sk-33

SK33 是一种有效的组织选择性抗雄激素药物，是一种肌醇类似物，能够降低雄激素受体 (AR) 的转录活性。

GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.

GSK3326595 (EPZ015938) 是一种选择性可逆的蛋白精氨酸甲基转移酶 5 抑制剂，IC50为6.2 nM，具有广谱的抗增殖活性。

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) 是一种具有口服活性和高效性的 I 型蛋白精氨酸甲基转移酶 (PRMTs) 抑制剂 ，具有抗癌和抗肿瘤活性，抑制PRMT1，PRMT3，PRMT4，PRMT6，PRMT8的活性，可用于研究晚期实体肿瘤。

GSK3395879 is a selective and orally bioavailable antagonist of transient receptor potential vanilloid-4 (TRPV4) (IC50: 1 nM for hTRPV4).

GSK3335103，一种非肽类αvβ6整合素抑制剂，具备口服活性，其pIC50值为8，主要应用于肺纤维化的研究领域。

GSK3368715, a potent inhibitor of type I protein arginine methyltransferases (PRMT), could inhibit PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM.

GSK334429 is an antagonist of histamine H3 receptor.

EZM 2302 (GSK3359088) 是选择性口服精氨酸甲基转移酶 CARM1 抑制剂，IC50值为 6 nM。[1]

Tomivosertib, also known as eFT508 is a MNK1 2 inhibitor. Tomivosertib binds to and inhibits the activity of MNK1 and 2. This prevents MNK1 2-mediated signaling, and inhibits the phosphorylation of certain regulatory proteins, including eukaryotic translation initiation factor 4E (eIF4E), that regulate the translation of messenger RNAs (mRNAs) involved in tumor cell proliferation, angiogenesis, survival and immune signaling.

Feladilimab (GSK3359609) 是一种 IgG4 单克隆抗体,是一种 ICOS 激动剂。Feladilimab 与表达 ICOS 的 T 细胞结合，诱导 IFNγ，增加 PD-1/L1 表达。Feladilimab 具有抗肿瘤活性，可用于研究癌症。

GSK3368715, a first-in-class, orally active, potent, and selective SAM-noncompetitive inhibitor of Type I Protein Arginine Methyltransferases (PRMTs), exhibits anti-tumor efficacy across multiple cancer models and alters exon usage with IC50 values in the lower nM range. It synergizes with GSK3326595 (Type II inhibitor) (Axon 3750) to inhibit tumor growth.

(-)-Epigallocatechin Gallate (EGCG) 属于茶类黄酮天然产物，可抑制 EGFR 信号传导，抑制 GLUD 1/2。(-)-Epigallocatechin Gallate 具有抗氧化、抗炎和抗肿瘤活性。(-)-Epigallocatechin Gallate 可以通过激活细胞色素 c 氧化酶来诱导氧化磷酸化。

Isoliquiritigenin (ISL) 属于黄酮类天然产物，抑制流感病毒复制 (EC50=24.7 μM)，也抑制 aldose reductase 的活性 (IC50=320 nM)。Isoliquiritigenin 具有抗肿瘤的活性。