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抑制剂&激动剂
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  • 抑制剂&激动剂
    54
    TargetMol | Inhibitors_Agonists
  • 重组蛋白
    1
    TargetMol | Recombinant_Protein
  • 抗体抑制剂
    1
    TargetMol | Inhibitory_Antibodies
  • PROTAC
    1
    TargetMol | PROTAC
  • 天然产物
    13
    TargetMol | Natural_Products
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    TargetMol | Isotope_Products
  • Araliadiol
    T135511354638-93-9
    Araliadiol is a polyacetylenic compound isolated from the leaves of Aralia cordata Thunb. Araliadiol inhibits MCF-7 cell growth (IC50: 6.41 µg mL).
    • ¥ 10600
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  • ANI-7
    T10325931417-26-4In house
    ANI-7是芳香烃受体(AhR)途径的激活剂。ANI-7抑制多种癌症细胞的生长,并有效且选择性地抑制MCF-7乳腺癌症细胞的生长(GI50:0.56μM)。
    • ¥ 147
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  • (Iso)-MS4322
    YS43-22 (isomer), MS4322 (isomer), (Iso)-YS43-22
    T402332601727-80-2In house
    (Iso)-MS4322 ((Iso)-YS43-22) 是一种具有选择性和强效性的蛋白质精氨酸甲基转移酶 5 (PRMT5) 降解剂,具有潜在的抗癌活性,有效地降低 MCF-7 细胞中的 PRMT5 蛋白水平,可抑制多种癌细胞的生长。
    • ¥ 3530 TargetMol
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  • Octyl gallate
    Gallic acid octyl ester, n-Octylgallate, Octyl 3,4,5-trihydroxybenzoate, 没食子酸辛酯, Progallin O, Stabilizer GA-8
    T2S18651034-01-1
    Octyl gallate (Octyl 3,4,5-trihydroxybenzoate) 具有抗菌、抗氧化作用,有选择性和敏感性的荧光特性,广泛用作食品添加剂。它对 HSV-1,水泡性口炎病毒和脊髓灰质炎病毒有显著的抗病毒作用。
    • ¥ 145
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  • Trabectedin
    曲贝替定, ET-743, Ecteinascidin 743
    T17155114899-77-3
    Trabectedin (Ecteinascidin 743) 是一种四氢异喹啉生物碱,有抗肿瘤的活性, 通过与 DNA 的小沟结合,阻断应激诱导的蛋白质的转录,诱导 DNA 骨架裂解和癌细胞凋亡,并增加 MCF-7 和 MDA-MB-453 细胞中 ROS 的生成。Trabectedin 在软组织肉瘤和卵巢癌中具有的研究价值。
    • ¥ 14725
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  • iNOS/TopoI-IN-1
    T200135
    iNOS TopoI-IN-1(compound AuL9)是一种具备多重靶点的杂交分子,表现出抗肿瘤、抗炎及抗氧化的特性。此化合物能有效抑制乳腺癌细胞株MCF-7和MDA MB-231的增长,IC50分别为3.5 μM及6.3 μM,其机制主要是通过抑制人类拓扑异构酶I(TopoI)(Ki=2.72 μM)的活动,导致DNA损伤并诱发细胞凋亡(apoptosis)。同时,iNOS TopoI-IN-1通过降低NF-kB的激活,抑制iNOS表达(Ki=1.49 μM),进一步增强其抗炎作用。
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  • VEGFR-2-IN-53
    T200472
    VEGFR-2-IN-53(Compound 15w)为一种 VEGFR-2 抑制剂,具备 4.34 μM 的 IC50 值。该化合物通过阻断 VEGFR-2 的活性及细胞迁移,进而诱导细胞凋亡(Apoptosis)并表现出抗血管生成特性。其对 MCF-7 细胞的生长抑制 IC50 值为 3.87 μM,适用于抗癌研究。
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  • Apoptosis inducer 30
    T201277
    Apoptosisinducer 30 (Compound 15a) 作为一种强效的抗癌化合物,特别通过线粒体途径促进MCF-7细胞的凋亡。它通过增加细胞内活性氧的水平和降低线粒体膜电位来实现其作用,并且使细胞周期在G0 G1期停滞。此外,Apoptosisinducer 30显著抑制细胞生长,其对MCF-7细胞的IC50为0.32 μM,并有效抑制小鼠乳腺癌模型中的肿瘤发展。
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  • DSPE-PEG(2000)-Biotin
    DSPE-PEG2000-Biotin, 1,2-DSPE-PEG(2000)-Biotin, 1,2-Distearoyl-sn-glycero-3-Phosphoethanolamine-Polyethylene Glycol-2000-Biotin, 1,2-Distearoyl-sn-glycero-3-PE-Polyethylene Glycol-2000-Biotin
    T201893740794-01-8
    DSPE-PEG(2000)-biotin 是一种对1,2-二硬脂酰-sn-甘油-3-PE进行PEG化和生物素化处理的化合物。它被广泛应用于体外和体内的脂质体输送、荧光标记纳米结构脂质载体(NLCs)的开发。此外,DSPE-PEG(2000)-biotin 也用于生成胶束,用作固定脂质体的前体,并被应用于生物层干涉测量结合实验中。当含有DSPE-PEG(2000)-biotin的脂质体内封装有多柔比星和槲皮素时,能对体外的MCF-7 adr多药耐药乳腺癌细胞产生细胞毒作用,并有效抑制MCF-7 adr小鼠移植瘤模型中的肿瘤增长。通过使用生物素偶联的FITC标记的avidin,已成功在NLCs中实现荧光标记。
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  • (E/Z)-Droloxifene
    (E Z)-3-Hydroxytamoxifen
    T203143165813-01-4
    (E Z)-Droloxifene 是 (E)-Droloxifene 和 (Z)-Droloxifene 的混合物,其中 (E)-Droloxifene 是一种选择性雌激素受体调节剂。在兔子子宫匀浆实验中,(E)-Droloxifene 结合雌激素受体 (ER) 的 IC50 值为 24 nM。它能够增加未成熟大鼠的子宫重量,并减少雌二醇诱导的幼年大鼠子宫重量增加。此外,(E)-Droloxifene 抑制 17β-雌二醇刺激的 MCF-7、ZR-75-1 和 T47D 人乳腺癌细胞的生长。(Z)-Droloxifene 则由于与 ER 结合较弱,无雌激素或抗雌激素活性。
    • 待询
    10-14周
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  • Tesmilifene hydrochloride
    T20412792981-78-7
    Tesmilifene hydrochloride 是一种兼具抗组胺和化学增敏作用的化合物。该化合物通过靶向细胞色素P450 (cytochrome P450),在MCF-7细胞中引发DNA合成的激素效应,并促进小鼠和大鼠模型中的肿瘤生长。此外,Tesmilifene hydrochloride 能够克服多药耐药性。
    • 待询
    10-14周
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  • CA IX/VEGFR-2-IN-3
    T204735
    CAIX VEGFR-2-IN-3 (Compound 6i) 是一种针对 Carbonic Anhydrase IX 和 VEGFR-2 的抑制剂,其 IC50 值分别为 41 和 48 nM。该化合物表现出抗癌活性,并能抑制 MCF-7 乳腺癌细胞(IC50 为 22.33 μM)及小鼠成纤维细胞系 3T3(在 100 μM 浓度下细胞存活率低于 40%)的生长。CAIX VEGFR-2-IN-3 可用于抗癌研究。
    • 待询
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  • Nur77 modulator 4
    T205370
    Nur77 modulator 4 (Compound 15h) 是一种Nur77诱导剂,其KD值为0.477 μM。该化合物显著增强Nur77的表达,并诱导细胞凋亡 (Apoptosis),在HepG2和MCF-7细胞中表现出明显的生长抑制效果,IC50均低于5 μM。Nur77 modulator 4 通过激活PERK-ATF4和IRE1信号通路来促进Nur77介导的ER应激,从而引发细胞凋亡。Nur77 modulator 4 可应用于癌症研究领域。
    • 待询
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  • EC 144
    EC144
    T22758911397-80-3
    EC 144是一种选择性的Hsp90(热休克蛋白90)的第二代抑制剂,对Hsp90α的IC50= 1.1 nM,MCF-7细胞中降解Her-2的EC50 =14 nM,能够抑制肿瘤生长。
    • ¥ 3560
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  • β-Rubromycin
    T3542827267-70-5
    β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycin inhibits HIV-1 reverse transcriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group, but it was revised to a para-quinone group in 2000 using organic and biosynthetic methods, as well as spectroscopic analysis.1,2,3References1. Ueno, T., Takahashi, H., Oda, M., et al. Inhibition of human telomerase by rubromycins: Implication of spiroketal system of the compounds as an active moiety. Biochemistry 39(20), 5995-6002 (2000).2. Puder, C., Loya, S., Hizi, A., et al. Structural and biosynthetic investigations of the rubromycins. Eur. J. Org. Chem. 2000(5), 729-735 (2000).3. Goldman, M.E., Salituro, G.S., Bowen, J.A., et al. Inhibition of human immunodeficiency virus-1 reverse transcriptase activity by rubromycins: Competitive interaction at the template.primer site. Mol. Pharmacol. 38(1), 20-25 (1990). β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycin inhibits HIV-1 reverse transcriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group, but it was revised to a para-quinone group in 2000 using organic and biosynthetic methods, as well as spectroscopic analysis.1,2,3 References1. Ueno, T., Takahashi, H., Oda, M., et al. Inhibition of human telomerase by rubromycins: Implication of spiroketal system of the compounds as an active moiety. Biochemistry 39(20), 5995-6002 (2000).2. Puder, C., Loya, S., Hizi, A., et al. Structural and biosynthetic investigations of the rubromycins. Eur. J. Org. Chem. 2000(5), 729-735 (2000).3. Goldman, M.E., Salituro, G.S., Bowen, J.A., et al. Inhibition of human immunodeficiency virus-1 reverse transcriptase activity by rubromycins: Competitive interaction at the template.primer site. Mol. Pharmacol. 38(1), 20-25 (1990).
    • ¥ 1500
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  • (5E)-7-Oxozeaenol
    T354381198574-97-8
    (5E)-7-Oxozeaenol is a resorcylic acid lactone that has been found in the fungus MSX 63935 and has enzyme inhibitory and anticancer activities.1,2 It inhibits TGF-β-activated kinase 1 (TAK-1; IC50 = 1.3 μM).1 (5E)-7-Oxozeaenol inhibits proliferation of MCF-7, H460, SF-268, HT-29, and MDA-MB-435 human cancer cells with IC50 values of 4.9, 1.2, 5.6, 4.4, and 5.5 μM, respectively.2 |1. Fakhouri, L., El-Elimat, T., Hurst, D.P., et al. Isolation, semisynthesis, covalent docking and transforming growth factor beta-activated kinase 1 (TAK1)-inhibitory activities of (5Z)-7-oxozeaenol analogues. Bioorg. Med. Chem. 23(21), 6993-6999 (2015).|2. Ayers, S., Graf, T.N., Adcock, A.F., et al. Resorcylic acid lactones with cytotoxic and NF-κB inhibitory activities and their structure-activity relationships. J. Nat. Prod. 74(5), 1126-1131 (2011).
    • ¥ 2670
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  • 17β-hydroxy Exemestane
    T35676122370-91-6
    17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1,500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7aro cells in a concentration-dependent manner. 17β-hydroxy Exemestane (20 mg/kg) inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae, in ovariectomized rats.
    • ¥ 4600
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  • Aszonapyrone A
    T3575483103-08-6
    Aszonapyrone A is a meroditerpene fungal metabolite that has been found in Neosartorya and has diverse biological activities.1,2,3 It inhibits the growth of MCF-7, NCI H460, and A375-C5 cancer cells (GI50s = 13.6, 11.6, and 10.2 μM, respectively).1 Aszonapyrone A is active against multidrug-resistant isolates of S. aureus, E. faecalis, and E. faecium (MICs = 8, 16, and 16 μg/ml, respectively) and inhibits S. aureus biofilm formation.2 It is also active against P. falciparum in vitro (IC50 = 1.34 μg/ml).3
    • ¥ 17821
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  • Milbemycin A4 oxime
    T3590293074-04-5
    Milbemycin A4 oxime is a derivative of milbemycin A4 and a component of milbemycin oxime , compounds that both have insecticidal and nematocidal activity. Milbemycin A4 oxime (0.05 mg kg) reduces the number of microfilariae of the heartworm D. immitis in naturally infested dogs. It inhibits the growth of clinical isolates of C. glabrata with MIC80 values ranging from 16 to greater than 32 μg ml. Milbemycin A4 oxime (2.5 μg ml) blocks efflux of fluconazole from a clinical isolate of C. glabrata, but not from a strain lacking the efflux pumps CgCDR1 and PDH1, and reduces the MICs of fluconazole and 4-nitroquinoline 1-oxide in wild-type C. glabrata. It enhances adriamycin-induced inhibition of cell growth, as well as increases the intracellular accumulation of adriamycin and the P-glycoprotein substrate rhodamine 123 , in adriamycin-resistant, but not -sensitive, MCF-7 breast cancer cells in a concentration-dependent manner.
    • ¥ 5490
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  • Pyrocoll
    T35912484-73-1
    Pyrocoll is a bacterial metabolite originally isolated from Streptomyces. It inhibits the growth of A. aurescens, A. globiformis, A. oxydans, A. pascens, and R. erythropolis bacteria (MICs = 10, 1, 10, 3, and 10 μg ml, respectively) and HMO2, HepG2, and MCF-7 cancer cells (GI50s = 0.28, 0.42, and 2.2 μg ml, respectively) in vitro. Pyrocoll is also active against P. falciparum and T. rhodesiense (IC50s = 1.19 and 1.97 μg ml, respectively).
    • ¥ 3356
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  • Diallyl Tetrasulfide
    ICD-1585
    T360572444-49-7
    Diallyl tetrasulfide is an organosulfur compound that has been found in A. sativum and has diverse biological activities, including antimicrobial, antioxidant, and anticancer properties.[1],[2],[3],[4] It is active against the bacteria S. aureus and methicillin-resistant S. aureus (MRSA; MICs = 0.5 and 2 mg L, respectively), as well as the fungi C. albicans, C. krusei, C. glabrata, A. niger, A. flavus, and A. fumigatus (MICs = 0.5, 4, 2, 1, 2, and 4 mg L, respectively).[1] It reduces cadmium-induced increases in hepatic levels of thiobarbituric acid reactive substances (TBARS) and increases cadmium-induced decreases in the hepatic activity of superoxide dismutase (SOD1), catalase, GST, and glucose-6-phosphate dehydrogenase (G6PDH) in rats when administered at a dose of 40 mg kg.[2] Diallyl tetrasulfide is cytotoxic to MCF-7 breast cancer cells (IC50 = 92 μM) and reduces tumor growth in a BGC-823 mouse xenograft model when administered at doses of 20, 30, and 40 mg kg for 32 days.[3],[4]
    • 待估
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  • (S)-α-Methylbenzyl Ricinoleamide
    T364491246776-22-6
    (S)-α-Methylbenzyl ricinoleamide is a fatty acid amide derived from ricinoleic acid and methyl benzylamine. It demonstrates potent growth inhibition of glioma (U251), breast (MCF-7), ovarian (NCI-ADR/RES and OVCAR-3), kidney (786-0), non-small cell lung (NCI-H460), and prostate (PC-3) cancer cells with a mean GI50 value of 6.9 μM.
    • 待估
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  • CAY10701
    CAY10701
    T364581616967-52-2
    CAY10701 is a 7-deazahypoxanthine analog that prevents microtubule formation, blocking the proliferation of HeLa and MCF-7 cells (GI50s = 22 and 38 nM, respectively). It also inhibits the growth of several different colorectal cancer cell lines (GI50 values range from 9 to 17 nM), while being at least 1,500-fold less effective against normal human fibroblast WI38 cells. CAY10701 is effective in vivo, reducing tumor volume in colorectal cell xenografts in mice without significantly altering body weight.
    • ¥ 10600
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  • Malformin A
    T364893022-92-2
    Malformin A is a cyclopentapeptide fungal metabolite that has been found in A. niger and has diverse biological activities. It is a plant growth regulator that induces malformations in plant structure. Malformin A inhibits replication of tobacco mosaic virus (TMV) in local lesion and leaf-disc assays (IC50s = 19.7 and 45.4 μg/ml, respectively). It is cytotoxic to NCI-H460, MIA PaCa-2, MCF-7, SF-268, and WI-38 cancer cells (IC50s = 70, 50, 100, 70, and 100 nM, respectively), inhibits proliferation of PC3 and LNCaP cells (IC50s = 130 and 90 nM, respectively), and induces apoptosis and necrosis in PC3 and LNCaP cells. Malformin A also increases the accumulation of reactive oxygen species, decreases the mitochondrial membrane potential, and induces autophagy in PC3 and LNCaP cells. It is toxic to mice when administered intraperitoneally (LD50 = 3.1 mg/kg) but not orally up to doses of 50 mg/kg.
    • ¥ 4560
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