growth-regulated a protein

DL-threo dihydrosphingosine is a cell-permeable inhibitor of the extracellular signal-regulated kinase (ERK) signalling cassette in mammalian cells. DL-threo dihydrosphingosine is effective against both growth factor- and G-protein-dependent activation of

Methylnissolin 是从黄芪中分离的一种天然产物，可抑制血小板衍生生长因子 (PDGF)-BB 诱导的细胞增殖，IC50为 10 μM。。它通过抑制ERK1 2MAP 激酶级联反应抑制 PDGF-BB 诱导的血管平滑肌细胞增殖。它还抑制 PDGF-BB 诱导的细胞外信号调节激酶 1 2 (ERIC1 2) 丝裂原活化蛋白 (MAP) 激酶的磷酸化，具有抗菌和抗癌作用。

WR-S-462 是一种STAT3抑制剂，在体外能有效地阻碍STAT3的磷酸化及其生物学功能。该化合物对MDA-MB-231细胞的IC50为0.03 μM，并表现出对STAT3蛋白的强结合亲和力，其Kd为58 nM。WR-S-462 能抑制p-STAT3的核转位，特异性抑制MDA-MB-231细胞中p-STAT3Tyr705的表达，以及由STAT3调控的下游靶基因如Cyclin D1、Bcl-2和Bcl-xl的表达。此外，WR-S-462 有效抑制三阴性乳腺癌 (TNBC) 的生长和转移。

M-525 binds to menin (IC50: 3 nM) and achieves low nanomolar potencies in cell growth inhibition and in the suppression of MLL regulated gene expression in MLL leukemia cells. M-525 is a first-in-class, highly potent, irreversible, and covalent menin-MLL

ARD-2128 是高效的雄激素受体降解剂 PROTAC。它可有效降低 雄激素受体蛋白并抑制肿瘤组织中雄激素受体调节的基因，在没有毒性迹象的情况下抑制肿瘤生长。它有用于前列腺癌研究的价值。

KRH102053 is a HIF-1alpha inhibitor. KRH102053 decreased the protein level of HIF-1alpha and the mRNA levels of HIF-regulated downstream target genes, such as vascular endothelial growth factor, aldolase A, enolase 1 and monocarboxylate transporter 4. Consistent with these results, KRH102053 also inhibited the rates of HIF-related migration and invasion of HOS cells as well as the degree of tube formation in human umbilical vein endothelium cells.