Modulateurs d'enzymes

Fasudil hydrochloride is a Rho-kinase inhibitor, which is a synthetic compound derived from natural sources, primarily used in scientific research. The mode of action of Fasudil hydrochloride involves the inhibition of Rho-associated protein kinase (ROCK), a crucial player in the regulation of the actin cytoskeleton. By inhibiting ROCK, Fasudil alters various cellular functions, including contraction, motility, proliferation, and apoptosis. Fasudil hydrochloride is primarily applied in neurological and cardiovascular research. It is utilized to investigate the therapeutic potential for conditions like cerebral vasospasm, ischemic stroke, and other vascular disorders. In the realm of neuroscience, it aids in studying the pathophysiological processes of neurodegenerative diseases, given its capacity to ameliorate the effects of vascular damage and enhance blood flow. Additionally, its role is being explored in areas related to hypertension and atherosclerosis. The broad applicability of Fasudil hydrochloride in diverse research areas accentuates its significance in understanding disease mechanisms and evaluating potential therapeutic interventions.

This product is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

First generation PI 3-kinase inhibitor

Inhibitor of DNA topoisomerase I

Inhibitor of cGMP-dependent phosphodiesterase 2A (PDE2A) with IC50 = 2 nM and has higher affinity over other phosphodiesterases (> 500-fold). Increases cGMP in rodent brain in vivo. Reverses anxiolytic behaviour, enhances performance of new object recognition and social recognition tasks.  Potentiates NMDA signalling and reverses behavioural effects of NMDA antagonists.

NMDA receptor antagonist

An irreversible GSK-3β inhibitor that reduces phosphorylation of tau proteins, protects from neuronal loss and has cognitive and behavioural benefits in murine models. Studied for its potential as a therapeutic agent in Alzheimer’s disease and other neurodegenerative diseases. Tideglusib was also shown to inhibit the main protease Mpro from the SARS-CoV-2 virus with IC50 of 1.55 μM.

Selective inhibitor of the mutated RET variant RETV804M, which is the anticipated drug-resistant RET mutant that can occur in tumours treated with kinase inhibitors. The compound has a biochemical IC50 of 0.02 µM and selectivity for purified RETV804M over purified RET and KDR of 3.7 and 110, respectively. The efficacy of the compound was shown also in cell cultures with IC50 of 4.4 µM, and cell assay selectivity for RETV804M over RET and KDR of 0.89 and 2.3, respectively.

LW-II-41-27 is a novel Eph receptor tyrosine kinase inhibitor used for cancer treatment.

Inhibitor of S-adenosylhomocysteine hydrolase that disrupts histone methylation by EZH2. Anti-proliferative in some breast cancer and invasive prostate cancer cell lines. One of four key molecules required for inducing chemical reprogramming of somatic cells into induced pluripotent stem cells (iPSC).

Inhibitor of IKKβ serine kinase

Inhibitor of calpain, a calcium-dependent cysteine protease which is implicated in the apoptosis as well as in synaptic plasticity, where it was seen to block long-term potentiation. Calpain inhibitor II has also antiviral properties as it was shown to inhibit the main protease Mpro (3CLpro) from SARS-CoV-2 with IC50 of 0.97 μM.

A potent and selective covalent inhibitor of fibroblast growth factor receptor 4 (FGFR4). This receptor tyrosine kinase activates an oncogenic driver in hepatocellular carcinoma, the fibroblast growth factor 19 (FGF19). The FGFR4 inhibitor is therefore a promising candidate for the treatment of advanced liver cancer.

Inhibitor of cyclin dependend kinases

Lysine-specific demethylase 1 ( LSD1) antagonist

Irreversible blocker of three members of the ErbB family (ErbB1, ErbB2/HER2, and ErbB4) with IC50 in nanomolar range. The compound binds covalently to cysteine 797 residue in HER2 and blocks downstream cellular signalling, inhibits cellular growth and promotes apoptosis. Afatinib has been used for the treatment of tyrosine kinase inhibitor-resistant tumours with mutations in ErbB genes, especially for deletions in exon 19 and single nucleotide substitutions in exon 21. It has been used for treatment of non-small cell lung cancer (NSCLC), breast cancer, pancreatic cancer, colorectal cancer, etc.

Pan-tyrosine kinase inhibitor (VEGFR2, c-MET, RET, KIT); anti-neoplastic

Inhibitor of CDK4/6 serine/threonine kinases; antineoplastic

Amino acids 651-660 of Poly(ADP-ribose) polymerase 1 (PARP1). PARP1 is a nuclear DNA repair enzyme that binds to DNA when damage is detected. PARP1 coordinates double and single strand break repair by first cleaving NAD+ into nicotinamide and ADP-ribose, and then synthesising poly-(ADP-ribose) (PAR) chains from ADP-ribose on target proteins (PARylation). PARylation of histone proteins mediates the relaxation of the chromatin and recruitment of DNA-break repair enzymes.PARP1 can also act as a transcriptional co-activator, modulating the expression of itself and many other genes by direct binding to or PARylation of enhancers and promoters. PARP1 is also involved in maintaining mtDNA.PARP1 belongs to the PARP family which has 7 known and 10 putative members. PARP1 accounts for >85% of the PARP activity in cellular systems.

Inhibits Jak kinases; immunosuppressive; anti-inflammatory