Tag: Cell-cycle

AC-4-130 is a Potent STAT5 SH2 Domain Inhibitor

Signal transducer and activator of transcription 5 (STAT5) is a member of the STAT protein family. It is relevant to cell growth and differentiation. Specifically, STAT5 protein has related to cytoplasmic signal transduction and mediates the expression of specific genes. Abnormal STAT5 activity is closely related to a variety...

Rosabulin is a Potent Microtubule Inhibitor

Chemotherapy is a cornerstone in the development of present-day cancer therapy. Moreover, Chemotherapy is one of the most effective and potent strategies to treat malignant tumors. However, Chemotherapy resistance occurs when cancers that have been responding to therapy suddenly begin to grow. Rosabulin is a potent tubulin inhibitor. In...

UZH1a is a Selective METTL3 Inhibitor

METTL3/14 plays a critical role in disorders associated with abnormal self-renewal, aberrant proliferation, and blocking differentiation of hematopoietic cells. Both METTL3 and METTL14 are upregulated in all subtypes of AML, despite the heterogeneity of this blood cell cancer in terms of chromosomal rearrangement and gene mutations. AML and B-cell...

NU6102 is a Potent CDK1 and CDK2 Inhibitor

CDKs remain attractive targets for anti-proliferative cancer chemotherapy. they play a central role in cell division and growth.  Amongst the cell cycle CDKs, CDK2 has attracted the most attention and its exploitation as a drug target based on structure-based drug design. In this article, we will introduce a potent...

Afatinib is an Irreversible and Orally Active EGFR Family Inhibitor

Lung cancer continues to be the leading cause of cancer-related mortality. Members of the ERBB receptor tyrosine kinase family include EGFR, HER2, HER3, and HER4. They present an attractive option for targeted therapy in patients with NSCLC, due to observed patterns of oncogenic mutation of EGFR and HER2. In addition, esophageal...

HJC0416 is a Highly Potent and Orally Active STAT3 Inhibitor

Signal transducer and activator of transcription 3 (STAT3) is involved in the regulation of early embryonic development, angiogenesis, immune response, cell proliferation, and apoptosis. Additionally, STAT3 overexpresses in many cancers. As a result, it becomes an attractive therapeutic target for various cancer treatment studies. However, despite much intensive researches...

ZINC69391 is a Specific Rac1 Inhibitor and Apoptosis Inducer

Rho-GTPases are molecular switches that cycle between an inactive GDP-bound form and an active GTP-bound form. Guanine nucleotide exchange factors (GEFs) catalyze nucleotide exchange and mediate activation in this cycle, While GTPase-activating proteins (GAPs) stimulate GTP hydrolysis and inactivate the GTPase. Only the active GTP-bound state binds to downstream...