Apoptosis Inducer
Apoptosis inducing factor is involved in initiating a caspase-independent pathway of apoptosis by causing DNA fragmentation and chromatin condensation. It also acts as an NADH oxidase. Another AIF function is to regulate the permeability of the mitochondrial membrane upon apoptosis. Normally it is found behind the outer membrane of the mitochondria and is therefore secluded from the nucleus. However, when the mitochondrion is damaged, it moves to the cytosol and to the nucleus. Inactivation of AIF leads to resistance of embryonic stem cells to death following the withdrawal of growth factors indicating that it is involved in apoptosis.
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Pemrametostat (GSK3326595, EPZ015938)是一种具有口服活性的、有效的、选择性protein arginine methyltransferase 5 (PRMT5)抑制剂，在体内外有效地抑制肿瘤生长。
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Inavolisib (GDC-0077, RG6114, RO-7113755) 是一种有效的 PI3K alpha (PI3Kα) 选择性抑制剂，IC50 为 0.038 nM。GDC-0077 对 PI3K α 的选择性比其他 I 类 PI3K 异构体（β、δ 和 γ）高 300 倍以上，对 PIK 家族成员的选择性高 2000 倍以上。GDC-0077 可与 PI3K 的 ATP 结合位点结合并抑制 PIP2 磷酸化为 PIP3
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KT-474 (SAR444656) 是一种IRAK4的选择性小分子降解剂，正在开发用于治疗 TLR/IL-1R 驱动的自身免疫性疾病。 KT-474 有效下调 R848 (TLR7/8) 和脂多糖 (LPS) 诱导的外周血单核细胞 (PBMC) 中 IL-6 和 IL-8 的产生
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Emavusertib (CA-4948) 是一种有效的、口服生物可利用的 interleukin-1 receptor-associated kinase 4/FMS-like Tyrosine Kinase 3 (IRAK4/FLT3) 的抑制剂，具有抗肿瘤活性
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Deguelin是抗癌和抗病毒试剂，促进细胞凋亡。
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