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抑制剂&激动剂
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TargetMol产品目录中 "

thp-10

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  • 抑制剂&激动剂
    24
    TargetMol | Inhibitors_Agonists
  • 多肽产品
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    TargetMol | Peptide_Products
  • PROTAC
    4
    TargetMol | PROTAC
  • 天然产物
    1
    TargetMol | Natural_Products
  • BAZ1A-IN-1
    T9552941521-45-5
    BAZ1A-IN-1 是BAZ1A(含溴结构域蛋白)抑制剂(Kd:0.52 μM)。它对低表达BAZ1A 的癌细胞表现出弱活性或无活性,但对高表达BAZ1A 的癌细胞系显示出良好的抗生存作用。
    • ¥ 575
    In stock
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  • THP104c
    T9777877792-12-6
    THP104c 是有效的线粒体分裂抑制剂。
    • ¥ 916
    In stock
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  • MLN-3897
    CCR1 antagonist 10, AVE-9897, AVE9897, AVE 9897
    T280721010731-97-1In house
    MLN-3897 (CCR1 antagonist 10) 是一种具有口服活性的 CCR1 拮抗剂,对于 125I-MIP-1α 与 THP-1 细胞膜的结合,Ki 为 2.3 nM。 MLN-3897 抑制 Akt 信号转导和 MM 细胞存活和增殖。
    • ¥ 24800
    5日内发货
    规格
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  • Rifampicin
    利福平, Rimactane, Rifamycin AMP, Rifampin
    T068113292-46-1
    Rifampicin (Rifamycin AMP) 是一种广谱抗生素。Rifampicin 对结核杆菌有较强抗菌作用,对革兰氏阳性或阴性细菌、病毒等也有疗效。
    • ¥ 331
    In stock
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  • Ursolic acid
    熊果酸, Urson, Prunol, NSC-4060, NSC 167406, Malol
    T072277-52-1
    Ursolic acid (Prunol) 属于天然产物,是一种五环三萜羧酸,提取自毛喉杜鹃。Ursolic acid 具有抗肿瘤、抗炎、抗菌、降血糖等活性。
    • ¥ 140
    In stock
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  • STING-IN-10
    T200847
    STING-IN-10 (P8) 身为双重STING降解剂和抑制剂,在 THP-1 细胞中表现出 2.58 μM 的 DC50 值,并且具备抗炎活性。
    • 待询
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  • 2-chloro Palmitic Acid
    T3622119117-92-1
    2-chloro Palmitic acid is a monochlorinated form of palmitic acid . It is produced in a myeloperoxidase (MPO) and time-dependent manner in neutrophils stimulated by phorbol 12-myristate 13-acetate . 2-chloro Palmitic acid (10 μM) induces neutrophil extracellular trap (NET) formation (NETosis) in human neutrophils, increasing DNA release from neutrophils, colocalization of MPO with extracellular DNA (ecDNA), and trapping of E. coli. It increases COX-2 protein levels in human coronary artery endothelial cells (HCAECs) when used at a concentration of 50 μM and increases production of P-selectin, von Willebrand factor, and angiopoietin-2 in HCAECs, as well as neutrophil and platelet adherence, when used at a concentration of 10 μM. 2-chloro Palmitic acid (10-50 μM) also induces apoptosis in THP-1 cells and primary human monocytes and increases caspase-3 activity in THP-1 cells.
    • 待估
    35日内发货
    规格
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  • CAY10748
    CAY10748
    T364612412902-55-5
    CAY10748 is an agonist of stimulator of interferon genes (STING; IC50= 0.3794 μM in a competition binding assay).1It activates STING in STING-expressing, but not STING knockout, THP-1 cells (EC50s = 0.287 and >100 μM, respectively, in a reporter assay). It induces phosphorylation of STING at the serine in position 366, as well as phosphorylation of TBK1 and IFN regulatory factor 3 (IRF3), indicating activation of the STING-TBK1-IRF3 signaling pathway. CAY10748 increases the secretion of IFN-β and the levels of chemokine (C-X-C motif) ligand 10 (CXCL10), and IL-6 in peripheral blood mononuclear cells (PBMCs) when used at a concentration of 10 μM. It also reduces tumor growth in a CT26 murine colon cancer model when administered at a dose of 0.15, but not 1.5, mg/kg. 1.Xi, Q., Wang, M., Jia, W., et al.Design, synthesis, and biological evaluation of amidobenzimidazole derivatives as stimulator of interferon genes (STING) receptor agonistsJ. Med. Chem.63(1)260-282(2019)
    • 待估
    35日内发货
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  • MSA-2 dimer
    T369962377881-92-8
    MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide[1]. MSA-2 dimer (60 mg kg; p.o.; 50 days) inhibits tumor growth and prolongs overall survival[1]. MSA-2 dimer (40 mg kg; s.c.; 25 days) induces complete tumor regression[1].MSA-2 dimer (60 mg kg; p.o.; 4 hours) increases proinflammatory cytokine (IFN-β) level in tumors[1].MSA-2 dimer (60 mg kg; s.c.; 4 hours) concentrations is observed in tumors than in plasma or other nontumor tissues [1].MSA-2 dimer (THP-1 cells) induces phosphorylation of both TBK1 and IR. MSA-2 dimer (10 μM and 33 μM; macrophages) induces IFN-β[1].MSA-2 dimer also exhibits dose-dependent antitumor activity when administered by IT, SC, or PO routes[1]. [1]. Pan BS, et al. An orally available non-nucleotide STING agonist with antitumor activity. Science. 2020;369(6506):eaba6098.
    • 待询
    10-14周
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  • Diprovocim-1
    T377222170867-89-5
    Diprovocim-1 is an agonist of the toll-like receptor 1/2 heterodimer.1It induces TNF-α release in THP-1 cells (EC50= 110 pM), an effect that can be inhibited by anti-TLR1 or anti-TLR2 antibodies. Diprovocim-1 (10 mg/kg) increases the production of ovalbumin-specific IgG1 in wild-type, but notTLR2-/-, mice sensitized to ovalbumin.2It also enhances anti-PD-L1 antibody-induced activation of cytotoxic T lymphocytes, reduction of tumor growth, and increases in survival in a B16/F10 murine melanoma model. 1.Morin, M.D., Wang, Y., Jones, B.T., et al.Diprovocims: A new and exceptionally potent class of toll-like receptor agonistsJ. Am. Chem. Soc.140(43)14440-14454(2018) 2.Wang, Y., Su, L., Morin, M.D., et al.Adjuvant effect of the novel TLR1/TLR2 agonist Diprovocim synergizes with anti-PD-L1 to eliminate melanoma in miceProc. Natl. Acad. Sci. U.S.A.115(37)E8698-E8706(2018)
    • 待估
    35日内发货
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  • STING Agonist 12b
    T381592411100-70-2
    STING agonist 12b is an agonist of stimulator of interferon genes (STING).1It binds to STING (Kd= 26.4 μM) and induces interferon reporter gene expression in cells expressing human or mouse STING (EC50s = 7.45 and 10.23 μM, respectively). STING agonist 12b (40 μM) induces expression of TNF-a, IL-6, IP-10, and IL-1b in THP-1 cells. 1.Hou, S., Lan, X.-j., Li, W., et al.Design, synthesis and biological evaluation of acridone analogues as novel STING receptor agonistsBioorg. Chem.95103556(2020)
    • 待估
    35日内发货
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  • STING Agonist 1a
    T38160652142-94-4
    STING agonist 1a is an agonist of stimulator of interferon genes (STING).1It induces expression of an IRF-inducible SEAP reporter gene in a cell-based assay (EC50= 16.77 μM). STING agonist 1a (12.5-100 μM) induces expression of IFN-β, IL-6, and chemokine (C-X-C motif) ligand 10 (CXCL10) in THP-1 cells, an effect that can be reversed by STING knockout or the STING inhibitor H-151 . 1.Hou, H., Yang, R., Liu, X., et al.Discovery of triazoloquinoxaline as novel STING agonists via structure-based virtual screeningBioorg. Chem.100103958(2020)
    • 待估
    35日内发货
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  • STING18
    T381622706536-26-5
    STING18 is a competitive ligand of stimulator of interferon genes (STING; IC50 = 0.068 μM in a radioligand binding assay).1 It inhibits cGAMP-induced IFN-β production (IC50 = 11 μM) but does not stimulate IFN-β production (EC50 = >30 μM) in THP-1 cells. |1. Siu, T., Altman, M.D., Baltus, G.A., et al. Discovery of a novel cGAMP competitive ligand of the inactive form of STING. Med. Chem. Lett. 10(1), 92-97 (2019).
    • ¥ 988
    待询
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  • CU-32
    T383282400954-16-5
    CU-32 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50= 0.45 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. It is also selective for cGAS over toll-like receptors (TLRs) at 50 μM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP synthase inhibitorsJ. Org. Chem.85(3)1579-1600(2020)
    • 待估
    35日内发货
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  • CU-76
    T383292400954-58-5
    CU-76 is an inhibitor of cyclic GMP-AMP synthase (cGAS; IC50= 0.24 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. CU-76 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP synthase inhibitorsJ. Org. Chem.85(3)1579-1600(2020)
    • 待估
    35日内发货
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  • THP-PEG10-OH
    THP-PEG10-OH
    T40531
    THP-PEG10-OH is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
    • 待询
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  • MS-PEG10-THP
    MS-PEG10-THP
    T4053242607-91-0
    MS-PEG10-THP is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
    • 待询
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  • THP-PEG10-THP
    THP-PEG10-THP
    T4053342749-29-1
    THP-PEG10-THP is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
    • 待询
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  • nod2 antagonist 1
    T630882411441-54-6
    NOD2 antagonist 1 (compound 32) 是一种有效的、选择性的 NOD2 拮抗剂 (IC50: 5.23 μM)。NOD2 antagonist 1 在 THP-1 细胞,对 Muramyl dipeptide (MDP) 诱导的 IL-8 分泌表现出抑制作用。NOD2 antagonist 1 在 PBMCs 细胞,可以抑制 MDP 诱导的 IL-6、IL-10 和 TNF-α 的水平升高。
    • ¥ 11217
    6-8周
    规格
    数量
  • STING modulator-4
    T726152839639-72-2
    STINGmodulator-4 是一种竞争性的 STING 调节剂,对 R232HSTING 的 Ki 为 0.0933 μM。STINGmodulator-4 在 THP-1 细胞中对 p-IRF3 的 EC50为 >10 μM。
    • ¥ 11700
    6-8周
    规格
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  • STING Agonist 12L
    Stimulator of Interferon Genes Agonist 12L
    T837752913152-30-2
    STING激动剂12L是一种刺激干扰素基因(STING)的激动剂。它与野生型STING结合(IC50 = 1.15 µM),以及STING的R232、AQ和Q变体(IC50分别为1.06、0.61和1.12 µM),并在THP-1和RAW 264.7细胞中诱导报告基因表达(EC50分别为0.38和12.94 µM)。STING激动剂12L (5 µM)在THP-1细胞中诱导IFNB1、CXCL10和IL6 mRNA的表达。在体内,STING激动剂12L (10 mg/kg)提高了血浆IFN-β水平,并且在B16/F10小鼠黑色素瘤模型中减少了肿瘤体积和肺转移灶的数量。
    • 待估
    35日内发货
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  • STING Agonist D61
    D61,Stimulator of Interferon Genes Agonist D61
    T838412850251-27-1
    STING激动剂D61(D61)是干扰素基因刺激剂(STING)的激动剂。它在基于细胞的分析中诱导IFN3诱导的分泌性碱性磷酸酶(SEAP)报告基因和IFN-β诱导的报告基因的表达(EC50分别为52.9和116 nM)。D61(4, 6, 和8 µM)增加了编码IFN-β和化学因子(C-X-C基序)配体10(CXCL10)的mRNA的表达以及TANK结合激酶1(TBK1)、IRF3和STING在THP-1单核细胞中的磷酸化。在体内,D61(每隔一天0.25 mg/kg)在CT26小鼠结肠癌模型中减少肿瘤体积,而不影响体重。
    • 待估
    35日内发货
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  • AP-1
    T83856
    AP-1是一种微型化的蛋白质水解靶向嵌合体(PROTAC),由吲哚美辛(±)连接的间变性淋巴瘤激酶(ALK)配体和E3泛素连接酶配体通过超短连接器相连。在10至300 nM浓度范围内使用时,AP-1能高效降解Karpas-299细胞中高表达的ALK融合蛋白NPM-ALK,此效应可被蛋白酶体抑制剂MG-132阻断。它还能降解在SN-N-SH和NCI H3122细胞中表达的ALK融合蛋白EML4-ALK及含有苯丙氨酸至亮氨酸替换突变(ALKF1174L)的ALK。AP-1对依赖ALK的Karpas-299细胞具有细胞毒性(IC50 = 0.1265 nM),但对非ALK依赖的THP-1细胞无细胞毒性(IC50 = 2,704 nM)。在给药剂量为25, 50, 和100 mg/kg时,能减小NCI H3122小鼠移植瘤模型中的肿瘤体积。
    • 待估
    35日内发货
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  • AI-10-47
    1H-Benzimidazole, 2-(2-pyridinyl)-6-(trifluoromethoxy)-AI-10-47
    T90161256094-31-1
    AI-10-47 (1H-Benzimidazole, 2-(2-pyridinyl)-6-(trifluoromethoxy)-AI-10-47) 是 CBFβ-RUNX 结合的小分子抑制剂(IC50:3.2 μM)。
    • ¥ 367
    In stock
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