mtor inhibitor 13

mTOR inhibitor 13是一种选择性的mTOR 抑制剂，对mTOR 和PI3Kα的IC50分别为0.29nM 和119nM。

PI3K/mTOR Inhibitor-13 是一种具有口服活性的磷酸肌醇 3-激酶 (PI3K) 和mTOR 激酶双重抑制剂。PI3K/mTOR Inhibitor-13 在性疾病、实体瘤和特发性肺纤维化 (IPF) 中有潜在应用。

mTORinhibitor-26 (Compound HPT-11) 是一种mTOR抑制剂，IC50为0.7 nM。mTORinhibitor-26 有效抑制AML细胞系Molm-13和MV-4-11的增殖。它具有抗肿瘤活性以及良好的代谢稳定性，可能在癌症研究中发挥作用。

MALT1-IN-13 (compound 10m) 是一种黏膜相关淋巴瘤转运蛋白抑制剂，通过与MALT1蛋白酶共价且不可逆结合来抑制其活性，IC50为1.7 μM。此化合物能抑制ABC-DLBCL的增殖并诱导ABC-DLBCL HBL1细胞的凋亡 (apoptosis)，同时调节mTOR和PI3K-Akt通路。

CC-115 是一种双重 mTOR/DNA-PK 的抑制剂，IC50分别为 21 nM 和 13 nM，可阻断mTORC1和mTORC2信号通路。

mTOR inhibitor WYE-28是一种mTOR抑制剂(IC50=0.08 nM)和PI3Kα抑制剂(IC50=6 nM)，在裸鼠微粒体中的半衰期为13分钟。

TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR[1]. TBK1/IKKε-IN-4 (Compound II; 96 hours; A549 andHCC44 cells) treatmentdisplays selective toxicity in TBK1-dependent cancer cell lines (IC50 of ~ 4.2 μM for H441 cells and IC50 of ~0.4 μM for A549 cells)[1].TBK1/IKKε-IN-4 (Compound II; 0-2 μM; 30 minutes; HCC44 cells) treatment inhibits the AKT activity[1].TBK1/IKKε-IN-4 (Compound II) inhibits LPS-induced expression of IFNβ (IC50 =62 nM), and the IFNβ target genes IP10 (IC50 =78 nM) and Mx1 (IC50=20 nM). TBK1/IKKε-IN-4 effectively blocksTLR3-dependent IRF3 nuclear translocation in cells with an IC50 under 100 nM, but does not impair TNFR1-dependent p65 NFκB nuclear translocation with doses as high as 20 μM[1]. [1]. Ou YH, et al. TBK1 directly engages Akt/PKB survival signaling to support oncogenic transformation. Mol Cell. 2011 Feb 18;41(4):458-70.

CC-115 hydrochloride is a potent dual inhibitor of DNA-PK and mTOR kinase, exhibiting IC50 values of 13 nM and 21 nM, respectively. It effectively blocks both mTORC1 and mTORC2 signaling pathways.

Resveratrol-13C6是13C标记的Resveratrol。Resveratrol (trans-Resveratrol; SRT501) 是一种天然多酚，具有抗氧化、抗炎、心脏保护和抗癌特性。它的靶标包括mTOR、JAK、β-amyloid、Adenylyl cyclase、IKKβ、DNA polymerase，并且是SIRT1的特异性活化剂。Resveratrol同样是有效的孕烷X受体 (PXR) 抑制剂和Nrf2激活剂，在小鼠模型中可改善与衰老相关的进行性肾损伤。此外，Resveratrol 作用于内皮细胞促进NO产生。