Month: September 2020

EEDi-5285 is an Orally Active Embryonic Ectoderm Development (EED) Inhibitor

Polycomb protein EED is a member of the Polycomb-group (PcG) family. Specifically, the Polycomb group (PCG) is a class of proteins responsible for cell differentiation during development through transcriptional inhibition. In mammals, PcG protein is part of two major transcriptional inhibition complexes, known as PRC1 and PRC2. Besides, the...

Ilorasertib is an Orally Active ATP-Competitive Multitargeted Kinase Inhibitor

Aurora kinases are key regulators of mitosis that overexpress in many cancer types. Ilorasertib (ABT-348) is a potent inhibitor of all three Aurora kinases, although it has greater activity versus Aurora B and C than Aurora-A. In addition, Ilorasertib also inhibits VEGFRs and PDGFRs, and the Src families of...

SJF620 is a Potent PROTAC BTK Degrader

Bruton’s tyrosine kinase (BTK) is an enzyme encoded by the BTK gene in human. BTK is critical for the survival of B-cell neoplasms. BTK plays a crucial role in B cell development, differentiation, and signaling. Inhibition of BTK kinase activity is an important and practical way of treating Non-Hodgkin’s...

CMLD012073, an Amidino-Rocaglates, is a Potent eIF4A Inhibitor

The eukaryotic translation initiation factors 4A (eIF4A) is crucial for the assembly of the translationally active ribosome. Especially, the eIF4A is an RNA helicase that forms part of the machinery of translation initiation. Small molecules targeting the translation machinery show considerable promise in the treatment of a variety of...

AZD-9833 is an Orally Active Estrogen Receptor (ER) Antagonist

Estrogens participate in numerous physiological processes such as cell growth, reproduction, and differentiation. In females, the ovaries are the major site of estrogen synthesis producing the predominant estrogen 17b-estradiol (E2). In addition to effects by E2 on normal physiology, estrogens also play an important role in several pathological processes...

SP-8356 is a Potent and Orally Active CD147 Inhibitor

Breast cancer is one of the most fatal diseases in women and exhibits high incidence and mortality among various cancers. Among various signaling pathways that promote tumor growth and progression, an inflammatory transcription factor NF-κB plays pivotal roles on cell proliferation and survival. Interestingly, NF-κB is highly activated in...