Category: Multiple Myeloma

LBW242 is a Potent and Orally Active Proapoptotic IAP Inhibitor

Acute myelogenous leukemia (AML) is a hematologic malignancy. The characteristics include a block in cellular differentiation and aberrant growth of myeloid precursor cells. Approximately 30% of AML patients and a portion of acute lymphoblastic leukemia (ALL) patients express a mutated form of the class III receptor tyrosine kinase, FLT3....

E64FC26 is a pan-Inhibitor of the Protein Disulfide Isomerase (PDI) Family

Multiple myeloma (MM) is an incurable hematological malignancy. MM results in the accumulation of clonal plasma cells within the bone marrow. The natural biology of the plasma cell makes MM uniquely sensitive to disruptions in protein homeostasis. Subsequently, it proposes targeting protein folding as a strategy for the treatment...

AMG 232 is an Orally Active and Best-in-Class MDM2-p53 Inhibitor

The p53 tumor suppressor induces cell growth arrest and apoptosis in response to DNA damage or stress. And inactivation of the p53 pathway plays an indispensable role in tumor survival. Approximately p53 mutations resulting in loss of its function account for 50% human cancers. And the wild-type p53, present...

CP-10 is a Specific PROTAC Degrader of CDK6

CDK6 plays a significant role in cell cycle entrance. However, overexpression of CDK6 correlates to CDK4/6 inhibitor resistance in breast cancer cell lines and patient samples. Moreover, point mutation of CDK6 could possibly result in attenuation of drug binding affinity or hyperactivation of CDK6. Thus, there is an urgent...

BAY1238097 is a Selective Inhibitor of BET Binding to Histones

Several BET inhibitors with strong anti-tumor efficacy have been described in recent years. Most of them are derived from diazepine and azepine scaffolds, besides, more recently quinazolinones and isoxazoles chemotypes have been identified. Additionally, a study from Pascale Lejeune identified and verified a novel BET inhibitor BAY1238097, which shows...

GNE-955 is a Potent Pan-Pim Inhibitor for Multiple Myeloma and Leukemia Research

Leukemia is a group of blood cancers, such as acute leukemia, as we mentioned in our previous blog “BSc5371, an Irreversible FLT3 Inhibitor for Acute Leukemia Treatment”. Multiple myeloma is a cancer of plasma cells, called plasma cell myeloma. Such diseases severely affect patients’ lives. What is worse, they...