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CAS No. : 1009820-21-6
MCE 国际站:Silmitasertib
产品活性:Silmitasertib (CX-4945) 是一种有效、可口服、高度选择性的 CK2 抑制剂,对 CK2α 和 CK2α' 的 IC50值均为 1 nM。
研究领域:Cell Cycle/DNA Damage | Stem Cell/Wnt | Autophagy
作用靶点:Casein Kinase | Autophagy
In Vitro: Silmitasertib (CX-4945) causes cell-cycle arrest and selectively induces apoptosis in cancer cells relative to normal cells, attenuates PI3K/Akt signalingand, and the antiproliferative activity of Silmitasertib (CX-4945) is correlated with expression levels of the CK2α catalytic subunit, Attenuation of PI3K/Akt signaling. Silmitasertib (CX-4945) with PS-341 treatment prevents leukemic cells from engaging a functional UPR in order to buffer the PS-341-mediated proteotoxic stress in ER lumen, and decreases pro-survival ER chaperon BIP/Grp78 expression. Silmitasertib (CX-4945) induces cytotoxicity and apoptosis, and exerts anti-proliferative effects in hematological tumors by downregulating CK2 expression and suppressing activation of CK2-mediated PI3K/Akt/mTOR signaling pathways.
In Vivo: Silmitasertib (CX-4945) (25 or 75 mg/kg, p.o.) is well tolerated and demonstrated robust antitumor activity with concomitant reductions of the mechanism-based biomarker phospho-p21 (T145) in murine xenograft models.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Stem Cell Signaling Compound Library | Wnt/Hedgehog/Notch Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Antiviral Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Endoplasmic Reticulum Stress Compound Library | Orally Active Compound Library | Targeted Diversity Library | Rare Diseases Drug Library | Human Metabolite Library | Non-steroidal Anti-Inflammatory Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | Highly Selective Activators Library | CK2-IN-4 | Umbralisib hydrochloride | 4,5,6,7-Tetrabromo-1H-benzimidazole | JNJ-6204 | CK2-IN-1 | PF-5006739 | TA-01 | Ellagic acid | EGFR-IN-57 | AMG-548 hydrochloride | CKI-7 free base | SR-1277 | CK2α-IN-1 | NCC007 | Emodin-d4 | Casein Kinase II Inhibitor IV | TMX-4113 | BTX161 | D4476 | Casein Kinase II Receptor Peptide | PI-828 | TBCA | CK2 inhibitor 2 | TTP 22 | Longdaysin | CK2/ERK8-IN-1 | TMCB | Silmitasertib sodium salt
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