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19

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7196	HG-10-102-01 [4-[[5-氯-4-(甲基氨基)-2-嘧啶基]氨基]-3-甲氧基苯基]-4-吗啉基甲酮	LRRK2	Autophagy
	HG-10-102-01 是富含亮氨酸重复激酶 2 和突变型G2019S 抑制剂，IC50分别为20.3 nM 和3.2 nM。
T21312	Afatinib 阿法替尼,Afatinib free base,BIBW 2992	EGFR; Autophagy	Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Afatinib (BIBW 2992) 是一种不可逆的 EGFR 家族抑制剂，抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。
T1773	Afatinib Dimaleate 马来酸阿法替尼,双马来酸盐阿法替尼,BIBW2992,Afatinib,BIBW 2992MA2,Afatinib (BIBW2992) Dimaleate	EGFR; HER; Autophagy	Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Afatinib Dimaleate (BIBW 2992MA2) 是一种可口服的苯胺基-喹唑啉衍生物和受体酪氨酸激酶表皮生长因子受体家族的抑制剂，具有抗肿瘤活性。它抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。
T11212	EPAC 5376753 5-{[5-(2,4-dichlorophenyl)furan-2-yl]methylidene}-2-thioxodihydropyrimidine-4,6(1H,5H)-dione	cAMP	GPCR/G Protein
	EPAC 5376753 是 EPAC1 的变构抑制剂，在瑞士 3T3 细胞中的 IC50 为 4 µM。
T9650	AZ12672857	Src; Ephrin Receptor	Angiogenesis; Tyrosine Kinase/Adaptors
	AZ12672857 是一种 EphB4 抑制剂，IC50 为 1.3 nM。 AZ12672857 抑制 Src 转染 3T3 细胞的细胞增殖，IC50 为 2 nM，抑制转染 CHO-K1 细胞中 EphB4 的自磷酸化，IC50 为 9 nM。
T28740	SDZ-62-434 SDZ 62 434,SDZ62434	Platelet aggregation	Others
	SDZ-62-434 是一种血小板活化因子抑制剂，具有抗肿瘤活性，抑制静止的瑞士 3T3 细胞中 bombesin 和血小板衍生生长因子诱导的 DNA 合成，可用于研究白血病、人异种移植结直肠癌和肺癌。
T9491	Pyraclostrobin	Antibacterial; Antifungal	Microbiology/Virology
	Pyraclostrobin 是一种球果苷杀菌剂，可诱导 3T3-L1 细胞内甘油三酯的积累，还可抑制真菌和哺乳动物细胞的线粒体复合物 III 。
T60857	MKK7-COV-9	Others	Others
	MKK7-COV-9 是一种具有选择性和有效性的 MKK7 共价抑制剂，对 MKK7 引导的蛋白-蛋白相互作用有抑制作用。MKK7-COV-9 中断原代 B 细胞应对 LPS 的激活。MKK7-COV-9 在高浓度下显示出较低的细胞毒性。
T10849	CMLD012612	Others	Others
	CMLD012612 is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. It inhibits cell translation and is cytotoxic to NIH/3T3 cells (IC50: 2 nM).
T10848	CMLD012073	Others	Others
	CMLD012073 is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. It inhibits NIH/3T3 cells (IC50: 10 nM). CMLD012073 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A).
T83127	AMPK activator 13	AMPK	Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	AMPK activator13作为AMPK激活剂，通过激活AMPK通路有效抑制3T3-L1细胞的有丝分裂克隆扩增，并增加细胞线粒体耗氧量，适用于肥胖研究。
T36821	FQI 1
	FQI 1 是一种 SV40 因子 (LSF) 抑制剂。FQI 1 抑制细胞增殖，对 NIH/3T3、HeLa、A549 细胞的 IC50s 分别为 3、0.79、6.3 μM。FQI1 可用于癌症研究。
T36542	Prostaglandin A2 Medullin
	PGA2 is a naturally occurring prostaglandin in gorgonian corals where it may function in self defense. It is generally not present in mammals. PGA2 has low biological potency in most bioassays, but it does show some antiviral/antitumor activity.[1] At a 25 uM concentration, PGA2 blocks the cell cycle progression of NIH 3T3 cells at the G1 and G2/M phase .[2] It has also been shown to act as a vasodilator with natriuretic properties.[3]
T36330	Terrecyclic Acid
	Terrecyclic acid is a sesquiterpene originally isolated from A. terreus with antibiotic and anticancer activity. It is active against S. aureus, B. subtilis, and M. roseus (MICs = 25, 50, and 25 μg/ml, respectively). Terrecyclic acid induces a heat shock response, increases levels of reactive oxygen species (ROS), and inhibits NF-κB activity and cell growth in 3T3-Y9-B12 cells. In vivo, terrecyclic acid (0.1, 1, and 10 mg/ml) reduces the number of ascitic fluid tumor cells in a mouse model of P3...
T62052	AMPK activator 6
	AMPK activator 6 (Compound GC) 可降低 HepG2 和 3T3-L1 细胞中的脂质含量并激活AMPK 通路。AMPK activator 6 对血清中甘油三酯 (TG)、总胆固醇 (TC)、低密度脂蛋白-C (LDL-C) 和其他生化指标的增加有显著的抑制作用。AMPK activator 6 在非酒精性脂肪肝（NAFLD）和代谢综合征中有研究价值。
T67442	CGP-53716
	The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase inhibition has been shown to be effective in blocking tyrosine phosphorylation at the PDGF and bFGF receptors in cultured fibroblast and vascular smooth muscle cells which in turn inhibits their proliferation[1]. CGP 53716 is a specific PDGFR tyrosine kinase inhibitor on SMC (smoo...
T35800	MD001
	MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It...
T35854	9(Z),11(E)-Conjugated Linoleic Acid (sodium salt)
	9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-co...
T37579	GW 1929 hydrochloride
	Highly selective orally active peroxisome proliferator-activated receptor (PPAR)γ agonist (pEC50 values are 8.05, < 4 and < 4 for human PPARγ, PPARα and PPARδ receptors respectively). Decreases glucose, fatty acid and triglyceride levels following oral administration in vivo. Brown et al (1999) A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-γ reverses the diabetic phenotype of the Zucker diabetic fatty rat. Diabetes 48 1415 PMID:10389847 \|Nugent et al (2001) Pote...

化合物

Cat.No: T7196

Synonym: [4-[[5-氯-4-(甲基氨基)-2-嘧啶基]氨基]-3-甲氧基苯基]-4-吗啉基甲酮

Target: LRRK2

Cat.No: T21312

Synonym: 阿法替尼,Afatinib free base,BIBW 2992

Target: EGFR, Autophagy

Afatinib Dimaleate

Cat.No: T1773

Synonym: 马来酸阿法替尼,双马来酸盐阿法替尼,BIBW2992,Afatinib,BIBW 2992MA2,Afatinib (BIBW2992) Dimaleate

Target: EGFR, HER, Autophagy

Cat.No: T11212

Synonym: 5-{[5-(2,4-dichlorophenyl)furan-2-yl]methylidene}-2-thioxodihydropyrimidine-4,6(1H,5H)-dione

Target: cAMP

Cat.No: T9650

Target: Src, Ephrin Receptor

Cat.No: T28740

Synonym: SDZ 62 434,SDZ62434

Target: Platelet aggregation

Cat.No: T9491

Target: Antibacterial, Antifungal

Cat.No: T60857

Target: Others

Cat.No: T10849

Target: Others

Cat.No: T10848

Target: Others

AMPK activator 13

Cat.No: T83127

Target: AMPK

Cat.No: T36821

Prostaglandin A2

Cat.No: T36542

Synonym: Medullin

Terrecyclic Acid

Cat.No: T36330

AMPK activator 6

Cat.No: T62052

Cat.No: T67442

Cat.No: T35800

9(Z),11(E)-Conjugated Linoleic Acid (sodium salt)

Cat.No: T35854

GW 1929 hydrochloride

Cat.No: T37579

Cat. No.	Product Name	Target	Signaling Pathways
T3220	Euphorbiasteroid Euphobiasteroid,Euphorbia factor L1,千金子甾醇	Others; AMPK	Chromatin/Epigenetic; Others; PI3K/Akt/mTOR signaling
	Euphorbiasteroid (Euphobiasteroid) 是续随子中的一种三环二萜，可抑制酪氨酸酶活性，增强AMPK 的磷酸化。它通过减少细胞内甘油三酯的积累来降低 3T3-L1 细胞的分化，具有抗癌、抗病毒、抗肥胖及多重耐药调节作用。
TN1206	2,4,6-Trihydroxybenzaldehyde	Others	Others
	2,4,6-Trihydroxybenzaldehyde 是一种天然产物。 2,4,6-三羟基苯甲醛是一种潜在的抗肥胖治疗药物，可抑制 C57BL/6 小鼠的 3T3-L1 细胞中的脂肪细胞分化和高脂饮食诱导的脂肪积累。它也是一种有效的抗糖尿病药物。 2,4,6-三羟基苯甲醛具有潜在的抗癌活性。
T81291	Retrofractamide A
	Retrofratamide A为源自Piper chaba果实的酰胺，能够促进3T3-L1细胞的脂肪生成。
TN5090	Tachioside	Glucokinase	Metabolism
	Tachioside has antiobesity, antioxidant and α-glucosidase inhibitory activities, it decreases lipid content in 3T3-L1 adipocytes by inhibiting lipogenesis, shows antiobesity activities. Tachioside can inhibit nitric oxide production in lipopolysaccharides-stimulated RAW 264.7 cells with IC50 value of 12.14 μM.
TN3112	5-Heneicosylresorcinol	NADPH-oxidase; Antifection	Immunology/Inflammation; Microbiology/Virology
	5-Heneicosylresorcinol 对 RBL-2H3 细胞中 β-己糖胺酶的释放具有抑制作用，它还可以防止 3T3-L1 细胞中甘油三酯的积累。它对红线虫、秀丽隐杆线虫和松材线虫具有杀线虫活性，ED50 值分别为 80、30 和 180 ug/mL。
TN5682	2,6,4'-Trihydroxy-4-methoxybenzophenone
	2,6,4'-Trihydroxy-4-methoxybenzophenone shows weak inhibitory activity of testosterone 5alpha-reductase, it also shows significant inhibition of pancreatic lipase activity. 2,6,4'-Trihydroxy-4-methoxybenzophenone has neurotrophic activity, it induced neurite outgrowth in PC-12 cells at concentration of 50 microg/ml. 2,6,4â²-Trihydroxy-4-methoxybenzophenone exhibits low cytotoxic effect against HeLa and 3T3 cell lines with IC50 values of 132 ug/ml and 158 ug/ml, repectively. It also shows antiox...
TN5655	Broussonin B
	Broussonins A and B, new phytoalexins from diseased paper mulberry. Broussonin B can induce neurite outgrowth in PC-12 cells at concentration of 50 microg/ml, and show moderate inhibitory activities against a chymotrypsin-like activity of the proteasome.B
TN3539	Broussonin A	ERK; IL Receptor; IκB/IKK; NOS; NF-κB; Akt	Cytoskeletal Signaling; Immunology/Inflammation; MAPK; NF-κB; PI3K/Akt/mTOR signaling
	Broussonins A and B, new phytoalexins from diseased paper mulberry. Broussonin A shows estrogenic activity with ligand-binding activity of estrogen receptor, transcriptional activity of estrogen-responsive element-luciferase reporter genes. Broussonin A c

天然产物

Euphorbiasteroid

Cat.No: T3220

Synonym: Euphobiasteroid,Euphorbia factor L1,千金子甾醇

Target: Others, AMPK

2,4,6-Trihydroxybenzaldehyde

Cat.No: TN1206

Target: Others

Retrofractamide A

Cat.No: T81291

Cat.No: TN5090

Target: Glucokinase

5-Heneicosylresorcinol

Cat.No: TN3112

Target: NADPH-oxidase, Antifection

2,6,4'-Trihydroxy-4-methoxybenzophenone

Cat.No: TN5682

Cat.No: TN5655

Cat.No: TN3539

Target: ERK, IL Receptor, IκB/IKK, NOS, NF-κB, Akt

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