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23

抑制剂 & 化合物

21

天然产物

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Cat. No. Product Name Target Signaling Pathways
T2676 PF-04217903

c-Met/HGFR Tyrosine Kinase/Adaptors
PF04217903 是一种高效的、 ATP 竞争性的c-Met 激酶抑制剂(Ki=4.8 nM),相对于 208 个激酶,PF04217903 显示出 1000 倍以上的选择性。它抗血管生成作用。
T28410 PHPS1

PHPS-1,PHPS 1

Phosphatase Metabolism
PHPS1 是 Shp2的选择性抑制剂,对 Shp2,Shp2-R362K,Shp1,PTP1B 和 PTP1B-Q 的 Ki 分别为 0.73,5.8,10.7,5.8 和 0.47 μM。
T6609 NMS-E973

HSP Cytoskeletal Signaling; Metabolism
NMS-E973 是一种有效且选择性的 Hsp90 抑制剂,与 Hsp90 结合的 DC50小于 10 nM。它能够穿越血脑屏障,具有抗肿瘤效果。
T19147 5-ALA benzyl ester hydrochloride

Benzyl-ALA hydrochloride

Others; Endogenous Metabolite Metabolism; Others
5-ALA benzyl ester hydrochloride (Benzyl-ALA hydrochloride) 是一种原卟啉前体,可用作光检测器。5-ALA benzyl ester hydrochloride 在结肠癌细胞系中可以诱导原卟啉 IX (PPIX) 的积聚。
T2455 PFK-015

PFK15,PFK 015

Glucokinase; Autophagy Autophagy; Metabolism
PFK-015 (PFK15) 是一种有效的 PFKFB3 抑制剂,对重组PFKFB3的IC50为110 nM。它能抑制 Y 细胞中的 PFKFB3 活性,IC50为20 nM。
TQ0157 EIPA

L593754,MH 12-43

Sodium Channel; TRP/TRPV Channel Membrane transporter/Ion channel
EIPA (L593754) 是一种有效的TRPP3 channel 抑制剂,IC50为 10.5 μM。EIPA 对Na+/H+交换 (NHE) 和巨噬细胞也有抑制作用。
T1520 Aliskiren hemifumarate

阿利克仑半富马酸盐,CGP 60536,SPP 100,CGP60536B

RAAS; Autophagy Autophagy; Endocrinology/Hormones
Aliskiren hemifumarate (CGP60536B) 一种可口服非肽肾素抑制剂,IC50为1.5 nM,具有抗高血压活性。
T5618 AK-1

Sirtuin Chromatin/Epigenetic; DNA Damage/DNA Repair
AK-1是一种特异性有效和细胞可渗透的SIRT2抑制剂,其IC50值为 12.5 μM。它可防止阿尔茨海默病模型中的海马神经退行性变并诱导结肠癌细胞中的细胞周期停滞。
T77651 Tubulin polymerization-IN-47

Microtubule Associated Cytoskeletal Signaling
Tubulin polymerization-IN-47 是一种 tubulin 聚合抑制剂和有丝分裂抑制剂,具有抗肿瘤活性,对神经母细胞瘤癌细胞增殖具有抑制作用,对 Chp-134 和 Kelly 细胞系的IC50 分别为 7 和 12 nM。Tubulin polymerization-IN-47 是治疗肝癌、结肠癌、肺癌和乳腺癌的候选化合物。
T71912 PD 173955-Analog1

PD 173955-Analog1 is a potent c-Src inhibitor known to have activity against a variety of cancers including colon, lung, head and neck carcinoma.
T20050 Cinnamamide

NSC 32953

Cinnamamide is an amide of trans-cinnamic acid and a metabolite of Streptomyces. It also reduced tumor weight in a mouse model of C26 murine colon carcinoma, in vivo.
T16034 Meclinertant

SR 48692

Others Others
Meclinertant is an effective, selective, nonpeptide, and orally active neurotensin receptor 1 (NTS1) antagonist. Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization (pA2 : 8.13), in human colon carcinoma (HT-29) cell
T72740 n-Octyl caffeate

n-Octyl caffeate 具有抗癌、诱导凋亡活性。
T71890 F5446

F5446 is a SUV39H1 inhibitor. F5446 has an EC50 of 0.496 μmol/L for SUV39H1 enzymatic activity. H3K9me3 was enriched in the promoters of GZMB, PRF1, FASLG, and IFNG in quiescent T cells. F5446 inhibited H3K9me3, thereby upregulating expression of these effectors in tumor-infiltrating CTLs and suppressing colon carcinoma growth in a CD8+ CTL-dependent manner in vivo. Our data indicate that SUV39H1 represses CTL effector gene expression and, in doing so, confers colon cancer immune escape.
T60727 B-Raf IN 8

B-Raf IN 8 (compound 7g) 是 B-Raf 的有效抑制剂 (IC50 = 70.65 nM)。B-Raf IN 8 显示出抗肿瘤活性,其对肝细胞癌 (HEPG-2)、结肠癌 (HCT-116),乳腺癌 (MCF-7) 和人前列腺癌 (PC-3) 细胞的 IC50值分别为9.78、13.78、18.52 和 29.85 μM。
T72927 IMD-catechol

NF-κB NF-κB
IMD-catechol为一种创新的NF-κB免疫调节剂二聚体,能够增强CT26小鼠结肠癌模型的疗效,同时降低辅助毒性至最低。
T60933 B-Raf IN 7

B-Raf IN 7 (compound 6a) 是 B-Raf 的有效抑制剂,IC50值为 110.23 nM。B-Raf IN 7 对结肠癌细胞(HCT-116)、乳腺癌细胞 (MCF-7)、肝癌细胞 (HEPG-2)、人宫颈癌细胞 (Hela) 和人前列腺癌细胞 (PC-3) 具有抗肿瘤活性。其 IC50值分别为 7.50、9.87、10.57、11.63 和 12.83 μM。
T69618 XR3054

XR3054 is a novel inhibitor of farnesyl protein transferase (FPTase). XR3054 inhibited the proliferation of the prostatic cancer cell lines LnCAP and PC3 and the colon carcinoma SW480 and HT1080 (IC50 values of 12.4, 12.2, 21.4 and 8.8 microM, respectively) but was relatively inactive when tested against a panel of breast carcinoma cell lines. The activity did not relate to the presence of mutant or wild-type ras in the cell lines tested. In conclusion XR3054 inhibits ras farnesylation, MAP kina...
T36426 Eicosapentaenoyl 1-propanol-2-amide

Monoacylglycerols (MAGs) of ω-3 polyunsaturated fatty acids have diverse physiological and health effects. In particular, MAGs containing docosahexaenoic acid or eicosapentaenoic acid have anti-proliferative properties against colon and lung cancer cell lines. Eicosapentaenoyl 1-propanol-2-amide is an EPA-containing MAG amide analog that inhibits the growth of human lung carcinoma A549 cells, producing 98.4% growth inhibition when applied at 3 μM. It is an analog of eicosapentaenoyl ethanolamide...
T36452 1-Arachidonoyl Lysophosphatidic Acid (ammonium salt)

1-Arachidonoyl lysophosphatidic acid is a phospholipid containing arachidonic acid at the sn-1 position. It has been found in rat brain as 37% of the arachidonic acid-containing lysophosphatidic acid (LPA) species and is a precursor to 1-arachidonoyl glycerol . 1-Arachidonoyl lysophosphatidic acid binds to the LPA2/EDG4 receptor with an EC50 value of approximately 10 nM. It prevents TNF-α and IL-6 secretion in wild-type but not Lpa2-/- dendritic cells stimulated by LPS. It also decreases differe...
T36627 Lysine-specific Demethylase Inhibitor (1C) (hydrochloride)

Lysine-specific demethylase inhibitor (1C) (LSD inhibitor (1C)) is an inhibitor of LSD1, a repressive demethylase selective for histone H3 lysine 4 (H3K4).1,2LSD inhibitor (1C) inhibits LSD1 activity by 85.9% when used at a concentration of 10 μM.1It increases the level of H3K4 methylation, including H3K4me1 and H3K4me2 but not H3K9me2 levels, in HCT116 human colon carcinoma cells.2LSD inhibitor (1C) also induces re-expression of the Wnt signaling pathway proteins secreted frizzle-related protei...
T36846 Chromomycin A2

Chromomycin A2 is an aureolic acid that has been found in several marine actinomycetes and has antibacterial and anticancer activities. Chromomycin A2 inhibits the growth of B. subtilis in an agar diffusion assay. It also inhibits the growth of human SGC7901 gastric cancer, HepG2 hepatocellular carcinoma, A549 lung epithelial adenocarcinoma, HCT116 colon cancer, and COC1 ovarian cancer cells, as well as human umbilical vein endothelial cells (HUVECs; IC50s = 4, 0.5, 3, 5, 5, and 8 nM, respective...
T71293 Nifuroxazide-d4

Nifuroxazide-d4 is intended for use as an internal standard for the quantification of nifuroxazide by GC- or LC-MS. Nifuroxazide is a nitrofuran antibiotic. It is active against strains of the enteropathogenic bacteria C. jejuni, Salmonella, Y. enterocolitica, Shigella, and E. coli. It inhibits quorum sensing and virulence factor production in P. aeruginosa. Nifuroxazide inhibits STAT3 activity in a reporter assay and decreases viability of U266 and INA-6 myeloma cells, which have constitutive S...

化合物

PF-04217903
Cat.No: T2676
Synonym:
Target: c-Met/HGFR
PHPS1
Cat.No: T28410
Synonym: PHPS-1,PHPS 1
Target: Phosphatase
NMS-E973
Cat.No: T6609
Synonym:
Target: HSP
5-ALA benzyl ester hydrochloride
Cat.No: T19147
Synonym: Benzyl-ALA hydrochloride
Target: Others, Endogenous Metabolite
PFK-015
Cat.No: T2455
Synonym: PFK15,PFK 015
Target: Glucokinase, Autophagy
EIPA
Cat.No: TQ0157
Synonym: L593754,MH 12-43
Target: Sodium Channel, TRP/TRPV Channel
Aliskiren hemifumarate
Cat.No: T1520
Synonym: 阿利克仑半富马酸盐,CGP 60536,SPP 100,CGP60536B
Target: RAAS, Autophagy
AK-1
Cat.No: T5618
Synonym:
Target: Sirtuin
Tubulin polymerization-IN-47
Cat.No: T77651
Synonym:
Target: Microtubule Associated
PD 173955-Analog1
Cat.No: T71912
Synonym:
Target:
Cinnamamide
Cat.No: T20050
Synonym: NSC 32953
Target:
Meclinertant
Cat.No: T16034
Synonym: SR 48692
Target: Others
n-Octyl caffeate
Cat.No: T72740
Synonym:
Target:
F5446
Cat.No: T71890
Synonym:
Target:
B-Raf IN 8
Cat.No: T60727
Synonym:
Target:
IMD-catechol
Cat.No: T72927
Synonym:
Target: NF-κB
B-Raf IN 7
Cat.No: T60933
Synonym:
Target:
XR3054
Cat.No: T69618
Synonym:
Target:
Eicosapentaenoyl 1-propanol-2-amide
Cat.No: T36426
Synonym:
Target:
1-Arachidonoyl Lysophosphatidic Acid (ammonium salt)
Cat.No: T36452
Synonym:
Target:
Lysine-specific Demethylase Inhibitor (1C) (hydrochloride)
Cat.No: T36627
Synonym:
Target:
Chromomycin A2
Cat.No: T36846
Synonym:
Target:
Nifuroxazide-d4
Cat.No: T71293
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5S1133 Ganoderic acid D

灵芝酸D,灵芝酸 D

Apoptosis; Sirtuin Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair
Ganoderic acid D 是高度氧化的四环三萜,是灵芝的主要活性成分,可诱导 HeLa 人宫颈癌细胞凋亡。它上调 SIRT3的蛋白质表达并通过 SIRT3 诱导脱乙酰化的亲环蛋白 D 。它抑制结肠癌细胞的能量重编程,包括结肠癌细胞中的葡萄糖摄取,乳酸、丙酮酸和乙酰辅酶的产生。
T1709 2'-Deoxyinosine

Guanine deoxyriboside,Deoxyinosine,2'-脱氧肌苷

Others; Endogenous Metabolite Metabolism; Others
2'-Deoxyinosine (Guanine deoxyriboside) 具有 抑制人癌细胞株生长的活性,并发现其与嘌呤核苷磷酸化酶缺乏有关。
T5746 Dictamine

Dictamnine,Dectamine,白鲜碱

Apoptosis; Anti-infection; Antibacterial; Antifungal Apoptosis; Microbiology/Virology
Dictamine (Dectamine) 显示抗胆碱酯酶、抗炎、致突变、抗菌和抗真菌活性。 它具有在人子宫颈、结肠和口腔癌细胞中发挥细胞毒性的能力。
TN1405 Arnicolide D

山金车内酯 D,山金车内酯D

Akt; Caspase; PI3K; STAT; mTOR Apoptosis; Cytoskeletal Signaling; JAK/STAT signaling; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
Arnicolide D 是从石胡荽中分离出的一种倍半萜内酯,以浓度和时间依赖性方式抑制鼻咽癌细胞活力。它调节细胞周期,激活 caspase 信号通路并抑制 PI3K/AKT/mTOR 和 STAT3 信号通路。
T5S0506 Rotundic acid

Rutundic acid,铁冬青酸

Apoptosis; Others; p38 MAPK; Akt; mTOR Apoptosis; Cytoskeletal Signaling; MAPK; Others; PI3K/Akt/mTOR signaling
Rotundic acid (Rutundic acid) 是一种从圆形肠球菌中获得的三萜类天然产物,具有抗炎和保护心脏的能力。它可通过 AKT/mTOR 和 MAPK 途径在肝细胞癌中诱导 DNA 损伤和细胞凋亡。
T1660 Silibinin

水飞蓟宾 A,水飞蓟宾,Silibinin A,Silybin,Silymarin I

Reactive Oxygen Species; Autophagy Autophagy; Immunology/Inflammation; Metabolism; NF-κB
Silibinin (Silybin) 是水飞蓟的主要活性成分,具有抗癌和化疗预防作用,能抑制细胞增殖和迁移。
TN2029 p-Hydroxy-5,6-dehydrokawain

4'-Hydroxydehydrokawain,4'-羟基-5,6-脱氢醉椒素

Others Others
p-Hydroxy-5,6-dehydrokawain (4'-Hydroxydehydrokawain) 是一种分离自 Kawain 的天然产物。
T40708 Neoanhydropodophyllol

Neoanhydropodophyllol, a cyclolignan derivative, exhibits potent antineoplastic activity by exerting cytotoxic effects on various cancer cell lines including leukemia, lung carcinoma, and colon carcinoma.
TN5093 Taiwanhomoflavone A

COX Immunology/Inflammation; Neuroscience
Taiwanhomoflavone A is cytotoxic with ED50 values of 3.4, 1.0, 2.0 and 2.5 microg/ml, respectively, against KB epidermoid carcinoma of nasopharynx, COLO-205 colon carcinoma, Hepa-3B hepatoma, and Hela cervix tumor cells.
TN3495 Benzyl ferulate

TNF; Antifection Apoptosis; Microbiology/Virology
Benzyl ferulate has antimicrobial activity. It also shows good anti-proliferative against three gastro-intestinal cancer cell lines(HCT-116 colon carcinoma, KYSE-30 oesophageal squamous cancer, and NCI-N87 gastric carcinoma).
TN2813 23-deoxojessic acid

Others Others
23-Deoxojessic acid possesses strong cytotoxicity towards highly liver metastatic murine colon 26-L5 carcinoma cells, with ED50 values equal to or less than 6 microM.
TN1645 Flavokawain C

NADPH-oxidase; MAPK; AChR Immunology/Inflammation; MAPK; Neuroscience
Flavokawain C is a melanogenesis inhibitor, it inhibited melanogenesis with IC50 values of 6.9 μM. Flavokawain C has anti-tumor activity, it inhibited cell cycle and promoted apoptosis, associated with endoplasmic reticulum stress and regulation of MAPKs and Akt signaling pathways in HCT 116 human colon carcinoma cells.
T73064 Rostratin C

Rostratin C,一种具有细胞毒性的二硫化物,在体外对人结肠癌(HCT-116)展现出细胞毒性,IC50值为0.76 μg/mL。
T73063 Rostratin B

Rostratin B为一种具体外细胞毒作用的二硫化物,针对人结肠癌HCT-116细胞线,展现了IC50值达1.9 μg/mL。
TN3660 Cinnamyl caffeate

Calcium Channel Membrane transporter/Ion channel; Metabolism
Cinnamyl caffeate has cardiovascular protective effects, it can increase H9c2 cellular antioxidant potential, decrease intracellular calcium ion ([Ca2+]i) level, and prevent cell apoptosis; it possesses potent antiproliferative activity with the EC(50) value of 0.114 microM, toward colon 26-L5 carcinoma. Cinnamyl caffeate possesses potent NO inhibitory activity with the IC(50) value of 9.53 microM.
TN4623 Nagilactone C

Antifection Microbiology/Virology
Nagilactone C and phyllanthoside are novel protein synthesis inhibitors, they are specific for the eukaryotic translation apparatus, function in vivo and in vitro, and interfere with translation elongation. Nagilactone C shows high insecticidal activity against second-instar nymphs of Eocanthecona furcellata. Nagilactone C possesses potent antiproliferative activity against human fibrosarcoma and murine colon carcinoma tumor cell lines exhibiting ED50 values of 2.3 and 1.2 microg/ml, respectivel...
T73062 Rostratin A

Rostratin A 是一种细胞毒性二硫化物,存在于海洋源性真菌Exserohilum rostratum 中。Rostratin A 对人结肠癌 (HCT-116) 具有体外细胞毒性,IC50值为 8.5μg/mL。
TMA1008 Ganoderic acid S

Others Others
A novel combination of triterpenoids includes at least ganoderic acid S (GAS), ganoderic acid T (GAT), ganoderic acid Me (GAMe), ganoderic acid R (GAR), and ganodermic acid S (GMAS), the composition is suitable for the treatment or prophylaxis of colon ca
TN3152 6-Acetonyldihydrochelerythrine

ERK; BCL; Akt; HIV Protease; PPAR; p53 Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair; MAPK; Metabolism; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
6-Acetonyldihydrochelerythrine exhibits significant antioxidant activities, it exhibits significant anti-HIV activity in H9 lymphocytes with EC50 and TI (Therapeutic Index) values of 1.77 microg/mL and 14.6, respectively. 6-Acetonyldihydrochelerythrine is
TN3404 Altholactone

BCL; p38 MAPK; ROS; Akt; Caspase; Antifection; p53 Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; MAPK; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
Altholactone may be a potential antimicrobial agent, particularly in ciprofloxacin-refractory S. aureus and E. faecalis infections. It can inhibit the growth of various types of cancer cells through inducing apoptosis via oxidative stress, including bladd
TN3870 Iriflophenone 2-O-Rhamnoside

Dimethylmatairesinol

Others Others
Dimethylmatairesinol can reduce the amount of Immunoglobulin E (IgE) secreted by human myeloma U266 cells, it has potential as an anti-allergic agent. Dimethylmatairesinol also exhibits significant cytotoxicity against three human tumor cells(A-549 lung c

天然产物

Ganoderic acid D
Cat.No: T5S1133
Synonym: 灵芝酸D,灵芝酸 D
Target: Apoptosis, Sirtuin
2'-Deoxyinosine
Cat.No: T1709
Synonym: Guanine deoxyriboside,Deoxyinosine,2'-脱氧肌苷
Target: Others, Endogenous Metabolite
Dictamine
Cat.No: T5746
Synonym: Dictamnine,Dectamine,白鲜碱
Target: Apoptosis, Anti-infection, Antibacterial, Antifungal
Arnicolide D
Cat.No: TN1405
Synonym: 山金车内酯 D,山金车内酯D
Target: Akt, Caspase, PI3K, STAT, mTOR
Rotundic acid
Cat.No: T5S0506
Synonym: Rutundic acid,铁冬青酸
Target: Apoptosis, Others, p38 MAPK, Akt, mTOR
Silibinin
Cat.No: T1660
Synonym: 水飞蓟宾 A,水飞蓟宾,Silibinin A,Silybin,Silymarin I
Target: Reactive Oxygen Species, Autophagy
p-Hydroxy-5,6-dehydrokawain
Cat.No: TN2029
Synonym: 4'-Hydroxydehydrokawain,4'-羟基-5,6-脱氢醉椒素
Target: Others
Neoanhydropodophyllol
Cat.No: T40708
Synonym:
Target:
Taiwanhomoflavone A
Cat.No: TN5093
Synonym:
Target: COX
Benzyl ferulate
Cat.No: TN3495
Synonym:
Target: TNF, Antifection
23-deoxojessic acid
Cat.No: TN2813
Synonym:
Target: Others
Flavokawain C
Cat.No: TN1645
Synonym:
Target: NADPH-oxidase, MAPK, AChR
Rostratin C
Cat.No: T73064
Synonym:
Target:
Rostratin B
Cat.No: T73063
Synonym:
Target:
Cinnamyl caffeate
Cat.No: TN3660
Synonym:
Target: Calcium Channel
Nagilactone C
Cat.No: TN4623
Synonym:
Target: Antifection
Rostratin A
Cat.No: T73062
Synonym:
Target:
Ganoderic acid S
Cat.No: TMA1008
Synonym:
Target: Others
6-Acetonyldihydrochelerythrine
Cat.No: TN3152
Synonym:
Target: ERK, BCL, Akt, HIV Protease, PPAR, p53
Altholactone
Cat.No: TN3404
Synonym:
Target: BCL, p38 MAPK, ROS, Akt, Caspase, Antifection, p53
Iriflophenone 2-O-Rhamnoside
Cat.No: TN3870
Synonym: Dimethylmatairesinol
Target: Others
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