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15

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T6157	Devimistat CPI-613,辛酸,CPI613,CPI 613,6,8-Bis(benzylthio)octanoic acid	Apoptosis; Dehydrogenase; Mitochondrial Metabolism	Apoptosis; Metabolism
	Devimistat (6,8-Bis(benzylthio)octanoic acid) 是一种线粒体代谢抑制剂，还是一种lipoic acid 拮抗剂，能阻断线粒体能量代谢，诱导多种癌细胞凋亡。
T7830	Windorphen	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	Windorphen 是一种 Wnt 抑制剂，可选择性地消除 Wnt 信号传导。
T29087	VA-K-14 hydrochloride VAK14 Hydrochloride,VA K 14 HCl,VA-K-14 HCl,VAK14 HCl	TSH Receptor	GPCR/G Protein
	VA-K-14 hydrochloride（VAK14 HCl）是一种选择性促甲状腺激素受体 (TSHR) 拮抗剂 (IC50= 12.3 μM)，对GD患者血清和单克隆刺激TSHR抗体对TSHR的刺激有抑制作用，可消除 TSHR 信号传导。
T7771	Brilliant Blue FCF FD&C Blue No. 1,Erioglaucine disodium salt,Acid Blue 9,E133,食用色素亮蓝	Others	Others
	Brilliant Blue FCF (Erioglaucine disodium salt) 是一种从石油中生产的合成染料，是一种芳香族烃类，用于食品和其它物质的着色剂，溶液最大吸收在628 nm。
T68455	AP23846 AP-23846	Src	Angiogenesis; Tyrosine Kinase/Adaptors
	AP23846 是一种新型高效的 Src 家族激酶抑制剂，可降低人实体瘤细胞系中血管内皮生长因子和白细胞介素-8 的表达，并消除下游血管生成过程。
T26629	Angstrom6 A-6,A 6 peptide,A6,A 6,A6 peptide,A-6 peptide	PAI-1	Metabolism
	Angstrom6 (A-6 peptide) 是一种从单链尿激酶纤溶酶原激活剂(scuPA)中提取的 8 肽，它能干扰 uPA/uPAR 级联反应并抑制下游效应。Angstrom6 具有抗肿瘤活性，能通过与 CD44 结合并调节 CD44 介导的细胞信号传导，抑制肿瘤细胞的迁移、侵袭和转移。
T73499	NG-497 NG497	Lipase	Metabolism
	NG-497 是一种具有选择性的小分子人类的脂肪甘油三酯脂肪酶 (ATGL) 抑制剂，可以靶向人类 ATGL 的酶促活性 patatin 样结构域。NG-497在活性位点附近的疏水腔内结合ATGL。NG-497以剂量依赖性和可逆的方式消除人脂肪细胞中的脂肪分解。NG-497 可用于研究癌症。
T21792	CGP 3466B maleate 马来酸CGP3466B,Omigapil (Maleate),Omigapil maleate	Apoptosis	Apoptosis
	CGP 3466B maleate (Omigapil maleate) 是一种口服有效的 GAPDH 亚硝基化抑制剂，可消除 Aβ1-42 诱导的小鼠 tau 乙酰化，记忆障碍和运动功能障碍，Omigapil maleate 具有研究阿尔茨海默症的潜力。Omigapil maleate (CGP3446B maleate) 是一种有效的凋亡 (apoptosis) 抑制剂。Omigapil maleate 可用于研究先天性肌营养不良 (CMD)。
T14904	CCT244747	Chk	Cell Cycle/Checkpoint
	CCT244747 is a CHK1 inhibitor (IC50: 7.7 nM) and also abrogates G2 checkpoint (IC50: 29 nM).
T68895	CBP-93872
	CBP-93872 is a G2 checkpoint inhibitor. CBP-93872 specifically abrogates the DNA double-stranded break (DSB)-induced G2 checkpoint through inhibiting maintenance. CBP-93872 is an inhibitor of maintenance of the DSB-specific G2 checkpoint and thus might be a strong candidate as the basis for a drug that specifically sensitizes p53-mutated cancer cells to DSB-inducing DNA damage therapy.
T70994	TAK-659 HCl
	TAK-659 is an inhibitor of spleen tyrosine kinase (syk), with potential anti-inflammatory, immunomodulating, and antineoplastic activities. Spleen tyrosine kinase inhibitor TAK-659 may inhibit the activity of syk, which abrogates downstream B-cell receptor (BCR) signaling and leads to an inhibition of B-cell activation, chemotaxis, adhesion and proliferation. Note: TAK-659 free base is less stable. This product is supplied as dihydrochloride form.
T70844	CM-118
	CM-118 is a potent and selective dual inhibitor of c-Met and ALK which potently abrogates hepatocyte growth factor (HGF)-induced c-Met phosphorylation and cell migration, as well as phosphorylation of ALK, EML4-ALK, and ALK resistance mutants in transfected cells.
T69723	Taminadenant mesylate
	Taminadenant, also known as PBF-509 and NIR-178, is a potent and orally active adenosine A2A receptor antagonist with potential antineoplastic activity. PBF-509 selectively binds to and inhibits A2AR expressed on T lymphocytes. This abrogates the adenosine/A2AR-mediated inhibition of T-lymphocytes and activates a T-cell-mediated immune response against tumor cells, thereby reducing proliferation of susceptible tumor cells. A2AR, a G protein-coupled receptor, is highly expressed on the cell sur...
T69682	AEW541 HCl
	AEW541, also known as NVP-AEW541, is a novel, potent IGF-IR kinase inhibitor. NVP-AEW541 is capable of distinguishing between the IGF-IR (IC50 = 0.086 microM) and the closely related InsR (IC50 = 2.3 microM) in cells. NVP- AEW541 abrogates IGF-I-mediated survival and colony formation in soft agar at concentrations that are consistent with inhibition of IGF-IR autophosphorylation. Note: AEW541 has a Cis-configuration on the cyclobutane ring. Its CAS# is 475489-16-8. Many vendors and Sc-finder sc...
T37602	GSK 143
	Spleen tyrosine kinase (Syk) inhibitor (pIC50 = 7.5). Also inhibits phosphorylated Erk (pIC50 = 7.1). Decreases cell number and viability in chronic lymphocytic leukemia (CCL) cell lines. Liddle et al (2011) Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. Bioorg.Med.Chem.Lett. 21 6188 PMID:21903390 \|Varghese et al (2018) Highly selective SYK inhibitor, GSK143, abrogates survival signals in chronic lymphocytic leukaemia. Br.J.Haematol 182 9...

化合物

Cat.No: T6157

Synonym: CPI-613,辛酸,CPI613,CPI 613,6,8-Bis(benzylthio)octanoic acid

Target: Apoptosis, Dehydrogenase, Mitochondrial Metabolism

Cat.No: T7830

Target: Wnt/beta-catenin

VA-K-14 hydrochloride

Cat.No: T29087

Synonym: VAK14 Hydrochloride,VA K 14 HCl,VA-K-14 HCl,VAK14 HCl

Target: TSH Receptor

Brilliant Blue FCF

Cat.No: T7771

Synonym: FD&C Blue No. 1,Erioglaucine disodium salt,Acid Blue 9,E133,食用色素亮蓝

Target: Others

Cat.No: T68455

Synonym: AP-23846

Target: Src

Cat.No: T26629

Synonym: A-6,A 6 peptide,A6,A 6,A6 peptide,A-6 peptide

Target: PAI-1

Cat.No: T73499

Synonym: NG497

Target: Lipase

CGP 3466B maleate

Cat.No: T21792

Synonym: 马来酸CGP3466B,Omigapil (Maleate),Omigapil maleate

Target: Apoptosis

Cat.No: T14904

Target: Chk

Cat.No: T68895

Cat.No: T70994

Cat.No: T70844

Taminadenant mesylate

Cat.No: T69723

Cat.No: T69682

Cat.No: T37602

Cat. No.	Product Name	Target	Signaling Pathways
T36961	Malformin C
	Malformin C is a natural fungus-derived bicyclic pentapeptide that has antibacterial properties, particularly against species of Bacillus. Malformin C potently blocks the ability of bleomycin to induce G2 arrest in human T-cell leukemia-derived Jurkat cells (IC50 = 0.9 nM). It less potently abrogates colchicine-induced M phase arrest in Jurkat cells (IC50 = 24 nM). Malformin C inhibits cell growth dose-dependently in Colon 38 and HCT 115 cancer cells (IC50s = 0.27 and 0.18 μM, respectively) but ...

天然产物

Cat.No: T36961

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