D4476, a cell‐permeant inhibitor of CK1, suppresses the …
WEBJan 1, 2004 — D4476 is the most useful CK1 inhibitor available and should facilitate the identification of its physiological substrates. Results and Discussion. Structure and specificity of D4476.
Oocyte Casein kinase 1α deletion causes defects in primordial …
WEBSep 17, 2022 — The oocyte-specific CK1α knockout (cKO) mouse model was then established by crossing Ddx4-Cre mice with Csnk1a1-floxp mice, and the effects of CK1α deletion on oogenesis and...
Casein Kinase-1-Alpha Inhibitor (D4476) Sensitizes Microsatellite ...
WEBSep 18, 2021 — Our findings showed that combination treatment with 5-FU and D4476 inhibited autophagy flux. Moreover, 5-FU and D4476 combination therapy induced G2, S and G1 phase arrests and it depleted mRNA of both cell proliferation-related genes and MDR-related genes ( ABCG2, cyclin D1 and c-myc).
Casein kinase 1α: biological mechanisms and theranostic potential
WEBMay 24, 2018 — Treatment with the CK1 inhibitor D4476 or short interfering RNA siRNA-mediated knockdown of CK1α results in nuclear accumulation of FOXO3A and increased expression of autophagy-related genes. CK1α protein abundance is regulated by PI3K/mTOR signaling induced by activated or oncogenic/mutant RAS .
Selective CK1α degraders exert antiproliferative activity against a ...
WEBJan 16, 2024 — Pharmacologic inhibition of CK1α using D4476, a pan-CK1 inhibitor, or CK1α knockdown via lentivirus-mediated shRNA, suppressed proliferation and clone formation by enhancing autophagic flux and...
CK1α Plays a Central Role in Mediating MDM2 Control of p53 and …
WEBAlthough the treatment of cells with D4476 resulted in a partial p53-dependent growth arrest, the induction of p53-independent apoptosis by D4476 suggested a critical role for the MDM2·CK1 complex in maintaining E2F-1 anti-apoptotic signaling.
D4476 | STEMCELL Technologies
WEB· Reprograms mouse somatic cells into pluripotent cells by acting as a chemical substitute for OCT4 (Hou et al.). CANCER RESEARCH · Induces apoptosis of multiple myeloma cell lines (Hu et al.).
Regulation of Ribosomal Protein S6 Phosphorylation by Casein …
WEBCK1 inhibition with D4476 or siRNA knockdown strongly suppressed serum-dependent phosphorylation of rpS6 on Ser-247, which is a consensus CK1 site. CK1 phosphorylated Ser-247 in vitro , consistent with a direct role for CK1 in rpS6 phospho-regulation.
Casein kinase I inhibitor D4476 influences autophagy and …
WEBMay 1, 2022 — The strong cell-permeant CK1 inhibitor D4476 (4- (4- (2,3-dihydrobenzo [1,4] dioxin-6-yl)-5-pyridin-2-yl-1H-imidazole-2-yl) benzamide) selectively targets CK1 isoforms, specifically CK1α/CK1δ, which are involved in upregulating the mRNA of autophagic genes (Carrino et al., 2019).
Knockdown of Csnk1a1 results in preimplantation developmental …
WEBMar 1, 2023 — Furthermore, treatment of zygotes with the CSNK1A1-specific inhibitor D4476 also resulted in embryonic developmental arrest. These results provide the first evidence for a novel function of CSNK1A1 in early embryonic development in mice.