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LCS-1

CAS No. : 41931-13-9

MCE 国际站：LCS-1

产品活性：LCS-1 是一种超氧化物歧化酶 1 (SOD1) 抑制剂。LCS-1 抑制 SOD1 活性，IC₅₀ 值为 1.07 μM。LCS-1 诱导多发性骨髓瘤细胞 (MM.1S) 的早期和晚期凋亡(apoptosis)。

研究领域：Apoptosis  |  Immunology/Inflammation

作用靶点：Apoptosis  |  SOD

In Vitro: LCS-1 (1-10000 nM; 24 hours) has selective cytotoxicity towards bloom syndrome gene product (BLM) -proficient and BLM-deficient HCT116 cells.
LCS-1 shows growth inhibitory effect on 10/27 adenocarcinoma cell lines (median IC₅₀=0.20 μM; such as H23, H2347, HCC827 cell lines) and normal human bronchial epithelial (NHBE) cells (IC₅₀=2.66 μM).
LCS-1 (0, 1.25, 2 μM; 4 h) in a concentration-dependent manner triggers significant inhibition of SOD1 enzymatic activity in multiple myeloma (MM) cells.
LCS-1 (0, 1.25, 2.5, 5 μM; 48 h) in a dose-dependent manner reduces the viability of various MM cell lines, including MM.1R (Dexamethasone-resistant), Dox40 (Doxorubicin-resistant), or LR5 (Melphalan-resistant) cell lines.
LCS-1 (48 h) has IC₅₀ values of 2.5 and 4.6 μM for cell viability of ANBL6-WT (Bortezomib-sensitive) and ANBL6-BR (Bortezomib- resistant) cells, respectively.
LCS-1 (1.25 μM; 16 h) induces a significant increase in ROS levels and O₂ levels in MM.1S cells.
LCS-1 (1.25 μM; 16 h) shows a significant decrease in GSH/GSSG ratio in MM.1S cells.
LCS-1 (1.25 μM; 24h) induces the release of mitochondrial cytochrome-c into the cytosol, and enriches the proteins (HSP60/CLPP) mediating mtUPR signaling in MM.1S cells.
LCS-1-induced O₂ (1.25 μM; 5 h) triggers a marked decrease in both RP₂CP and RP₁CP forms of 26S proteasomes.
LCS-1 (2 μM; 16 h) induces the early- and late-stage apoptosis of MM.1S cells.
LCS-1 (0, 0.5, 1, 1.5, 2 μM) upregulates p53/p21 signaling, as well as downregulates survival pathway proteins MCL-1, BclxL, or c-Myc in MM.1S cells.
LCS-1 (0, 4, 8, 16, 24 h; 2 μM) shows a rapid and robust induction of mitochondrial unfolded protein response (UPR) proteins (BIP, PERK, phosphorylated eIF2α, or a lectin protein calnexin) in MM.1S and ANBL6-BR cells.

In Vivo: LCS-1 (20 mg/kg; i.p. every other day for 14 days) inhibits MM growth and prolongs host survival in MM.1S-bearing mice.

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