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.

GT19630 is an orally active c-Myc PROTAC targeted degrader based on the cereblon E3 ubiquitin ligase, with an IC₅₀ of 1.5 nM against human c-Myc. GT19630 mediates the degradation of MYC, GSPT1, GSPT2, CK1 alpha, N-Myc, B7-H3 and XIAP, and disrupts the MYC-GSPT1 synergistic regulatory feedback loop. GT19630 inhibits cell proliferation, blocks S-phase progression of the cell cycle, promotes cell apoptosis, reduces cell migration capacity, induces integrated stress response, and blocks oxidative phosphorylation by inhibiting the TCA cycle. GT19630 can be used in the research of Myc-driven hematological cancers, small cell lung cancer, breast cancer, TP53-mutant cancers, and venetoclax-resistant cancers.

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.