Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
LCS-1 41931-13-9 Inhibitor inhibitor inhibit