Casein Kinase Degrader

SJ3149 is a selective and potent molecular glue degrader of CK1α protein with broad antiproliferative activity. SJ3149 can be used in cancer research.

DEG-77 is a molecular glue targeting IKZF2 and CK1α, with DC₅₀ values of 15.3 nM and 10 nM, respectively. DEG-77 exhibits significant anti-tumor activity, inducing increased transcriptional levels of the pro-apoptotic protein Bax and the cell cycle arrest protein p21. DEG-77 is applicable to the research of acute myeloid leukemia (AmL), diffuse large B-cell lymphoma and ovarian cancer.

PROTAC c-Myc degrader-1 (Compound A153) is a multiple target protein degrader (PROTAC). PROTAC c-Myc degrader-1 effective degrades c-MYC, CK1α, GSPT1 and IKZF1/2/3 proteins in a variety of tumor cells. PROTAC c-Myc degrader-1 can be used for c-Myc high expression related disease research, such as cancer, cardiovascular and cerebrovascular diseases, and viral infection.

Sontigidomide is a protein degrader that can effectively degrade IKAROS and GSPT1 proteins.. Sontigidomide can be used to study inflammatory and immune system diseases.

DEG-35 is a CRBN-dependent, dual IKZF2 and CK1α molecule glue degrader, with DC₅₀ values of 1.4 nM and 4.4 nM for CK1α and IKZF2, respectively. DEG-35 activates the p53 apoptosis pathway. DEG-35 can be used in the research for Acute Myeloid Leukemia (AML).

MGD-28 is a potent, orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC₅₀=3.8 nM), IKZF2 (DC₅₀=56.3 nM), and IKZF3 (DC₅₀=7.1 nM) in a dose-dependent manner. In addition, MGD-4 also degrades CK1α (DC₅₀=7.8 nM). MGD-28 has antiproliferative activity and can be used in multiple myeloma research.

dCK1α-2 is an orally active CK1α molecular glue degrader that targets p53 pathway-related targets. dCK1α-2 exhibits anti-tumor efficacy in mouse models and can increase the expression of p53-related genes..

WH-10417-099 is a CRBN-based PROTAC multi-kinase degrader that induces the degradation of the maximum number of unique kinases (over 125 unique kinases, such as CSNK1E and PI3Kγ) simultaneously. WH-10417-099 induces protein degradation via the ubiquitin biotinylation (E-STUB) pathway, exhibits synergistic effects with SB-405483 (HY-W1135319). The E3 ligase ligand and linker of WH-10417-099 can form the conjugate Pomalidomide 4'-PEG5-acid (HY-131647).

CK1α degrader-1 (Compound 82) is an orally active CK1α degrader with a DC₅₀ of 0.105 μM. CK1α degrader-1 can be used for the research of cancer.

(R,R)-BMS-986397 is a CK1α degrader (DC₅₀ between 0.1-0.5 pM). (R,R)-BMS-986397 can be used in anti-leukemia research.

IBA-11 is a selective CRBN-dependented CK1α molecular glue degrader. IBA-11 binds to the canonical tri-tryptophan pocket of CRBN, forming a ternary complex with CK1α to mediate its degradation. IBA-11 induces CRBN-dependent ubiquitin-proteasome system-mediated degradation of CK1α. IBA-11 exhibits cytotoxicity against cancer cells. IBA-11 demonstrates in vitro metabolic stability in rat liver microsomes and minimal hERG inhibition. IBA-11 can be used for the research of cancer, such as acute myeloid leukemia.

MI-2-80 is a molecular glue degrader. MI-2-80 induces proteins (such as IKZF1/3 and CSNK1A1) to bind to CRBN, promoting their ubiquitination and degradation.