- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Bioactive Molecules
- Anti-infection
- Apoptosis
- Autophagy
- Cell Cycle/DNA Damage
- Cytoskeleton
- Epigenetics
- GPCR/G Protein
- Immunology/Inflammation
- JAK/STAT Signaling
- MAPK/ERK Pathway
- Membrane Transporter/Ion Channel
- Metabolic Enzyme/Protease
- Neuronal Signaling
- NF-κB
- PI3K/Akt/mTOR
- PROTAC
- Protein Tyrosine Kinase/RTK
- Stem Cell/Wnt
- TGF-beta/Smad
- Vitamin D Related/Nuclear Receptor
- Others
- Methylation
- Cytoskeletal Signaling
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 41931-13-9] LCS-1
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-115445 |
| Brand: | MCE |
| CAS: | 41931-13-9 |
Overview
| MDL | MFCD00814448 |
|---|---|
| Molecular Weight | 255.10 |
| Molecular Formula | C11H8Cl2N2O |
| SMILES | O=C1C(Cl)=C(Cl)C=NN1C2=CC=CC(C)=C2 |
Summary
IC50 & Target
|
SOD1 1.07 μM (IC 50 ) |
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 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]
.
MCE 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 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). |
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] .
MCE 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 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 196.00 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (9.80 mM); Clear solution
References
- [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.
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.