LCS-1

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LCS-1  纯度: 99.11%

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)。

LCS-1

LCS-1 Chemical Structure

CAS No. : 41931-13-9

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LCS-1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Endoplasmic Reticulum Stress Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

LCS-1 is a superoxide dismutase 1 (SOD1) inhibitor. LCS-1 inhibits SOD1 activity with an IC50 value of 1.07 μM. LCS-1 induces the early- and late-stage apoptosis of multiple myeloma (MM.1S) cells[1][2][3].

IC50 & Target[2]

SOD1

1.07 μM (IC50)

体外研究
(In Vitro)

LCS-1 (1-10000 nM; 24 hours) has selective cytotoxicity towards 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 IC50=0.20 μM; such as H23, H2347, HCC827 cell lines) and normal human bronchial epithelial (NHBE) cells (IC50=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 IC50 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 O2 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 O2 (1.25 μM; 5 h) triggers a marked decrease in both RP2CP and RP1CP 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: BLM-proficient and BLM-deficient HCT116 cells
Concentration: 1-10000 nM
Incubation Time: 24 hours
Result: Had IC50 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).

体内研究
(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[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 5-week-old female CB17 SCID mice (MM.1S tumors volume=100 mm3)[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

255.10

Formula

C11H8Cl2N2O

CAS 号

41931-13-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (196.00 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9200 mL 19.6002 mL 39.2003 mL
5 mM 0.7840 mL 3.9200 mL 7.8401 mL
10 mM 0.3920 mL 1.9600 mL 3.9200 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.80 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.80 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Gupta A, et al. Nanocarrier Composed of Magnetite Core Coated with Three Polymeric Shells Mediates LCS-1 Delivery for Synthetic Lethal Therapy of BLM-Defective Colorectal Cancer Cells. Biomacromolecules. 2018 Mar 12;19(3):803-815.

    [2]. Somwar R, et al. Superoxide dismutase 1 (SOD1) is a target for a small molecule identified in a screen for inhibitors of the growth of lung adenocarcinoma cell lines. Proc Natl Acad Sci U S A. 2011;108(39):16375-16380.

    [3]. Du T, et al. Proteomic analysis identifies mechanism(s) of overcoming bortezomib resistance via targeting ubiquitin receptor Rpn13. Leukemia. 2021 Feb;35(2):550-561.

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