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13

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T23372	SMIFH2	Others	Others
	SMIFH2 是formin 特异性抑制剂。它利用 Formins 阻碍肌动蛋白聚合，影响肌动蛋白细胞骨架。
T5994	KPT-6566 2-[[4-[[[4-(叔丁基)苯基]磺酰基]亚氨基]-1-氧代-1,4-二氢-2-萘基]硫基]乙酸	Others	Others
	KPT-6566 是共价结合的脯氨酰异构酶PIN1选择性抑制剂，能够与 PIN1 的催化位点共价结合，抑制并降解PIN1，具有抗癌活性。它对PIN1 PPIase 结构域的IC50=640 nM，Ki=625.2 nM。
T4102	Goserelin acetate 醋酸戈舍瑞林,Fertilan,ICI-118630 acetate,Zoladex	Apoptosis; GNRH Receptor	Apoptosis; GPCR/G Protein
	Goserelin acetate (Fertilan) 是一种促性腺激素释放激素 (GnRH/LHRH) 十肽类似物，能作为GnRH 激动剂。它可研究乳腺癌、上皮性卵巢癌和前列腺癌。
T38752	EW-7195	ALK; TGF-beta/Smad	Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors
	EW-7195 是一种具有选择性和高效性的 ALK5 (TGFβR1) 抑制剂，IC50 值为 4.83 nM。EW-7195 对 ALK5 的亲和力是 p38α 的 300 多倍。EW-7195 对 TGF-β1 诱导的 Smad 信号转导、上皮间质转化 (EMT) 和乳腺癌向肺转移有抑制作用。
T77701	FL118 FL 118,FL-118,10,11-(Methylenedioxy)-20(S)-camptothecin	Survivin	Apoptosis
	FL118是一种新型存活素抑制剂，可抑制癌症干细胞样特性。FL118 是一种新型喜树碱类似物，具有抗癌活性，通过 Wnt/β-catenin 信号通路抑制上皮-间充质转化，从而抑制人乳腺癌细胞的迁移和侵袭。
T36696	DMBA
	7,12-Dimethylbenz[a]anthracene (DMBA) is a polycyclic aromatic hydrocarbon (PAH) that has been found in tobacco smoke and diesel exhaust and has carcinogenic activity.1,2It undergoes metabolic activation by numerous enzymes, including the cytochrome P450 (CYP450) isoform CYP1B1, as well as microsomal epoxide hydrolase (mEH), producing a variety of reactive metabolites that form DNA adductsin vivo, and it has been commonly used to induce tumor formation in various rodent models.2,3,1DMBA increase...
T36860	C22 Sphingomyelin (d18:1/22:0) C22 Sphingomyelin (d18:1/22:0)
	C22 Sphingomyelin is a naturally occurring form of sphingomyelin . Plasma levels of C22 sphingomyelin positively correlate with hepatic steatosis severity in patients with chronic hepatitis C virus (HCV). C22 Sphingomyelin levels are decreased in T-47D mammary epithelial cells and increased in MDA-MB-231 breast cancer cells relative to C16 sphingomyelin .
T63827	HSP90-IN-10
	HSP90-IN-10 是 HSP90 的有效抑制剂。HSP90-IN-10 对 HCC1954 乳腺癌细胞表现出强大的抗增殖效果 (IC50: 6 μM)。HSP90-IN-10 能够诱导细胞凋亡 (apoptosis)，且不抑制正常上皮细胞的生长。
T37564	C4 Ceramide (d18:1/4:0) C4 Ceramide (d18:1/4:0),Cer(d18:1/4:0)
	C4 Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. [1] [2] [3] It inhibits IL-4 production by 16% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. [1] C4 Ceramide is cytotoxic to SK-BR-3 and MCF-7/Adr breast cancer cells (IC50s = 15.9 and 19.9 μM, respectively). [2] C4 Ceramide also increases maturation and stability of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing...
T36460	CAY10736 CAY10736
	CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a ...
T36497	CAY10735 CAY10735
	CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells ...
T73419	JMX0293
	JMX0293是一种O-烷基氨基连接的水杨酰胺衍生物化合物，具有针对MDA-MB-231细胞系的高效力(IC50=3.38 μM)，且对MCF-10A人非致瘤性乳腺上皮细胞系的毒性极低(IC50>60 μM)。该化合物能抑制STAT3磷酸化，促进TNBC MDA-MB-231细胞的凋亡，同时在体内显著抑制MDA-MB-231异种移植肿瘤的生长，无明显毒性。
T83765	Dendrogenin A DDA
	Dendrogenin A (DDA) 作为一种选择性肝X受体(LXR)调节剂(SLiM)、胆固醇环氧水解酶(ChEH; Ki = 120 nM)的抑制剂及胆固醇的活性代谢产物，通过DDA合成酶将5,6α-环氧胆固醇与组胺结合形成。DDA在非癌性人乳腺上皮细胞和上皮黑色素细胞中存在，但在多种乳腺癌细胞或黑色素瘤细胞中未发现，且在分离的人乳腺肿瘤组织中仅以低水平存在。它抑制22(R)-羟基胆固醇诱导的LXRβ和LXRα激活(分别以IC50 = 76和362 nM)，但也是LXR的部分激动剂，在B16/F10小鼠黑色素瘤细胞中增加Nur77、NOR-1、LC3-I和LC3-II的蛋白水平。DDA选择性调节LXRα和LXRβ，而非孕烯X受体(PXR)、芳香烃受体(AhR)、维生素D受体(VDR)、维甲酸X受体γ(RXRγ)、维甲酸受体α(RARα)、过氧化物酶体增殖物激活受体α(PPARα)、PPARγ、糖皮质激素受体、雄激素受体、雌激素受体α(ERα)及ERβ在2.5 µM下。此外，DDA在2.5和5 µM的浓度下增加B16/F10和SK-MEL-28癌细胞中LC3-II的蛋白水平，并在2...

化合物

Cat.No: T23372

Target: Others

Cat.No: T5994

Synonym: 2-[[4-[[[4-(叔丁基)苯基]磺酰基]亚氨基]-1-氧代-1,4-二氢-2-萘基]硫基]乙酸

Target: Others

Goserelin acetate

Cat.No: T4102

Synonym: 醋酸戈舍瑞林,Fertilan,ICI-118630 acetate,Zoladex

Target: Apoptosis, GNRH Receptor

Cat.No: T38752

Target: ALK, TGF-beta/Smad

Cat.No: T77701

Synonym: FL 118,FL-118,10,11-(Methylenedioxy)-20(S)-camptothecin

Target: Survivin

Cat.No: T36696

C22 Sphingomyelin (d18:1/22:0)

Cat.No: T36860

Synonym: C22 Sphingomyelin (d18:1/22:0)

Cat.No: T63827

C4 Ceramide (d18:1/4:0)

Cat.No: T37564

Synonym: C4 Ceramide (d18:1/4:0),Cer(d18:1/4:0)

Cat.No: T36460

Synonym: CAY10736

Cat.No: T36497

Synonym: CAY10735

Cat.No: T73419

Cat.No: T83765

Synonym: DDA

Cat. No.	Product Name	Target	Signaling Pathways
T4S0969	Obtusifolin 决明蒽醌,决明蒽醌；美决明子素	Antioxidant; NF-κB	NF-κB; oxidation-reduction
	Obtusifolin 是分离自决明子的种子中，能够抑制NF-kB 通路，调节气道上皮细胞中 MUC5AC 粘蛋白的基因表达和产生。它通过靶向甲状旁腺激素相关蛋白来抑制邻苯二甲酸酯诱导的乳腺癌骨转移。
T7982	3,6-Dihydroxyflavone	Others	Others
	3,6-Dihydroxyflavone 是一种抗癌剂。它能够提高细胞内氧化应激和脂质过氧化。它是能够根据剂量和时间依赖性地降低细胞活力，并活化半胱天冬酶级联、切割聚 (ADP-核糖) 聚合酶 (PARP) 诱导细胞凋亡。
T3330	trans-Trimethoxyresveratrol trans-trismethoxy Resveratrol,E-Resveratrol Trimethyl Ether,MR-3,Tri-O-methylresveratrol,白藜芦醇三甲醚,3,4',5-Trimethoxy-trans-stilbene,Trimethoxystilbene	Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	trans-Trimethoxyresveratrol (MR-3) 是一种 Resveratrol(RSV) 的衍生物，与Resveratrol(RSV)相比，它可能是一个更有效的抗炎、抗血管新生的化合物。
T4S0797	Berberine 小檗碱,Berberin,Umbellatine,黄连素	Reactive Oxygen Species; Topoisomerase; Endogenous Metabolite; Antibacterial; Antibiotic; Autophagy	Autophagy; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB
	Berberine (Umbellatine) 是从中草药黄连中分离出来的一种生物碱抗生素。它诱导活性氧生成并抑制 DNA 拓扑异构酶，具有抗肿瘤特性。

天然产物

Cat.No: T4S0969

Synonym: 决明蒽醌,决明蒽醌；美决明子素

Target: Antioxidant, NF-κB

3,6-Dihydroxyflavone

Cat.No: T7982

Target: Others

trans-Trimethoxyresveratrol

Cat.No: T3330

Synonym: trans-trismethoxy Resveratrol,E-Resveratrol Trimethyl Ether,MR-3,Tri-O-methylresveratrol,白藜芦醇三甲醚,3,4',5-Trimethoxy-trans-stilbene,Trimethoxystilbene

Target: Reactive Oxygen Species

Cat.No: T4S0797

Synonym: 小檗碱,Berberin,Umbellatine,黄连素

Target: Reactive Oxygen Species, Topoisomerase, Endogenous Metabolite, Antibacterial, Antibiotic, Autophagy

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