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TargetMol产品目录中 "

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  • 抑制剂&激动剂
    4
    TargetMol | Inhibitors_Agonists
  • 重组蛋白
    1
    TargetMol | Recombinant_Protein
  • JS1310
    PRMT7-IN-1, JS-1310
    T624742247753-73-5
    JS1310 是一种选择性的 PRMT7 抑制剂,对人 PRMT7 的 IC50 为 5 μM。JS1310 对不同癌细胞均表现出抗癌效果。
    • ¥ 10600
    6-8周
    规格
    数量
  • AJS1669
    AJS-1669,AJS 1669
    T265831853130-05-8
    AJS1669, an activator of muscle glycogen synthase, improves glucose metabolism and reduces body fat mass in mice.
    • ¥ 11700
    6-8周
    规格
    数量
  • JS11
    T895651394592-04-1
    JS11 是一种针对利钠多肽受体 1 (Npr1) 的抑制剂,具有对hNpr1 的IC50 值为 1.9 μM.在小鼠模型中,JS11 能有效改善瘙痒症状.
    • 待询
    10-14周
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  • Givinostat
    T36629497833-27-9
    Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 100 and 200 nM, there is no reduction[1]. As shown by the CCK-8 assay, Givinostat (ITF-2357) inhibits JS-1 cell proliferation in a concentration-dependent manner. Treatment with Givinostat ≥500 nM is associated with significant inhibition of JS-1 cell proliferation (P<0.01). Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat ≥250 nM plus LPS and the group without LPS treatment (same Givinostat concentration) (P<0.05)[2]. Givinostat (ITF2357) at 10 mg kg is used as a positive control and, as expected, reduced serum TNFα by 60%. Strikingly, pretreatment of ITF3056 starting at 0.1 mg kg significantly reduces the circulating TNFα by nearly 90%. To achieve a significant increase in serum IL-1β production, a higher dose of LPS is injected (10 mg kg), and blood is collected after 4 h. Similarly, when pretreated with lower doses of Givinostat (ITF-2357) (1 or 5 mg kg), there is a 22% reduction for 1 mg kg and 40% for 5 mg kg[1]. [1]. Li S, et al. Specific inhibition of histone deacetylase 8 reduces gene expression and production of proinflammatory cytokines in vitro and in vivo. J Biol Chem. 2015 Jan 23;290(4):2368-78. [2]. Wang YG, et al. Givinostat inhibition of hepatic stellate cell proliferation and protein acetylation. World J Gastroenterol. 2015 Jul 21;21(27):8326-39. [3]. Leoni F, et al. The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo. Mol Med. 2005 Jan-Dec;11(1-12):1-15.
    • ¥ 447
    5日内发货
    规格
    数量