BSc2118

BSc2118 is a 20S proteasome inhibitor with an IC₅₀ of approximately 50 nM. BSc2118 induces G₂/M phase cell cycle arrest and apoptosis in myeloma cells, inhibits cytoprotective autophagy, and suppresses tumor angiogenesis. BSc2118 reduces MMP9 activity, promotes angioneurogenesis, and alleviates recombinant tissue-type plasminogen activator-induced cerebral toxicity. BSc2118 is applicable to studies related to cerebral ischemia and multiple myeloma^[1][2]. In Vitro:BSc2118 (0-2000 nM; 48 h) potently reduces the cell viability of human multiple myeloma cell lines MM.1S, MM.1R, RPMI-8226, U266 and NCI-H929 in a dose-dependent manner, with IC₅₀ values of 121.4 nM, 116.8 nM and 313.7 nM in MM.1S, MM.1R and RPMI-8226 cells, respectively^[2].
BSc2118 (100-200 nM; 24 h) induces G2/M cell cycle arrest in the human multiple myeloma cell line MM.1S^[2].
BSc2118 (100-200 nM; 24 h) induces dose-dependent apoptosis in MM.1S and MM.1R human multiple myeloma cells^[2].
BSc2118 (100-200 nM; 24 h) upregulates the protein levels of p53 and p21 in MM.1S human multiple myeloma cells^[2].
BSc2118 (100-200 nM; 24 h) activates the apoptotic signaling cascade in MM.1S and MM.1R human multiple myeloma cells by cleaving caspase-9, caspase-8, caspase-3 and PARP^[2].
BSc2118 (100-200 nM; 3-24 h) potently and persistently inhibits CT-L proteasome activity in MM.1S human multiple myeloma cells^[2].
BSc2118 (100-200 nM; 3-24 h) induces the accumulation of ubiquitinated proteins in human multiple myeloma cells MM.1S^[2].
BSc2118 (200 nM; 30 h) inhibits capillary-like tube formation in human umbilical vein endothelial cells (HUVECs)^[2].
BSc2118 (100-200 nM; 24 h) upregulates the protein level of PHD2 and downregulates the protein levels of HIF1α and VE-cadherin in human umbilical vein endothelial cells (HUVECs)^[2].
BSc2118 (100-200 nM; 48 h) downregulates the expression of angiogenic cytokine genes including IL-6, VEGFA and bFGF in human MM-BMSCs in a dose-dependent manner^[2].
BSc2118 (100-500 nM; 24 h) does not induce upregulation of the autophagy markers Beclin-1 or LC3b; instead, it slightly reduces LC3b levels in both Bortezomib (HY-10227)-sensitive ANBL-6.WT and Bortezomib-resistant ANBL-6.BR human multiple myeloma cells^[2]. In Vivo:BSc2118 (10-60 mg/kg; intrastriatal injection; single dose) exerts acute and long-term neuroprotective effects against reperfusion-induced cerebral ischemia in male C57BL/6N mice, and improves long-term neuronal survival, functional recovery, angioneurogenesis and blood-brain barrier stability^[1].
BSc2118 (30 mg/kg; i.p.; twice weekly for 3 consecutive weeks) reduces tumor volume by 61.5% in a multiple myeloma NOD/SCID mouse model, inhibits tumor angiogenesis and decreases basal autophagy levels, with no hematological toxicity observed^[2].