Month: September 2020

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...

PU02 is an Allosteric Antagonist of 5-HT3 Receptor

Cancer is a usual disease and a leading cause of death in the world. Therefore, developing new agents specifically targeting cancer cells has achieved more and more researches. As it is widely believed that cancer can be treated by inducing tumor cells to undergo senescence or apoptosis, screening for...

SC99 is an Orally Active and Selective STAT3 Inhibitor

STAT3 is a member of the STAT protein family. STAT3 mediates the expression of a variety of genes in response to cell stimulation. So it plays a key role in many cell processes, such as cell growth and apoptosis. Specifically, the oncogenic STAT3 signaling pathway is becoming a promising...

MPT0G211 is an Orally Active and Selective HDAC6 Inhibitor

Alzheimer’s disease (AD) is one of the most common neurodegenerative diseases, accounting for more than 80% of dementia cases worldwide. AD leads to the progressive loss of mental capacity and behavior, with a functional decline in the ability to learn. HDAC6 belongs to the HDAC family, and its structure contains...

MSA-2 is an Orally Available STING Agonist with Anti-tumor Activity

Stimulator of interferons genes (STING) is an adaptor protein. It plays a critical role in the secretion of type I interferons and pro-inflammatory cytokines in response to cytosolic nucleic acid. STING is also an endoplasmic reticulum-associated homodimeric protein. It is the receptor for cGAMP. The cGAMP is a second...

EPI-001 is a Selective Inhibitor of Androgen Receptor with Anti-tumor Activity

The androgen receptor (AR) is a type of nuclear receptor and a modular steroid hormone receptor transcription factor. Specifically, the androgen receptor is activated by binding any of the androgenic hormones then translocating into the nucleus. Besides, the main function of the androgen receptor is to regulate gene expression...