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TargetMol产品目录中 "

sting in 3

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  • 抑制剂&激动剂
    21
    TargetMol | Inhibitors_Agonists
  • 重组蛋白
    2
    TargetMol | Recombinant_Protein
  • 天然产物
    3
    TargetMol | Natural_Products
  • STING-IN-3
    C-171
    T90292244881-69-2
    STING-IN-3 (C-171) 是干扰素基因刺激物 (STING) 的抑制剂。 它与 STING 结合,抑制其棕榈酰化,并阻止 TBK1 的募集和磷酸化。
    • ¥ 255
    In stock
    规格
    数量
    TargetMol | Inhibitor Sale
  • STING modulator-3
    T726142839639-94-8
    STINGmodulator-3 是一种 STING 抑制剂。在闪烁接近实验中,STINGmodulator-3 抑制 R232STING 的 Ki 值为 43.1 nM。STINGmodulator-3 对 THP-1 细胞的 IRF-3 激活和 TNF-β诱导无影响。
    • ¥ 15000
    8-10周
    规格
    数量
  • STING agonist-3
    T130142138299-29-1
    STING agonist-3 is a selective and non-nucleotide small-molecule STING agonist(pEC50 and pIC50 of 7.5 and 9.5, respectively), has durable anti-tumor effect and tremendous potential to improve treatment of cancer.
    • 待估
    35日内发货
    规格
    数量
  • STING agonist-3 trihydrochloride
    STING agonist-3 trihydrochloride (2138299-29-1 free base)
    T13014L
    STING agonist-3 trihydrochloride is a selective and non-nucleotide agonist of small-molecule STING(pEC50 and pEC50 of 7.5 and 9.5, respectively), has durable anti-tumor effect and tremendous potential to improve treatment of cancer.
    • 待询
    规格
    数量
  • TargetMol
    2',3'-cGAMP sodium
    2'-3'-cyclic GMP-AMP sodium
    T10065L2734858-36-5In house
    2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) 是细胞天然免疫中第二信使,在 DNA 结合条件下由 cGAMP 合成酶 (cGAS) 催化形成。2',3'-cGAMP sodium 可与 STING 结合形成二聚体,诱导 IFN-β 及其他细胞因子的产生和表达。
    • ¥ 2980
    In stock
    规格
    数量
    TargetMol | Inhibitor Hot
  • MSA-2
    T8798129425-81-6
    MSA-2 是可口服的非核苷酸 STING 激动剂,MSA-2 的非共价体系二聚体与 STING 纳摩尔亲和力结合。它在同基因小鼠肿瘤模型中显示抗肿瘤活性,与抗 PD-1 协同作用,可刺激肿瘤分泌干扰素-β,诱导肿瘤消退,具有持久的抗肿瘤免疫。[3]
    • ¥ 987
    In stock
    规格
    数量
    TargetMol | Inhibitor Hot
  • 2',3'-cGAMP
    2'-3'-cyclic GMP-AMP
    T100651441190-66-4
    2',3'-cGAMP (2'-3'-cyclic GMP-AMP) 是细胞天然免疫中第二信使,在DNA结合条件下由 cGAMP 合成酶 (cGAS) 催化形成。2',3'-cGAMP 可与 STING 结合形成二聚体,诱导干扰素-β(IFN-β)及其他细胞因子的产生和表达。
      5日内发货
      询价
    • diABZI-V/C-DBCO
      T200187
      diABZI-V C-DBCO(Compound 3)作为一种高效的STING激动剂,通过组织蛋白酶B的作用释放diABZI-胺,激活STING,从而使干扰素及其他免疫激活分子的生成得以提高,有效增强免疫系统对肿瘤的攻击能力。在THP1-Dual细胞中,diABZI-V C-DBCO与diABZI-胺激活STING的EC50值分别为1.47 nM和0.144 nM;在原代小鼠脾细胞中,这些值分别为7.7 μM和0.17 μM。因此,diABZI-V C-DBCO在癌症免疫研究领域具有重要的应用价值。
      • 待询
      规格
      数量
    • cAIMP
      CL-592, CL592, CL 592, CHEMBL4776666
      T2020101507367-51-2
      cAIMP作为STING激动剂,在体外的哺乳动物细胞中,与标准的小鼠(DMXAA)和人类(2',3'-cGAMP)STING激动剂相比,cAIMP类似物能更强烈地激活STING依赖的IRF和NF-κB信号通路。在人类血液的离体实验中,它们能诱导I型干扰素(IFNs)和促炎细胞因子的产生。
      • 待询
      10-14周
      规格
      数量
    • 5'-pApA (sodium salt)
      T35422
      5'-pApA is a linearized form of cyclic di-AMP, a bacterial second messenger that activates the host innate immune system through stimulator of interferon genes (STING).1,2,3,4It is a metabolite of cyclic di-AMP formedviahydrolysis by various phosphodiesterases (PDEs).55'-pApA is intended for use as a negative control for cyclic di-AMP signaling. 1.Burdette, D.L., Monroe, K.M., Sotelo-Troha, K., et al.STING is a direct innate immune sensor of cyclic-di-GMPNature478(7370)515-518(2011) 2.Parvatiyar, K., Zhang, Z., Teles, R.M., et al.DDX41 recognizes bacterial secondary messengers cyclic di-GMP and cyclic di-AMP to activate a type I interferon immune responseNat. Immunol.13(12)1155-1161(2012) 3.Woodward, J.J., Iavarone, A.T., and Portnoy, D.A.c-di-AMP secreted by intracellular Listeria monocytogenes activates a host type I interferon responseScience328(5986)1703-1705(2010) 4.Witte, C.E., Whiteley, A.T., Burke, T.P., et al.Cyclic di-AMP is critical for Listeria monocytogenes growth, cell wall homeostasis, and establishment of infectionmBio4(3)e00282-00213(2013) 5.Fahmi, T., Port, G.C., and Cho, K.H.c-di-AMP: An essential molecule in the signaling pathways that regulate the viability and virulence of gram-positive bacteriaGenes (Basel)8(8)197(2017)
      • ¥ 3740
      35日内发货
      规格
      数量
    • 3,3'-((2-Chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one)
      T361334322-58-1
      3,3'-((2-Chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) is a non-nucleotide inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; Ki = 50 μM).1,2 It also inhibits urease (IC50 = 84.53 μM for the Jack bean enzyme).3 |1. Choudhary, M.I., Fatima, N., Khan, K.M., et al. New biscoumarin derivatives-cytotoxicity and enzyme inhibitory activities. Bioorg. Med. Chem. 14(23), 8066-8072 (2006).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, and small molecule inhibitors - A STING in the tale of ENPP1. Molecules 24(22), E4192 (2019).|3. Khan, K.M., Iqbal, S., Lodhi, M.A., et al. Biscoumarin: New class of urease inhibitors; economical synthesis and activity. Bioorg. Med. Chem. 12(8), 1963-1968 (2004).
      • 待估
      35日内发货
      规格
      数量
    • 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
      规格
      数量
    • CAY10761
      CAY10761
      T37832333409-31-7
      CAY10761 is an inhibitor of ectonucleotide pyrophosphatase phosphodiesterase 1 (ENPP1; IC50s = 467 and 429 μM for the human and snake venom enzymes, respectively).1,2 It also inhibits mushroom tyrosinase (Ki = 1.9 μM) and urease from jack bean, P. mirabilis, and B. pasteurii (IC50s = 0.093, <0.125, and 0.089 mM, respectively, at pH 8.2).3,4 |1. Khan, K.M., Fatima, N., Rasheed, M., et al. 1,3,4-Oxadiazole-2(3H)-thione and its analogues: A new class of non-competitive nucleotide pyrophosphatases phosphodiesterases 1 inhibitors. Bioorg. Med. Chem. 17(22), 7816-7822 (2009).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, and small molecule inhibitors - A STING in the tale of ENPP1. Molecules 24(22), E4192 (2019).|3. Ghani, U., and Ullah, N. New potent inhibitors of tyrosinase: Novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site. Bioorg. Med. Chem. 18(11), 4042-4048 (2010).|4. Amtul, Z., Rasheed, M., Choudhary, M.I., et al. Kinetics of novel competitive inhibitors of urease enzymes by a focused library of oxadiazoles thiadiazoles and triazoles. Biochem. Biophys. Res. Commun. 319(3), 1053-1063 (2004).
      • 待估
      35日内发货
      规格
      数量
    • STING Agonist C11
      STING Agonist C11
      T38161875863-22-2
      STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.1 It induces secretion of type I IFN from THF and MM6 cells when used at a concentration of 50 μM. STING agonist C11 induces phosphorylation of IFN regulatory factor 3 (IRF3) and increases expression of IFIT1 and viperin, but not IL-1β, IL-6, or IL-8 in THF cells in a STING-dependent manner. It reduces viral titers of chikungunya, Venezuelan equine encephalitis, o'nyong-nyong, Mayaro, and Ross River viruses grown in THF cells (EC90s = 16.44, 16.7, 18.84, 25.19, and 22.57 μM, respectively), an effect that is dependent on the presence of STING and the IFN-α β receptor (IFNAR).References1. Gall, B., Pryke, K., Abraham, J., et al. Emerging alphaviruses are sensitive to cellular states induced by a novel small-molecule agonist of the STING pathway. J. Virol. 92(6), e01913-01917 (2018). STING agonist C11 is an agonist of the stimulator of interferon genes (STING) pathway.1 It induces secretion of type I IFN from THF and MM6 cells when used at a concentration of 50 μM. STING agonist C11 induces phosphorylation of IFN regulatory factor 3 (IRF3) and increases expression of IFIT1 and viperin, but not IL-1β, IL-6, or IL-8 in THF cells in a STING-dependent manner. It reduces viral titers of chikungunya, Venezuelan equine encephalitis, o'nyong-nyong, Mayaro, and Ross River viruses grown in THF cells (EC90s = 16.44, 16.7, 18.84, 25.19, and 22.57 μM, respectively), an effect that is dependent on the presence of STING and the IFN-α β receptor (IFNAR). References1. Gall, B., Pryke, K., Abraham, J., et al. Emerging alphaviruses are sensitive to cellular states induced by a novel small-molecule agonist of the STING pathway. J. Virol. 92(6), e01913-01917 (2018).
      • 待估
      35日内发货
      规格
      数量
    • 2',3'-cGAMP-C2-PPA
      2',3'-cGAMP-C2-PPA
      T402242586047-11-0
      2',3'-cGAMP-C2-PPA (45) is a cyclic di-nucleotide that acts as a STING agonist (US20210015941A1). It is a drug-linker conjugate for antibody-drug conjugates (ADC) used in the targeted treatment of cancer.
      • 待询
      规格
      数量
    • 3',3'-cGAMP sodium salt
      T41205
      3',3'-cGAMP sodium salt is a STING agonist. Reduces B cell proliferation and induces apoptosis of malignant B cellsin vitro. Suppresses 5TGM1 multiple myeloma xenograft growth in immunodeficient mice, and induces leukemic regression in Eμ-TCL1 mice.
      • 待询
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    • cGAMP diammonium
      T73717
      cGAMP (Cyclic GMP-AMPP) diammonium 是一种内源性第二信使,通过触发干扰素的产生来响应胞浆 DNA。它通过激活干扰素基因刺激因子(STING),启动信号级联,进而导致I型干扰素及其他免疫介质的生成。
      • 待询
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    • c-di-AMP disodium
      T738732734909-87-4
      c-di-AMP (Cyclic diadenylate) sodium 作为一种STING 激动剂,通过结合STING 激活TBK3-IRF3 信号途径,引发I 型 IFN 和 TNF 产生,兼具细菌第二信使功能,在革兰氏阳性细菌中调控细胞生长、存活及毒力,并影响宿主免疫反应。此外,作为有效的粘膜佐剂,它能刺激体液和细胞反应。
      • ¥ 3180
      35日内发货
      规格
      数量
    • STING-IN-7
      T81082899947-07-0
      STING-IN-7(化合物 21),作为一种STING抑制剂,具有11.5 nM的IC50值,能够抑制STING与干扰素调节因子 3 (IRF3) 的磷酸化。
      • 待询
      8-10周
      规格
      数量
    • S-72
      T838742446799-14-8
      S-72是一种微管聚合抑制剂,以1, 3, 10 µM的浓度在无细胞测定中抑制微管聚合,并在MCF-7和耐紫杉醇的MCF-7/T乳腺癌细胞中降低细胞活性(IC50分别为15.64和26.32 nM)。50 nM浓度的S-72能抑制MCF-7和MCF-7/T细胞的迁移和侵袭,并减少划痕实验中的伤口闭合百分比。100 nM的S-72在MCF-7/T细胞中诱导G2/M期的细胞周期阻滞以及凋亡,并在同一浓度下抑制这些细胞中干扰素基因激活剂(STING)的激活。以每天15 mg/kg的剂量,S-72抑制了耐紫杉醇的MCF-7/T和MX-1/T小鼠异种移植模型中的肿瘤生长。
      • 待估
      35日内发货
      规格
      数量
    • BDW568
      T83901335401-44-0
      BDW568是一种刺激素干扰素基因(STING)的激动剂,同时是BDW-OH的前药形式。在使用THP-1细胞的报告基因测定中,它能诱导STING转录活性(EC50 = 7.6 µM)。BDW568(50 µM)在THP-1细胞中诱导TANK结合激酶1(TBK1)和IFN调节因子3(IRF3)的磷酸化。
      • 待估
      35日内发货
      规格
      数量
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