

Cat. No.	Product Name	Target	Signaling Pathways
TN1112	Morellic acid	Others	Others
	Morellic acid 提取于 Garcinia Morella 中，具有抗血管生成作用。
T2P2870	Damascenone trans-damascenone,Beta-Damascenone,大马烯酮,大马酮	Others; NF-κB; Endogenous Metabolite	Metabolism; NF-κB; Others
	Damascenone (trans-damascenone) 是一种 E-和 Z-异构体大马士革酮的混合物，源于 Epipremnum pinnatum 的具有抗炎特性的特性化合物。
T3982	Vulpinic Acid 狐衣酸,Vulpic acid,Pulvinic acid methyl ester	Others	Others
	Vulpinic Acid (Pulvinic acid methyl ester) 是地衣代谢物，可降低人脐静脉内皮细胞 (HUVEC) 中 H2O2诱导的ROS，氧化应激和氧化应激相关损伤，可作用于厌氧菌、葡萄球菌及肠球菌。它对脉粥样硬化的研究具有潜在的价值。
T3402	20(S)-Ginsenoside Rg3 20(S)-人参皂苷 Rg3,人参皂苷 Rg3,20(S)-Ginsenoside-Rg3,Rg3,20S-Ginsenoside Rg3,Ginsenoside Rg3,S-Ginsenoside Rg3	EGFR; Beta Amyloid; Potassium Channel; NF-κB; COX; Sodium Channel; Endogenous Metabolite	Angiogenesis; Immunology/Inflammation; JAK/STAT signaling; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB; Tyrosine Kinase/Adaptors
	20(S)-Ginsenoside Rg3 (Rg3) 是红参的主要成分，通过抑制肿瘤细胞的粘附和侵袭来抑制肿瘤细胞肺转移。它抑制Na+和hKv1.4通道，IC50分别为 32.2±4.5 和 32.6±2.2 μM。它还抑制Aβ，NF-κB 活性和COX-2表达，抑制人脐静脉内皮细胞的增殖并具有抗血管生成活性。
T6S1784	Brazilin Natural Red 24,巴西苏木素;苏枋精,Braziletto,Brasilin,Superbresiline,巴西苏木素	Apoptosis; Others; AMPK; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; Others; PI3K/Akt/mTOR signaling
	Brazilin (Braziletto) 是来自几种热带硬木的心材的一种红色染料前体，有软骨保护和抗炎活性。它抑制细胞增殖，促进细胞凋亡并通过 AMPK/mTOR 途径诱导自噬。
T3923	Calycosin Cyclosin,3'-Hydroxyformononetin,异黄酮,毛异黄酮	Apoptosis; Tyrosinase	Apoptosis; Proteases/Proteasome
	Calycosin (Cyclosin) 是一抗氧化和抗炎症活性天然产物。
T6S1572	Sauchinone	ERK; p38 MAPK; NF-κB	MAPK; NF-κB
	Sauchinone 是一种从Saururus chinensis 中获得的非对映异构的木脂素。它通过抑制I-κBα磷酸化和p65核易位来抑制 LPS 诱导的 iNOS，TNF-α 和 COX-2 表达。它具有抗炎和抗氧化活性。
T5768	bruceine B	TNF; Parasite	Apoptosis; Microbiology/Virology
	Bruceine B 是一种有效的白细胞-内皮细胞粘附抑制剂，可抑制蛋白质和核酸合成。
TN5351	Cycloshizukaol A
	Cycloshizukaol A prevents monocyte adhesion to HUVEC through the inhibition of cell adhesion molecules expression stimulated by TNF-alpha, it inhibits PMA-induced homotypic aggregation of HL-60 cells without cytotoxicity with MIC values of 0.9 microM.
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
TN1988	Nephthenol	Others	Others
	Nephthenol shows antiproliferative activity against the cell lines HUVEC and K-562 and for cytotoxicity against the cell line HeLa.
TN5100	Taspine	ERK; EGFR; BCL; VEGFR; MAPK; Akt	Angiogenesis; Apoptosis; Cytoskeletal Signaling; JAK/STAT signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	Taspine shows antitumor activity by modulating the EGFR signaling pathway of Erk1/2 and Akt in vitro and in vivo, it can inhibit growth and induce apoptosis of HUVEC in a dose-dependent manner, it has shown meaningful angiogenesis activity. Taspine exhibi
TN5011	Shizukaol B	ERK; IL Receptor; p38 MAPK; TNF; NOS; NF-κB; COX; HIV Protease; DNA/RNA Synthesis; Prostaglandin Receptor; JNK	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; MAPK; Microbiology/Virology; Neuroscience; NF-κB; Proteases/Proteasome
	Shizukaol B exerts anti-inflammatory effects in LPS-activated microglia partly by modulating JNK-AP-1 signaling pathway; it also shows significant anti-neuroinflammatory effects by inhibiting nitric-oxide (NO) production in lipopolysaccharide (LPS)-stimul

天然产物

Cat.No: TN1112

Target: Others

Cat.No: T2P2870

Synonym: trans-damascenone,Beta-Damascenone,大马烯酮,大马酮

Target: Others, NF-κB, Endogenous Metabolite

Cat.No: T3982

Synonym: 狐衣酸,Vulpic acid,Pulvinic acid methyl ester

Target: Others

20(S)-Ginsenoside Rg3

Cat.No: T3402

Synonym: 20(S)-人参皂苷 Rg3,人参皂苷 Rg3,20(S)-Ginsenoside-Rg3,Rg3,20S-Ginsenoside Rg3,Ginsenoside Rg3,S-Ginsenoside Rg3

Target: EGFR, Beta Amyloid, Potassium Channel, NF-κB, COX, Sodium Channel, Endogenous Metabolite

Cat.No: T6S1784

Synonym: Natural Red 24,巴西苏木素;苏枋精,Braziletto,Brasilin,Superbresiline,巴西苏木素

Target: Apoptosis, Others, AMPK, Autophagy

Cat.No: T3923

Synonym: Cyclosin,3'-Hydroxyformononetin,异黄酮,毛异黄酮

Target: Apoptosis, Tyrosinase

Cat.No: T6S1572

Target: ERK, p38 MAPK, NF-κB

Cat.No: T5768

Target: TNF, Parasite

Cycloshizukaol A

Cat.No: TN5351

Cat.No: TN3706

Cat.No: TN1988

Target: Others

Cat.No: TN5100

Target: ERK, EGFR, BCL, VEGFR, MAPK, Akt

Cat.No: TN5011

Target: ERK, IL Receptor, p38 MAPK, TNF, NOS, NF-κB, COX, HIV Protease, DNA/RNA Synthesis, Prostaglandin Receptor, JNK

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