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LCS-1

LCS-1

产品编号 T60386   CAS 41931-13-9

LCS-1, a superoxide dismutase 1 (SOD1) inhibitor, effectively inhibits the enzymatic activity of SOD1 with an IC50 value of 1.07 μM. Additionally, LCS-1 triggers both early and late-stage apoptosis in multiple myeloma (MM.1S) cells [1] [2] [3].

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LCS-1 Chemical Structure
LCS-1, CAS 41931-13-9
规格 价格/CNY 货期 数量
2 mg ¥ 249 5日内发货
1 mL * 10 mM (in DMSO) ¥ 477 5日内发货
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: LCS-1 (T60386)
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产品描述 LCS-1, a superoxide dismutase 1 (SOD1) inhibitor, effectively inhibits the enzymatic activity of SOD1 with an IC50 value of 1.07 μM. Additionally, LCS-1 triggers both early and late-stage apoptosis in multiple myeloma (MM.1S) cells [1] [2] [3].
体外活性 LCS-1 (1-10000 nM; 24 hours) is selective cytotoxic to both bloom syndrome gene product (BLM) -proficient and BLM-deficient HCT116 cells [1]. LCS-1 shows growth inhibitory effect on 10/27 adenocarcinoma cell lines (median IC 50 =0.20 μM; such as H23, H2347, HCC827 cell lines) and normal human bronchial epithelial (NHBE) cells (IC 50 =2.66 μM) [2]. 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 [3]. 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 [3]. LCS-1 (48 h) has IC 50 values of 2.5 and 4.6 μM for cell viability of ANBL6-WT (Bortezomib-sensitive) and ANBL6-BR (Bortezomib- resistant) cells, respectively [3]. LCS-1 (1.25 μM; 16 h) induces a significant increase in ROS levels and O 2 levels in MM.1S cells [3]. LCS-1 (1.25 μM; 16 h) shows a significant decrease in GSH/GSSG ratio in MM.1S cells [3]. 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 [3]. LCS-1-induced O 2 (1.25 μM; 5 h) triggers a marked decrease in both RP 2 CP and RP 1 CP forms of 26S proteasomes [3]. LCS-1 (2 μM; 16 h) induces the early- and late-stage apoptosis of MM.1S cells [3]. 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 [3]. 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 [3]. Cell Viability Assay [1] Cell Line: BLM-proficient and BLM-deficient HCT116 cells Concentration: 1-10000 nM Incubation Time: 24 hours Result: Had IC 50 values of 1462 nM and 24.92 nM for the viability of BLM-proficient and BLM-deficient HCT116 cells, respectively. Western Blot Analysis [3] Cell Line: MM.1S and ANBL6-BR cells Concentration: 2 μM Incubation Time: 16 hours Result: Decreased the expression of cell-cycle regulatory proteins (cyclin-B1, CDC25C, and CDC2). Western Blot Analysis [3] Cell Line: MM.1S cells Concentration: 0, 0.5, 1, 1.5, 2 μM Incubation Time: Result: Upregulated p53/p21 signaling, as well as downregulated survival pathway proteins MCL-1, BclxL, or c-Myc. Western Blot Analysis [3] Cell Line: MM.1S cells Concentration: 2 μM Incubation Time: 0, 4, 8, 16, 24 hours Result: Showed a rapid and robust induction of UPR proteins (BIP, PERK, phosphorylated eIF2α, or a lectin protein calnexin).
体内活性 LCS-1 (20 mg/kg; i.p. every other day for 14 days) inhibits the growth of MM and prolongs host survival in MM.1S-bearing mice [3]. Animal Model: 5-week-old female CB17 SCID mice (MM.1S tumors volume=100 mm 3 ) [3] Dosage: 20 mg/kg (diluted in saline) Administration: Intraperitoneal injections; treated on an every other day schedule for 14 days Result: Inhibited MM growth and prolongs host survival.
分子量 255.1
分子式 C11H8Cl2N2O
CAS No. 41931-13-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

LCS-1 41931-13-9 Inhibitor inhibitor inhibit

 

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