(2-Chloropyridin-4-yl)methanamine hydrochloride (Synonyms: LOXL2-IN-1 hydrochloride) |
Catalog No.GC30544
One-Click Copy Product Info
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(2-Chloropyridin-4-yl)methanamine hydrochloride is a highly selective inhibitor of lysyl oxidase-like protein-2 (LOXL2), with an IC50 of 126nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 916210-98-5
Sample solution is provided at 25 µL, 10mM.
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(2-Chloropyridin-4-yl)methanamine hydrochloride is a highly selective inhibitor of lysyl oxidase-like protein-2 (LOXL2), with an IC50 of 126nM[1]. LOXL2 is a secreted copper-dependent amine oxidase that catalyzes the cross-linking of lysine residues in collagen and elastin, thereby regulating extracellular-matrix remodeling and playing a key role in tumor metastasis, fibrosis, and tissue repair[2]. (2-Chloropyridin-4-yl)methanamine hydrochloride is widely used in the research of tumor invasion, metastasis and epithelial-mesenchymal transition (EMT) mechanisms[3][4].
In vitro, treatment of cervical cancer cells (SIHA and HELA) with (2-Chloropyridin-4-yl)methanamine hydrochloride (0–2792.5μM; 24–96h) significantly inhibits cell viability (with IC50 values of 465.25μM for SIHA cells and 246.909μM for HELA cells), cell migration, invasion, and proliferation, induces apoptosis, and suppresses malignant transformation by reversing the LOXL2-induced epithelial-mesenchymal transition (EMT) process in a concentration-dependent manner[5]. Treatment of Huh7 and Hep3B cells with (2-Chloropyridin-4-yl)methanamine hydrochloride (50nM; 12h) significantly upregulates FBP1 expression, downregulates Snail, HIF-1α, and VEGF expression, and inhibits cell proliferation, glycolysis, and angiogenesis[6].
In vivo, (2-Chloropyridin-4-yl)methanamine hydrochloride(100μg/kg/day; i.p.; 4 weeks) significantly reduced atrial fibrosis and vulnerability to atrial fibrillation, attenuated atrial inflammation and cardiac hypertrophy, and reversed the activation of the TGF-β1/Smad2/3 pathway and collagen I expression in Angiotensin II-induced mice atrial fibrillation (AF) models[7].
References:
[1] Hutchinson JH, Rowbottom MW, Lonergan D, et al. Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors: The Identification of an Inhibitor Selective for LOXL2 over LOX. ACS Med Chem Lett. 2017;8(4):423-427.
[2] Moon HJ, Finney J, Ronnebaum T, Mure M. Human lysyl oxidase-like 2. Bioorg Chem. 2014;57:231-241.
[3] Ye C, Jiang S, Zeng T, He S, Cao J, Xiao J. The role of LOXL2 in tumor progression, immune response and cellular senescence: a comprehensive analysis. Discov Oncol. 2024;15(1):245.
[4] Ferreira S, Saraiva N, Rijo P, Fernandes AS. LOXL2 Inhibitors and Breast Cancer Progression. Antioxidants (Basel). 2021;10(2):312.
[5] Peng T, Lin S, Meng Y, et al. LOXL2 small molecule inhibitor restrains malignant transformation of cervical cancer cells by repressing LOXL2-induced epithelial-mesenchymal transition (EMT). Cell Cycle. 2022;21(17):1827-1841.
[6] Fan Z, Zheng W, Li H, et al. LOXL2 upregulates hypoxia inducible factor 1α signaling through Snail FBP1 axis in hepatocellular carcinoma cells. Oncol Rep. 2020;43(5):1641-1649.
[7] Wu Y, Can J, Hao S, Qiang X, Ning Z. LOXL2 Inhibitor Attenuates Angiotensin II-Induced Atrial Fibrosis and Vulnerability to Atrial Fibrillation through Inhibition of Transforming Growth Factor Beta-1 Smad2/3 Pathway. Cerebrovasc Dis. 2022;51(2):188-198.
| Cell experiment [1]: | |
Cell lines | human cervical cancer cell lines HELA and SIHA |
Preparation Method | The human cervical cancer cell lines HELA and SIHA were cultured in Dulbecco’s modified Eagle’s medium with 10% fetal bovine serum and antibodies (100U/ml penicillin plus streptomycin). They were cultured at 37°C in an incubator containing 5%CO2. One thousand cells were planted in each pore of 96-well plate. After the cells adhered to the wall, (2-Chloropyridin-4-yl)methanamine hydrochloride with different concentrations (0–2792.5μM) were added into the corresponding pore according to the experimental design. The cell viability was measured by the Cell Counting Kit-8 (absorbance=450nm) at 0 hours, 24 hours, 48 hours, 72 hours and 96 hours, respectively. SIHA and HELA cells were harvested after treatment, and further measured by an Annexin V APC (650nm) and 7-AAD(546nm). All experiments were performed three times. |
Reaction Conditions | 0–279.25μM; 24–96h |
Applications | (2-Chloropyridin-4-yl)methanamine hydrochloride significantly inhibits cell viability (with IC50 values of 465.25μM for SIHA cells and 246.909μM for HELA cells) and induces cell apoptosis. |
| Animal experiment [2]: | |
Animal models | male C57BL/6 mice |
Preparation Method | Eight-week-old male C57BL/6 mice were subcutaneously infused with saline or Ang II (2.0mg/kg/day) using osmotic mini-pumps for 4 weeks. The LOXL2 inhibitor, (2-Chloropyridin-4-yl)methanamine hydrochloride (100μg/kg/day), or saline was administered intraperitoneal for 4 weeks. The control mice received saline infusion. After mice were anesthetized with 1% pentobarbital sodium, the heart was obtained and weighed to calculate the ratio of heart weight (HW) to body weight. Then the atrial tissue was collected. Some tissue was snap-frozen in liquid nitrogen for molecular biology analysis. Another tissue was fixed in 4% paraformaldehyde for histological studies. |
Dosage form | 100μg/kg/day; i.p.; 4 weeks |
Applications | (2-Chloropyridin-4-yl)methanamine hydrochloride significantly reduced Angiotensin II-induced atrial fibrosis reversed the activation of the TGF-β1/Smad2/3 pathway and collagen I expression. |
References: | |
| Cas No. | 916210-98-5 | SDF | |
| Synonyms | LOXL2-IN-1 hydrochloride | ||
| Canonical SMILES | [H]Cl.ClC1=NC=CC(CN)=C1 | ||
| Formula | C6H8Cl2N2 | M.Wt | 179.05 |
| Solubility | Water : ≥ 50 mg/mL (279.25 mM);DMSO : ≥ 33 mg/mL (184.31 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 5.585 mL | 27.9252 mL | 55.8503 mL |
| 5 mM | 1.117 mL | 5.585 mL | 11.1701 mL |
| 10 mM | 558.5 μL | 2.7925 mL | 5.585 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)