Category: Lymphoma

DS-437 is a Dual PRMT5/7 Inhibitor

Protein arginine methyltransferases are a class of enzymes. They transfer a methyl group from the cofactor S-adenosylmethionine (SAM) onto the arginine omega nitrogens of substrate proteins, including histones. There are three subclasses based on their product specificity: type I, II, and III PRMTs asymmetrically dimethylate, symmetrically dimethylate, and monomethylate their...

SB-218078 is an ATP Competitive and Reversible Chk1 Inhibitor

Research from Jeffrey R. Jackson, et al. discovered and identified an indolocarbazole inhibitor of human checkpoint Kinase (Chk1) SB-218078. SB-218078 is an ATP Competitive and Reversible Chk1 Inhibitor The regulation of cell cycle checkpoints is a critical determinant of the manner in which tumor cells in response to chemotherapies...

CKI-7 is a Dual CK1 and Cdc7 Kinase Inhibitor

Protein phosphorylation plays a fundamental role in the regulation of a variety of cellular processes. Casein kinase I (CK1) is a cyclic nucleotide independent kinase. It is highly purified from various tissues, including calf thymus, rabbit reticulocytes, liver, and skeletal muscle. The widespread distribution of CK1 suggests its importance...

CA-4948 is a Selective and Orally Bioavailable IRAK4 Kinase Inhibitor for Lymphoma Treatment

Interleukin-1 receptor-associated kinase 4 (IRAK4) is the most upstream kinase in Toll/Interleukin-1 receptor (TIR) signaling. Toll-like receptor (TLR) and interleukin-1 receptor (IL-1R) signaling in a variety of myeloid and lymphoid cell types require IRAK4 kinase activity. The MYD88 adaptor protein facilitates the recruitment of IRAK4 to these receptors and...

SI-109, a STAT3 Transcription Inhibitor, is the Ligand of PROTAC Degrader SD-36

As we have written in the article “SD-36 is a Selective PROTAC STAT3 Degrader”, proteolysis targeting chimera (PROTAC) technology has been a type of therapeutics that induces targeted protein degradation. Signal transducer and activator of transcription 3 (STAT3) is an attractive cancer therapeutic target. Longchuan Bai, et al have...

SD-36 is a Selective PROTAC STAT3 Degrader

Proteolysis targeting chimera (PROTAC) technology has been a type of therapeutics that induces targeted protein degradation. Signal transducer and activator of transcription 3 (STAT3) is an attractive cancer therapeutic target. In this study, Longchuan Bai, et al developed a potent and specific PROTAC degrader of STAT3 and evaluate its...

sAJM-589 is a Myc Inhibitor by Disrupts the Myc-Max Heterodimer

The proto-oncogene Myc belongs to the basic helix-loop-helix leucine zipper (B-HLH-LZ) transcription factor family. It plays a key role in cellular proliferation, differentiation, and apoptosis. Myc expression is normally under tight control. Its expression is transient and responsive to mitogen stimulation. Indeed, in more than 70% of human malignancies,...