Seliciclib (Roscovitine) is an Orally Active and Selective CDKs Inhibitor
Cyclin-dependent kinases (CDKs) are serine/threonine kinases whose activity depends on a regulatory subunit-a cyclin. Based on the sequence of the kinase domain, CDKs belong to the CMGC group of kinases, along with MAPKs, Gsk3β, DYRK family and CDK-like kinases. There are around 20 Cyclin-dependent kinases (CDK1-20) known till date....
IMD-0354 is a Selective IKKβ Inhibitor
IKKβ is an enzyme that is part of an intracellular signaling pathway activated by cytokines involved in triggering an immune response. Particularly, Phosphorylated IκB degrades and releases NF-κB through the ubiquitination pathway. Importantly, it enters the nucleus and participates in a variety of genes in inflammation and other immune...
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...