Modulateurs d'enzymes

Dual inhibitor of the adaptor protein 2-associated kinase 1 (AAK1) and BMP2-inducible kinase (BMP2K) with IC50 values of 270 nM and 1 μM, respectively. In a recent study, SGC AAK1 1 stabilised β-catenin, inhibited phosphorylation of the AP2 complex subunit mu protein (AP2M1) and activated Wnt signalling in in vitro experiments._x000D_

A pan-WNK kinase inhibitor, acting on WNK1, WNK2, WNK3, and WNK4 kinases. Affects blood pressure, heart rate, body fluid and electrolyte homeostasis in rodent models of hypertension.

Meloxicam is a non-steroidal anti-inflammatory drug (NSAID) which is used to treat various types of pain and inflammation caused by arthritis. It is also a COX-2 inhibitor which reduces gastrointestinal effects of this drug. Inhibiting these enzymes, allow for a decrease in inflammatory symptoms. Meloxicam 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.

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.

Inhibitor of FLT3 kinase and acid sphingomyelinase

Dual IGF-1R and InsR kinase inhibitor; antineoplastic

Competitive, reversible inhibitor of α-glucosidases used for the control of postprandial hyperglycaemia in patients with type 2 diabetes mellitus. It inhibits digestive enzymes with α-glucosidase activity, which breakdown complex sugars to absorbable monosaccharides. It also reduces the levels of glycated haemoglobin (HbA1c).

Anti-parasitic; pyruvate ferredoxin oxidoreductase inhibitor

Orally available prodrug of gemcitabine

MGMT, known as O6-methylguanine-DNA methyltransferase, is a DNA repair enzyme that plays an important role in chemoresistance to alkylating agents. MGMT repairs the toxic DNA O6-Methylguanine lesion caused by Temozolomide (TMZ), an oral alkylating agent used for the treatment of glioblastoma. MGMT repairs damaged guanine nucleotides by transferring the methyl at O6 site of guanine to its cysteine residues, thus avoiding gene mutation, cell death and tumorigenesis. The expression of MGMT gene is mainly regulated by epigenetic modification. Loss of MGMT expression is due to methylation of the CpG island of MGMT promoter.

O8 OGG1 Inhibitor is a glycosylase enzyme that catalyses the conversion of guanine to xanthine. It is a key enzyme in the DNA repair mechanism called base excision repair or BER. This enzyme inhibits the hydrolysis of glycosidic bond required for the excision of 8-oxoguanine from double stranded DNA, which leads to accumulation of mutations. Additionally, it has been proposed as monotherapy for certain types of cancers. Furthermore, it has been seen to sensitise tumours for chemotherapy therefore research is being carried out to identify its potential to be used alongside cancer therapy. O8 OGG1 Inhibitor 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.

Inhibitor of poly (ADP-ribose) polymerase enzyme; antineoplastic

EGFR tyrosine kinase inhibitor

A potent non ATP-competitive inhibitor of MAP/ERK kinase (MEK). Has anti-tumor activity in melanoma and papillary thyroid cancer cells with B-Raf mutations. Enhances generation and survival of induced pluripotent stem cells (iPSCs).

A potent inhibitor of histone deacetylases (HDACs) of class I and II with anti-tumoral activity. The compound blocks HDAC catalytic activity by chelating zinc ion in the enzyme’s active site. Extensively used in research as epigenetic modifier able to block cell growth and downregulate proliferation-associated factors. It has also been reported that trichostatin A induces apoptosis via a histone-modification independent mechanism in oral squamous cell carcinoma cell lines. Initially discovered as anti-fungal compound from Streptomyces hygroscopicus for the control of fungal infections caused by the genus Trichophyton.

Activator of soluble guanylyl cyclase (sGC) which stimulates cGMP production and is effective in cells under oxidative stress. Ataciguat stimulates the heme-free form of the sGC enzyme via the sGC N-terminus of β1-subunit. Ataciguat can promote vasorelaxation and hypotension by restoring or potentiating the nitric oxide (NO) signalling pathway.

Amino acids 487-496 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 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.

Inhibitor of ErbB2 (IC50 = 3 nM) and EGFR kinase (IC50 = 6.4 nM) with anti-proliferative effects. It inhibits ErbB2 receptor autophosphorylation and induces G1 cell cycle block. The CP 724714 treatment induces reduction of downstream ErbB2 receptor tyrosine kinase signalling, tumor cell apoptosis, release of caspase 3 and regression of tumors in in vivo and in vitro models.

Monoamine oxidase-B inhibitor; anti-parkinsonian; neuroprotective

Inhibitor of the Bruton tyrosine kinase