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  • 抑制剂&激动剂
    26
    TargetMol | Inhibitors_Agonists
  • 重组蛋白
    38
    TargetMol | Recombinant_Protein
  • 多肽产品
    2
    TargetMol | Peptide_Products
  • 染料试剂
    5
    TargetMol | Dye_Reagents
  • 天然产物
    3
    TargetMol | Natural_Products
  • 检测抗体
    22
    TargetMol | Antibody_Products
  • C75
    C-75
    T10657218137-86-1
    C75 是一种合成脂肪酸合酶 (FASN) 抑制剂,可抑制前列腺癌细胞 PC3 (IC50: 35 μM)。C75 增加 CPT1 活性,降低 DIO。
    • ¥ 368
    In stock
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  • trans-C75
    (±)-C75, 反-4-羧基-5-辛基-3-甲基-丁内酯
    T10656191282-48-1
    trans-C75 ((±)-C75) 是一种 C75 的对映异构体。其中 C75 是一种脂肪酸合成酶 (FASN) 的抑制剂。
    • ¥ 326
    In stock
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    TargetMol | Inhibitor Sale
  • SP600125
    Pyrazolanthrone, Nsc75890, JNK Inhibitor II, 1PMV
    T3109129-56-6
    SP600125 (JNK Inhibitor II) 是一种 JNK 抑制剂,抑制 JNK1、JNK2 和 JNK3 (IC50=40 40 90 nM),具有口服有效性、可逆性和 ATP 竞争性。SP600125 是一种有效的铁死亡抑制剂,可以抑制自噬,诱导凋亡。
    • ¥ 449
    In stock
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    数量
    TargetMol | Inhibitor Hot
  • Trifluridine
    曲氟胸苷, 曲氟尿苷, Viroptic, Trifluridina, Trifluorothymidine, NSC 75520, NSC 529182, 5-Trifluorothymidine
    T142870-00-8
    Trifluridine (NSC-75520) 是一种氟化胸苷类似物,具有潜在的抗肿瘤活性,还具有抗病毒活性。它掺入 DNA 并抑制胸苷酸合酶,从而抑制 DNA 合成、抑制蛋白质合成和细胞凋亡。
    • ¥ 130
    In stock
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  • SC-75416
    SC75416, SC 75416
    T28703215122-74-0
    SC-75416 是一种选择性COX-2抑制剂,可用于研究疼痛。
    • ¥ 1980 TargetMol
    In stock
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  • SC75741
    T6661913822-46-5
    SC75741 是NF-κB 抑制剂,对p65的IC50为 200 nM。它可阻断流感病毒复制。它通过损害NF-κB 亚基 p65 的 DNA 结合,导致细胞因子,趋化因子和促凋亡因子的表达降低,抑制 caspase 活化和阻断 caspase 介导的病毒核糖核蛋白的核输出。
    • ¥ 285
    In stock
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  • NSC756093
    NSC-756093, NSC 756093
    T245571629908-92-4
    NSC756093 可能抑制 GBP1:PIM1 相互作用。 NSC756093 可用于卵巢癌研究。
    • ¥ 589
    In stock
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    TargetMol | Inhibitor Sale
  • Sulfinpyrazone
    (+ -)-Sulfinpyrazone, 苯磺保泰松, G-28315, NSC 75925
    T043557-96-5
    Sulfinpyrazone (NSC-75925) 是一种口服有效的尿酸剂,具有抗血栓和血小板抑制作用。它可作用于慢性和间歇性痛风性关节炎。
    • ¥ 99
    In stock
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  • LDC7559
    T118282407782-01-6
    LDC7559 通过在晚期阻断中性粒细胞胞外陷阱 (NET)来抑制gasdermin D (GSDMD)。
    • ¥ 689
    In stock
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  • Pentaerythritol diacrolein acetal
    NSC-7585, NSC7585, NSC 7585
    T2021078-19-3
    Pentaerythritol diacrolein acetal is an agent of biochemical.
    • 待询
    3-6月
    规格
    数量
  • Isoliquiritigenin
    异甘草素, Isoliquiritigen, ISL, GU17
    T0725961-29-5
    Isoliquiritigenin (ISL) 属于黄酮类天然产物,抑制流感病毒复制 (EC50=24.7 μM),也抑制 aldose reductase 的活性 (IC50=320 nM)。Isoliquiritigenin 具有抗肿瘤的活性。
    • ¥ 230
    In stock
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  • CHMFL-ABL/KIT-155
    CHMFL-ABL-KIT-155
    T108012081093-21-0
    CHMFL-ABL KIT-155 is a highly potent and orally active type II ABL c-KIT dual kinase inhibitor (IC50s: 46 nM 75 nM). It arrests cell cycle progression and induces apoptosis.
    • ¥ 11700
    6-8周
    规格
    数量
  • PPO-IN-17
    T205070
    PPO-IN-17 (Compound 6R) 是一种原卟啉原 IX 氧化酶(PPO)抑制剂,其能够抑制烟草 PPO(NtPPO),Ki 为 30.34 nM。PPO-IN-17 展现除草效果,在浓度为 37.5 g hm² 时,对稗草(E. crus-galli)、狐尾草(D. sanguinalis)、苜蓿(M. sativa)及加拿大苍耳(C. canadensis)的抑制率超过95%。该化合物对水稻(浓度为 75 g hm²)和蜜蜂(浓度为 6400 mg kg)无毒性。
    • 待询
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  • Masitinib
    马赛替尼, SB-75 diacetate, AB1010
    T2609790299-79-5
    Masitinib (AB1010) 是生物口服可利用的选择性 c-Kit 抑制剂 (对于人重组c-Kit,IC50=200 nM),它还抑制PDGFRα β(IC50s=540 800 nM),Lyn(对 LynB 的IC50=510 nM),Lck,较小程度上抑制FGFR3和FAK。它有抗增殖,促凋亡活性,且毒性低。
    • ¥ 198
    In stock
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  • Ajoene
    T3562492285-01-3
    Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg ml) and Gram-negative bacteria (MICs = 136-200 µg ml), as well as yeasts (MICs = 10-20 µg ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16 BL6 mouse model of melanoma when administered at a dose of 25 mg kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg kg.3Ajoene (25 mg kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16 BL6 melanoma cells in C57BL 6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)
    • ¥ 19800
    待询
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  • AAA
    T35855
    AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension when administered prior to induction or after establishment of hypertension.2 1.Cárdenas, S., Colombero, C., Panelo, L., et al.GPR75 receptor mediates 20-HETE-signaling and metastatic features of androgen-insensitive prostate cancer cellsBiochim. Biophys. Acta Mol. Cell Biol. Lipids1865(2)158573(2020) 2.Sedláková, L., Kikerlová, S., Husková, Z., et al.20-Hydroxyeicosatetraenoic acid antagonist attenuates the development of malignant hypertension and reverses it once established: a study in Cyp1a1-Ren-2 transgenic ratsBiosci. Rep.38(5)BSR20171496(2018)
    • ¥ 8599
    待询
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    数量
  • Arecaidine propargyl ester (hydrobromide)
    T36241116511-28-5
    Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecaidine propargyl ester decreases mean arterial blood pressure in normotensive cats (ED25= 1.9 nmol kg).3It is toxic to house flies (Musca) when administered at a dose of 75 μg fly.4 1.Scapecchi, S., Matucci, R., Bellucci, C., et al.Highly chiral muscarinic ligands: the discovery of (2S,2’R,3’S,5’R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonistJ. Med. Chem.49(6)1925-1931(2006) 2.Di Bari, M., Tombolillo, B., Conte, C., et al.Cytotoxic and genotoxic effects mediated by M2 muscarinic receptor activation in human glioblastoma cellsNeurochem. Int.90261-270(2015) 3.Porsius, A.J., and Van Zwieten, P.A.Central action of some cholinergic drugs (arecaidine esters) and nicotine on blood pressure and heart rate of catsProg. Brain Res.47131-135(1977) 4.Honda, H., Tomizawa, M., and Casida, J.E.Insect muscarinic acetylcholine receptor: Pharmacological and toxicological profiles of antagonists and agonistsJ. Agric. Food Chem.55(6)2276-2281(2007)
    • 待估
    35日内发货
    规格
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  • D-erythro/L-threo Lysosphingomyelin (d18:1)
    D-erythro L-threo Lysosphingomyelin (d18:1)
    T3718782970-80-7
    Lysosphingomyelin is an endogenous bioactive sphingolipid and a constituent of lipoproteins.1,2It is produced by the removal of the acyl group from sphingomyelin by a deacylase and acts as a precursor in the biosynthesis of sphingosine-1-phosphate . D-erythroLysosphingomyelin is an agonist of the S1P receptors S1P1, S1P2, and S1P3(EC50s = 167.7, 368.1, and 482.6 nM, respectively, for the human receptors).3It is also an agonist of the orphan receptor ovarian cancer G protein-coupled receptor 1 (ORG1) that induces calcium accumulation in cells overexpressing OGR1 (EC50= ~35 nM).4Levels of D-erythrolysosphingomyelin are increased in skin isolated from patients with atopic dermatitis, as well as postmortem brain from patients with Niemann-Pick disease type A, but not type B.2,5L-threolysosphingomyelin is also an S1P1-3agonist (EC50s = 19.3, 131.8, and 313.3 nM, respectively).3This product is a mixture of D-erythroand L-threolysosphingomyelin. [Matreya, LLC. Catalog No. 1321] 1.Ito, M., Kurita, T., and Kita, K.A novel enzyme that cleaves the N-acyl linkage of ceramides in various glycosphingolipids as well as sphingomyelin to produce their lyso formsJ. Biol. Chem.270(41)24370-24374(1995) 2.Nixon, G.F., Mathieson, F.A., and Hunter, I.The multi-functional role of sphingosylphosphorylcholineProg. Lipid Res.47(1)62-75(2008) 3.Im, D.-S., Clemens, J., Macdonald, T.L., et al.Characterization of the human and mouse sphingosine 1-phosphate receptor, S1P5 (Edg-8): Structure-activity relationship of sphingosine1-phosphate receptorsBiochemistry40(46)14053-14060(2001) 4.Meyer zu Heringdorf, D., Himmel, H.M., and Jakobs, K.H.Sphingosylphosphorylcholine-biological functions and mechanisms of actionBiochim. Biophys. Acta1582(1-3)178-189(2002) 5.Rodriguez-Lafrasse, C., and Vanier, M.T.Sphingosylphosphorylcholine in Niemann-Pick disease brain: Accumulation in type A but not in type BNeurochem. Res.24(2)199-205(1999)
    • ¥ 2131
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  • PD-85639
    T70538149838-21-1
    PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM 40% & 20 μM 60% at pH 9.0, 5 nM 28% & 3 μM 72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM 39% & 10 μM 61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1 2 = 1.2 at 4°C, <0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 μM against 5 nM [3H]-BTX for binding rat neocrotical membranes).
    • ¥ 10600
    6-8周
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  • gne-3500
    T719331537859-24-7
    GNE-3500 is a Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C (RORc or RORγ) Inverse Agonist. Retinoic acid receptor-related orphan receptor C (RORc, RORγ, or NR1F3) is a nuclear receptor that plays a major role in the production of interleukin (IL)-17. Considerable efforts have been directed toward the discovery of selective RORc inverse agonists as potential treatments of inflammatory diseases such as psoriasis and rheumatoid arthritis. GNE-3500 possessed favorable RORc cellular potency with 75-fold selectivity for RORc over other ROR family members and >200-fold selectivity over 25 additional nuclear receptors in a cell assay panel. The favorable potency, selectivity, in vitro ADME properties, in vivo PK, and dose-dependent inhibition of IL-17 in a PK PD model support the evaluation of GNE3500 in preclinical studies (J. Med. Chem., 2015, 58 (13), pp 5308–5322)
    • ¥ 10600
    6-8周
    规格
    数量
  • N-Myristoyl-Lys-Arg-Thr-Leu-Arg
    T76185125678-68-4
    N-Myristoyl-Lys-Arg-Thr-Leu-Arg 是一种蛋白激酶 C (PKC) 抑制剂,其 IC50值为 75 μM。N-Myristoyl-Lys-Arg-Thr-Leu-Arg 抑制人白血病细胞系 Jurkat 中 IL-2受体的诱导和 IL-2的产生。
    • 待询
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  • SP-A (196-215) (human) TFA
    Surfactant Protein A,SPA4
    T83847
    表面活性蛋白A(SP-A)(196-215)是一种合成肽,与人类SP-A的C末端碳水化合物识别域的196至215氨基酸序列相对应。当浓度为1和10 µM时,它能抑制JAWSII鼠树突细胞中由LPS诱导的TNF-α释放。SP-A(196-215)(75 µM)促使JAWSII细胞吞噬P. aeruginosa。通过气管内给药,SP-A(196-215)(50 µg/动物)降低了小鼠P. aeruginosa感染模型的疾病严重程度和肺部形成菌落数。
    • 待估
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  • CYY292
    T839112644673-04-9
    CYY292是一种针对PDGFRα、PDGFRβ、FGFR1、-2和-3的抑制剂(IC50分别为5.35、4.6、28、28和78 nM)。该化合物对这些激酶的选择性高于FGFR4(IC50 > 1,000 nM),但也能抑制c-Kit、VEGFR2、VEGFR1和胰岛素样生长因子1受体(IGF-1R;IC50分别为67、33、36和75 nM),以及EGFR、布鲁顿酪氨酸激酶(BTK)、细胞周期依赖性激酶4(Cdk4)/cyclin D3和MET(IC50分别为128、198、214和396 nM)。CYY292抑制MG-63、U2OS、MNNG/HOS和Saos-2骨肉瘤细胞的增殖(IC50分别为0.84、0.76、1.36和0.72 µM)。在0.3和0.5 µM的浓度下,它抑制U87MG和LN-229胶质母细胞瘤细胞的迁移和侵袭。CYY292(30 mg/kg)在U87MG原位小鼠异种移植模型中降低肿瘤体积并增加生存率。
    • 待估
    35日内发货
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  • c-Met-IN-24
    T89911
    c-Met-IN-24(compound 3g)为一种对STAT-3(=4.7 μM)和c-MET(=12.67 μM)具有双重抑制作用的分子,显示出防癌活性。该化合物在阻断SNB-75细胞中的G2 M细胞周期并促进细胞凋亡(apoptosis)方面表现出疗效。此外,c-Met-IN-24也被应用于中枢神经系统癌症的相关研究。
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