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19

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9927	Panitumumab	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Panitumumab 是一种重组全人源 IgG2 单克隆抗体，可与表皮生长因子(EGFR)结合，具有抗肿瘤活性。
T13224	Tubulin inhibitor 6 iHAP1	Microtubule Associated	Cytoskeletal Signaling
	Tubulin inhibitor 6 (iHAP1) 是一种微管蛋白抑制剂，抑制微管蛋白聚合，IC50为 0.87 μM。它抑制多种癌细胞系，抑制 K562 细胞生长，IC50为 840 nM。
T5007	Benproperine phosphate 磷酸苯丙哌林,Blascorid,Pirexyl phosphate	Others; Microtubule Associated	Cytoskeletal Signaling; Others
	Benproperine phosphate (Pirexyl phosphate) 是一种具有口服活性的，肌动蛋白相关蛋白 2/3 复合亚基 2 (ARPC2) 抑制剂。它通过削弱 Arp2/3 功能来减弱肌动蛋白的聚合反应速率。它可抑制癌细胞迁移和肿瘤转移，有用于治疗止咳的潜力。
T5208	BAY-8002 BAY8002,BAY 8002	Monocarboxylate transporter	Membrane transporter/Ion channel
	BAY-8002 是一种可口服的单羧酸转运蛋白第 1 亚型 MCT1 选择性抑制剂，在表达 MCT1 的 DLD-1 细胞中，IC50值为 85 nM，具有抗肿瘤活性。
T60485	DIF-3
	DIF-3 is a chemical compound that acts by activating GSK-3β to facilitate the degradation of cyclin D1 and c-Myc, resulting in reduced expression levels of these proteins. In addition, DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. This compound exerts a potent antiproliferative effect on the HeLa human cervical cancer cell line by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression [1].
T6768	AZ6102	PARP; Wnt/beta-catenin	Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; Stem Cells
	AZ6102 是TNKS1和TNKS2双重抑制剂，IC50值分别为 3 和 1 nM，选择性是对 PARP 家族其他蛋白的 100 多倍，对 PARP1、PARP2 和 PARP6 的IC50值分别为 2.0、0.5 和大于 3 μM。
T68449	JFD00950
	JFD00950 is a human flap endonuclease 1 (FEN1) inhibitor with in vitro inhibition of flap cleavage activity as well as cytotoxic activity against a colon cancer cell line, DLD-1.
T36702	CAY10753
	CAY10753 is an inhibitor of tankyrase 2 (TNKS2; IC50= 0.3 nM).1It is selective for TNKS2 over TNKS1 (IC50= 6.1 nM), as well as poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 89.6 and 37.8 nM, respectively). CAY10753 inhibits proliferation of DLD-1 colorectal cancer cells when used at a concentration of 1 μM. 1.Tomassi, S., Pfahler, J., Mautone, N., et al.From PARP1 to TNKS2 inhibition: A structure-based approachMed. Chem. Lett.(2020)
T36409	Roccellic Acid
	Roccellic acid is a lichen secondary metabolite that has been found in R. montagnei and has antibacterial and anticancer activities.1,2 It is active against the bacteria S. gordonii and P. gingivalis (MIC = 46.9 μg/ml for both).1 Roccellic acid (100 μg/ml) inhibits proliferation of MDA-MB-231, MCF-7, and DLD-1 cancer cells by 65.3, 75.8, and 87.9%, respectively.2 \|1. Sweidan, A., Chollet-Krugler, M., Sauvager, A., et al. Antibacterial activities of natural lichen compounds against Streptococcus ...
T35690	Myceliothermophin E
	Myceliothermophin E is a polyketide-amino acid hybrid fungal metabolite that has been found inT. thermophilusand has anticancer and antimicrobial activities.1,2It is cytotoxic to DLD-1, Hep3B, HepG2, and HGC-27 cancer cells (IC50s = 0.32, 0.42, 0.26, and 0.08 μg/ml, respectively).1Myceliothermophin E is active against methicillin-resistant, but not -sensitive,S. aureus(MICs = 15.8 and >100 μM, respectively).2 1.Gao, Y.-L., Zhang, M.-L., Wang, X., et al.Isolation and characterization of a new cyt...
T81446	PKM2 activator 6
	PKM2 activator 6 (Compound Z10) 作为一种PKM2激活剂同时抑制PDK1，其KD值分别为121 μM和19.6 μM。该化合物诱导结直肠细胞发生凋亡，并显著抑制细胞增殖与迁移。通过抑制糖酵解作用，PKM2 activator 6降低DLD-1、HCT-8、HT-29、MCF-10A细胞的增殖，IC50值分别为10.04、2.16、3.57、66.39 μM。
T70138	AZ0108
	AZ0108 is an orally bioavailable, potent PARP1,2,6 inhibitor that potently inhibits centrosome clustering and is suitable for in vivo efficacy and tolerability studies. AZ0108 has been utilized as in vitro tools and in vivo probes to investigate the biological consequences of inhibiting centrosome clustering through PARP enzymes. AZ0108 is more selective in its enzyme inhibition profile and effects on cellular pathways and phenotypes. Specifically, AZ0108 inhibits PARPs 1, 2, and 6 with approxi...
T78157	PARP-1-IN-3	Apoptosis; PARP	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair
	PARP-1-IN-3 是一种高效的 PARP-1 抑制剂，对 PARP-1 和 PARP-2 具有抑制作用， IC50 值分别为 0.25 nM 和 2.34 nM。PARP-1-IN-3 具有潜在的抗炎活性，促使细胞凋亡并使细胞周期停滞在 G2/M 期。PARP-1-IN-3 可用于研究与癌症相关的疾病。
T36698	9(Z),11(E),13(E)-Octadecatrienoic Acid
	9(Z),11(E),13(E)-Octadecatrienoic Acid (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1...
T38381	CAY17c
	CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620,...
T36887	8(E),10(E),12(Z)-Octadecatrienoic Acid
	8(E),10(E),12(Z)-Octadecatrienoic acid is a conjugated polyunsaturated fatty acid (PUFA) that has been found inC. officinalisseed oil and has anticancer activity.1,2,3It inhibits the growth of Caco-2 cells when used at concentrations ranging from 10 to 50 μM.28(E),10(E),12(Z)-Octadecatrienoic acid (10 μM) induces formation of thiobarbituric acid reactive substances (TBARS) and apoptosis in DLD-1 colorectal adenocarcinoma cells.3It also inhibits prostaglandin biosynthesis in sheep vesicular gland...
T36888	9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester
	9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPA...
T36889	Methyl alpha-eleostearate
	Methyl alpha-eleostearate (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supple...
T13226	Tubulin inhibitor 8	Microtubule Associated	Cytoskeletal Signaling
	Tubulin inhibitor 8是管蛋白和多种癌症细胞系的抑制剂，对管蛋白聚合和K562细胞生长具有抑制作用，IC50分别为0.73μM 和14nM。

化合物

Cat.No: T9927

Target: EGFR

Tubulin inhibitor 6

Cat.No: T13224

Synonym: iHAP1

Target: Microtubule Associated

Benproperine phosphate

Cat.No: T5007

Synonym: 磷酸苯丙哌林,Blascorid,Pirexyl phosphate

Target: Others, Microtubule Associated

Cat.No: T5208

Synonym: BAY8002,BAY 8002

Target: Monocarboxylate transporter

Cat.No: T60485

Cat.No: T6768

Target: PARP, Wnt/beta-catenin

Cat.No: T68449

Cat.No: T36702

Cat.No: T36409

Myceliothermophin E

Cat.No: T35690

PKM2 activator 6

Cat.No: T81446

Cat.No: T70138

Cat.No: T78157

Target: Apoptosis, PARP

9(Z),11(E),13(E)-Octadecatrienoic Acid

Cat.No: T36698

Cat.No: T38381

8(E),10(E),12(Z)-Octadecatrienoic Acid

Cat.No: T36887

9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester

Cat.No: T36888

Methyl alpha-eleostearate

Cat.No: T36889

Tubulin inhibitor 8

Cat.No: T13226

Target: Microtubule Associated

Cat. No.	Product Name	Target	Signaling Pathways
T38243	Hygrolidin
	Hygrolidin is a macrocyclic lactone originally isolated from S. hygroscopicus. It inhibits proliferation of a variety of cancer cell lines, including DLD-1 colon cancer, LNCaP prostate cancer, and K562 leukemia cells (IC50s = 2.9, 5.2, and 33 ng/ml, respectively). Hygrolidin induces the expression and levels of p21 in DLD-1 cells, but not WI-38 fibroblasts, and leads to cell accumulation in the G1 and S phases without inducing apoptosis. It has antiparasitic activity against T. cruzi, L. donovan...
TN5538	6-Methoxykaempferol	Others	Others
	6-Methoxykaempferol 是一种存在于 brazilian propolis 中的黄酮。6-Methoxykaempferol 对癌细胞具有抗增殖活性，对离体大鼠脑突触体的神经保护作用，可降低的谷胱甘肽水平。6-Methoxykaempferol 表现出一定的脂肪酶活性，可用于恶病质的治疗。

天然产物

Cat.No: T38243

6-Methoxykaempferol

Cat.No: TN5538

Target: Others

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