RNA synthesis inhibitor
Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.
Chloroquine diphosphate 50 mg
£97.00
Target: ATM (cell-free-assay)
Chemical name: 1,4-Pentanediamine, N4-(7-chloro-4-quinolinyl)-N1,N1-diethyl-, phosphate (1:2)
Formula: C18H26ClN3.2H3O4P
Molecular weight: 515.86
Size: 50 mg
Purity: 99.65 % (HPLC)
Solubility: 100 mg/mL (water)
Storage: 3 years -20°C powder, 2 years -80°C in solvent
In vitro:
Chloroquine is a chemotherapeutic agent for the clinical treatment of malaria. Chloroquine is able to bind to DNA, and inhibit DNA replication and RNA synthesis which in turn results in cell death. The effect of Chloroquine may also be related to the formation of a toxic heme-Chloroquine complex. Chloroquine inhibits trophozoite hemoglobin degradation through increasing vacuolar pH and inhibiting the activity of vacuolar phospholipase, vacuolar proteases, and heme polymerase[1]. Chloroquine possesses definite antirheumatic properties. Chloroquine has immuno-modulatory effects, suppressing the production/release of tumour necrosis factor and interleukin 6. Moreover, Chloroquine exerts direct antiviral effects, inhibiting pH-dependent steps of the replication of several viruses including members of the flaviviruses, retroviruses, and coronaviruses. Its best-studied effects are those against HIV replication[2]. Chloroquine can accumulate inside the macrophage phagolysosome by ion trapping where it exerts potent antifungal activity against Histoplasma capsulatum and Cryptococcus neoformans by distinct mechanisms. Chloroquine inhibits growth of H. capsulatum by pH-dependent iron deprivation, whereas it is directly toxic to C. neoformans[3].
References:
1] Slater AF. Pharmacol Ther, 1993, 57(2-3), 203-235.
[2] Savarino A, et al. Lancet Infect Dis, 2003, 3(11), 722-727.
[3] Weber SM, et al. Curr Opin Microbiol, 2000, 3(4), 349-353.
Chloroquine diphosphate has been referenced in publications:
Zika virus degrades the ω-3 fatty acid transporter Mfsd2a in brain microvascular endothelial cells and impairs lipid homeostasis. [ Sci Adv, 2019, 5(10):eaax7142] PubMed: 31681849
A genome-wide RNAi screen reveals essential therapeutic targets of breast cancer stem cells. [ EMBO Mol Med, 2019, 11(10):e9930] PubMed: 31476112
CACYBP Enhances Cytoplasmic Retention of P27Kip1 to Promote Hepatocellular Carcinoma Progression in the Absence of RNF41 Mediated Degradation. [ Theranostics, 2019, 9(26):8392-8408] PubMed: 31754404
E3 ubiquitin ligase RNF170 inhibits innate immune responses by targeting and degrading TLR3 in murine cells [ Cell Mol Immunol, 2019, 10.1038/s41423-019-0236-y] PubMed: 310767237
Deoxynarciclasine shows promising antitumor efficacy by targeting Akt against hepatocellular carcinoma [ Int J Cancer, 2019, 10.1002/ijc.32395] PubMed: 31081930
Synergy between arsenic trioxide and JQ1 on autophagy in pancreatic cancer. [ Oncogene, 2019, 38(47):7249-7265]PubMed: 31420604
Targeting the deubiquitinase STAMBPL1 triggers apoptosis in prostate cancer cells by promoting XIAP degradation [ Cancer Lett, 2019, 456:49-58] PubMed: 31004702
A Simple Three-dimensional Hydrogel Platform Enables Ex Vivo Cell Culture of Patient and PDX Tumors for Assaying Their Response to Clinically Relevant Therapies [ Mol Cancer Ther, 2019, 18(3):718-725] PubMed: 30755456
Autophagy mediates serum starvation-induced quiescence in nucleus pulposus stem cells by the regulation of P27. [ Stem Cell Res Ther, 2019, 10(1):118]PubMed: 30987681
Maternal exposure to di-n-butyl phthalate promotes Snail1-mediated epithelial-mesenchymal transition of renal tubular epithelial cells via upregulation of TGF-β1 during renal fibrosis in rat offspring. [ Ecotoxicol Environ Saf, 2019, 169:266-272] PubMed: 30453174