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22

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T22414	RBN012759	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	RBN012759 是选择性和具有口服活性的 PARP14抑制剂，IC50值小于3 nM，可降低促肿瘤巨噬细胞功能并在肿瘤外植体中引发炎症反应，比对 monoPARPs 的选择性高 300 倍，比对 polyPARPs 的选择性高 1000 倍。
T76371	Tumor targeted pro-apoptotic peptide
	Tumor targeted pro-apoptotic peptide (CNGRC-GG-D(KLAKLAK)2) 为抗肿瘤肽，具有破坏线粒体膜和促进细胞凋亡功能，展现小鼠的抗癌活性。
T4169	N-Nitroso-N-methylurea 1-甲基-1-亚硝基脲,1-Methyl-1-nitrosourea,N-Methyl-N-nitrosourea,Methylnitrosourea	Others; DNA Alkylator/Crosslinker	DNA Damage/DNA Repair; Others
	N-Nitroso-N-methylurea (Methylnitrosourea) 是一种具有烷基化、致癌和致突变特性的亚硝基脲化合物。它靶向多种动物器官，可引起各种癌症和变性疾病，可用于重氮甲烷合成。
T77059	Leronlimab PRO 140	CCR	Immunology/Inflammation; Microbiology/Virology
	Leronlimab (PRO 140) 是一种人源化 IgG4 抗 CCR5 单克隆抗体。leronlimumab 具有抗 HIV 病毒活性和抗肿瘤活性，抑制 CCR 介导的 HIV-1 病毒和小鼠肿瘤模型中癌细胞转移。Leronlimab 可用于研究 HIV 非酒精性脂肪性肝炎 (NASH) 和乳腺癌。
T14075	A-802715	IL Receptor	Immunology/Inflammation
	A-802715 是一种新型甲基黄嘌呤衍生物，可降低促炎物质的内源性形成和血液水平，并增加白细胞介素10受体和肿瘤坏死因子受体等抗炎物质的形成和血液水平。
T31020	CP 461 OSI 461,UNII-68OJX9I7DT,CP-461,CP461	Apoptosis; PDE	Apoptosis; Metabolism
	CP 461 (UNII-68OJX9I7DT) 是一种特异性 PDE2A 抑制剂，是一种新型促凋亡化合物，能抑制环 GMP 磷酸二酯酶，但不能抑制环氧化酶-1 或-2。CP 461 在体外可抑制多种人类肿瘤细胞系的生长，并选择性地诱导癌细胞系而不是正常细胞凋亡。
T15594	MKC8866	IRE1	Cell Cycle/Checkpoint
	MKC8866 是一种选择性IRE1 RNase 抑制剂，在体外的IC50为 0.29 μM，是水杨醛类似物。它抑制乳腺癌细胞中的 IRE1 RNase，导致促肿瘤因子的产生减少，并且可以抑制前列腺癌 (PCa) 肿瘤的生长。它强烈抑制二硫苏糖醇诱导的 XBP1s 表达，EC50为 0.52 μM。
T77493	Murlentamab 3C23K,GM102	Others	Others
	Murlentamab (GM102) 是一种人源化抗 AMHRII 抗体。Murlentama 具有潜在的抗肿瘤活性，可诱导巨噬细胞介导的抗体依赖的细胞介导的细胞毒性作用 (ADCC)。Murl可通过募，集、活化T细胞激发促炎和抗肿瘤内环境。Murlentama 通过促进幼稚的巨噬细胞定向，促进肿瘤相关巨噬细胞 (TAM) 重编程来发挥抗肿瘤活性。
T67924	ABzOH
	ABzOH 是一种苯甲酸衍生物，结构类似于阿司匹林等非甾体抗炎药，具有抗炎、抗肿瘤和抗增殖作用。ABzOH 不仅可以抑制肿瘤坏死因子- α (TNF-a)、白细胞介素-1β (IL-1β)和白细胞介素-6 (IL-6)等促炎细胞因子的表达还对乳腺癌、肺癌和胰腺癌具有抑制作用。
T1185	Rofecoxib MK 966,罗非昔布,罗非考昔,MK-0966	COX	Immunology/Inflammation; Neuroscience
	Rofecoxib (MK 966) 是可口服的 COX-2特异性抑制剂，具有抗炎、解热和镇痛特性以及潜在的抗肿瘤特性。在人骨肉瘤细胞和中国仓鼠卵巢细胞中，对人 COX-2 的 IC50值分别为 26 和 18 nM。
T60202	MMRi62 7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol	Ferroptosis	Apoptosis
	MMRi62 (7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol) 是一种铁死亡 (ferroptosis) 诱导剂，靶向 MDM2-MDM4 (抑癌基因 p53 负调控因子)。MMRi62 对胰腺导管腺癌 (PDAC) 细胞显示出 p53 独立的促凋亡 (apoptosis) 活性，并诱导其自噬 (autophagy)。MMRi62 诱导铁死亡，伴随着活性氧增加和铁蛋白重链 (FTH1) 溶酶体降解。MMRi62 还可导致突变型 p53 的蛋白酶体降解，并对具有 KRAS 和 TP53 高频突变特征的原位异种移植 PDAC 小鼠模型具有体内药效。
T38406	L-Proline 4-methoxy-β-naphthylamide hydrochloride H-Pro-4MβNA hydrochloride,L-Proline 4-methoxy-β-naphthylamide hydrochloride
	L-Proline 4-methoxy-β-naphthylamide hydrochloride, also known as H-Pro-4MβNA hydrochloride, is a chemical compound utilized in the preparation of Fap-activated anti-tumor compounds.
T80687	γ3-MSH
	γ3-MSH 源于 pro-opiomelanocortin (POMC) 的 N 端，能够激活人肾上腺肿瘤细胞分泌醛固酮。
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).
T82633	Cys-Asp-Pro-Gly-Tyr-Ile-Gly-Ser-Arg-NH2
	Cys-Asp-Pro-Gly-Tyr-Ile-Gly-Ser-Arg-NH2是源自层粘连蛋白B1链的线性肽，能够干预肿瘤细胞对基底膜的附着与侵袭，且表现出抗血管生成活性。
T80127	FITC-Ahx-Gly-Arg-Gly-Asp-Ser-Pro	Integrin	Cytoskeletal Signaling
	FITC-Ahx-Gly-Arg-Gly-Asp-Ser-Pro为FITC标记的GRGDSP，后者为整联蛋白(integrin)抑制剂，能阻止肿瘤细胞与血管内皮细胞粘附，进而抑制肿瘤转移。
T69821	AMP423
	AMP423 is a naphthyl derivative of 2-cyanoaziridine-1-carboxamide with structural similarity to the pro-oxidant anti-tumor agent imexon. AMP423 was active in SCID mice bearing 8226/S myeloma and SU-DHL-6 B-cell lymphoma tumors, with a median tumor growth delay (T-C) of 21 days (P = 0.0002) and 5 days (P = 0.004), respectively, and a median tumor growth inhibition (T/C) of 33.3% (P = 0.03) and 82% (P = 0.01), respectively. In non-tumor-bearing mice, AMP423 was not myelosuppressive.
T69223	CC-1088
	CC-1088 is an analog of thalidomide with potential antineoplastic activity that belongs to the functional class of agents called selective cytokine inhibitory drugs (SelCIDs). SelCIDs inhibit phosphodiesterase-4 (PDE 4), an enzyme involved in tumor necrosis factor alpha (TNF alpha) production. CC-1088 inhibits production of the cytokines vascular endothelial growth factor (VEGF) (a pro-angiogenic factor) and interleukin-6 (IL-6).
T76315	HKPao
	HKPao (Hunter-killer peptide ao) 是一种具有抗肥胖和抗肿瘤促凋亡活性的生物活性肽，能够促使细胞释放囊泡中的细胞色素 c。
T72570	Antitumor agent-83
	Antitumor agent-83 是一种促凋亡蛋白 BAX 的激活剂，对肿瘤细胞有显著的抗增殖作用。Antitumor agent-83 通过诱导 BAX 的构象激活介导细胞凋亡 (Apoptosis)，对 A549 细胞周期有抑制作用。Antitumor agent-83 具有良好的体外代谢稳定性和 CYP 谱。
T28874	SU11652 SU-11652,SU 11652
	SU11652 is a potent cell-permeable pyrrole-indolinone compound. SU11652 acts as an ATP-competitive tyrosine kinase receptor and angiogenic inhibitor with greater selectivity for PDGFR-β (PDGFRβ, IC50 = 3 nM), Flk-1 (VEGFR2, IC50 = 27 nM), FGFR1 (IC50= 170
T37861	Talabostat
	Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9,...

化合物

Cat.No: T22414

Target: PARP

Tumor targeted pro-apoptotic peptide

Cat.No: T76371

N-Nitroso-N-methylurea

Cat.No: T4169

Synonym: 1-甲基-1-亚硝基脲,1-Methyl-1-nitrosourea,N-Methyl-N-nitrosourea,Methylnitrosourea

Target: Others, DNA Alkylator/Crosslinker

Cat.No: T77059

Synonym: PRO 140

Target: CCR

Cat.No: T14075

Target: IL Receptor

Cat.No: T31020

Synonym: OSI 461,UNII-68OJX9I7DT,CP-461,CP461

Target: Apoptosis, PDE

Cat.No: T15594

Target: IRE1

Cat.No: T77493

Synonym: 3C23K,GM102

Target: Others

Cat.No: T67924

Cat.No: T1185

Synonym: MK 966,罗非昔布,罗非考昔,MK-0966

Target: COX

Cat.No: T60202

Synonym: 7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol

Target: Ferroptosis

L-Proline 4-methoxy-β-naphthylamide hydrochloride

Cat.No: T38406

Synonym: H-Pro-4MβNA hydrochloride,L-Proline 4-methoxy-β-naphthylamide hydrochloride

Cat.No: T80687

Cat.No: T69599

Cys-Asp-Pro-Gly-Tyr-Ile-Gly-Ser-Arg-NH2

Cat.No: T82633

FITC-Ahx-Gly-Arg-Gly-Asp-Ser-Pro

Cat.No: T80127

Target: Integrin

Cat.No: T69821

Cat.No: T69223

Cat.No: T76315

Antitumor agent-83

Cat.No: T72570

Cat.No: T28874

Synonym: SU-11652,SU 11652

Cat.No: T37861

Cat. No.	Product Name	Target	Signaling Pathways
T8193	α-Thujone Thujone,ALPHA-(-)-THUJONE,α-侧柏酮,(-)-α-侧柏酮	Apoptosis; Reactive Oxygen Species; GABA Receptor; AChR; Parasite; Autophagy	Apoptosis; Autophagy; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; NF-κB
	α-Thujone 是一种从西方金钟柏精油中分离出来的单萜，可穿透血脑屏障。它是 GABAA 受体的可逆调节剂，在抑制 GABA 诱导的电流时，它的 IC50为 21 μM。它诱导 ROS 依赖性细胞毒性，还诱导细胞凋亡和自噬。它具有抗伤害，抗肿瘤、杀虫和驱虫活性。
TN1291	7,3',4'-Tri-O-methylluteolin 5-Hydroxy-3',4',7-trimethoxyflavone,木犀草素-7,3',4'-三甲醚	TNF; COX; Interleukin	Apoptosis; Immunology/Inflammation; Neuroscience
	7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) 是来自草药马鞭草科的一种类黄酮，具有抗炎，解热，镇咳，抗糖尿病、抗癌和抗黑素生成特性。它以浓度依赖方式明显抑制促炎细胞因子，可显著降低在转录水平的诱导型一氧化氮合酶和环加氧酶-2 的 mRNA 表达。
T3395	Timosaponin AIII Filiferin B,知母皂苷 A-III,AneMarsaponin A3,Timosaponin A3	AChE; mTOR	Neuroscience; PI3K/Akt/mTOR signaling
	Timosaponin AIII (Timosaponin A3) 是一种乙酰胆碱酯酶活性抑制剂，其IC50=35.4 μM。
T3S0737	Flavokawain A 2'-羟基-4,4',6'-三甲氧基查耳酮,Flavokavain A	Apoptosis; p38 MAPK	Apoptosis; MAPK
	Flavokawain A (Flavokavain A) 是 kava 提取物中的查耳酮，是一种抗癌试剂，具有抗肿瘤活性。它通过 Bax 蛋白依赖和线粒体依赖的凋亡途径诱导细胞凋亡，有潜力用于膀胱癌的相关研究。
T36715	Tetrac Tetraiodothyroacetic acid,3,3',5,5'-Tetraiodothyroacetic acid	Apoptosis; EGFR	Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Tetrac (Tetraiodothyroacetic acid)是L-甲状腺素(T4)的衍生物，是一种甲状腺整合素受体拮抗剂。Tetrac通过阻断EGFR介导的结直肠癌细胞信号传导来诱导抗增殖。Tetrac 可阻断 T4 和 3,5,3'-triiodo-L-thyronine (T3)在细胞表面甲状腺素整合素 αvβ3 受体上的作用。Tetra 具有抗血管生成、抗肿瘤活性和促凋亡活性。
T2S2264	Linalool Linalol,(±)-Linalool,Phantol,沉香醇	Apoptosis; IL Receptor; TNF; Endogenous Metabolite; iGluR	Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience
	Linalool (Linalol) 是存在芫荽等植物中的单萜类天然产物，是竞争性NMDA 受体拮抗剂，具有抗肿瘤和抗心脏毒性的作用。它通过激活 Nrf2 诱导抗氧化防御和通过抑制 NF-κB 减少炎症反应来保护其免受 LPS/GalN 诱导的肝损伤，具有镇痛、抗菌和抗炎的特性。
TMA2576	Episappanol	IL Receptor; TNF	Apoptosis; Immunology/Inflammation
	Episappanol has anti-inflammatory activity , it can significantly inhibit the secretion of the pro-inflammatory cytokines interleukin (IL-6) and tumor necrosis factor-alpha (TNF-α).

天然产物

Cat.No: T8193

Synonym: Thujone,ALPHA-(-)-THUJONE,α-侧柏酮,(-)-α-侧柏酮

Target: Apoptosis, Reactive Oxygen Species, GABA Receptor, AChR, Parasite, Autophagy

7,3',4'-Tri-O-methylluteolin

Cat.No: TN1291

Synonym: 5-Hydroxy-3',4',7-trimethoxyflavone,木犀草素-7,3',4'-三甲醚

Target: TNF, COX, Interleukin

Timosaponin AIII

Cat.No: T3395

Synonym: Filiferin B,知母皂苷 A-III,AneMarsaponin A3,Timosaponin A3

Target: AChE, mTOR

Cat.No: T3S0737

Synonym: 2'-羟基-4,4',6'-三甲氧基查耳酮,Flavokavain A

Target: Apoptosis, p38 MAPK

Cat.No: T36715

Synonym: Tetraiodothyroacetic acid,3,3',5,5'-Tetraiodothyroacetic acid

Target: Apoptosis, EGFR

Cat.No: T2S2264

Synonym: Linalol,(±)-Linalool,Phantol,沉香醇

Target: Apoptosis, IL Receptor, TNF, Endogenous Metabolite, iGluR

Cat.No: TMA2576

Target: IL Receptor, TNF

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