Enzyme Modulators

<p>Malotilate is a pharmacological agent that is used to treat symptoms of hepatitis, bowel disease, and collagen diseases. This drug reduces collagen synthesis and cell migration activity of fibroblasts in vitro. It also has been shown to facilitate liver regeneration in rats.</p>

<p>Inhibitor of glycogen synthase 3 (GSK-3) and cyclin-dependent kinases CDK1, CDK2 and CDK5. Kenpaullone can substitute transcription factor Klf4 in reprogramming of fibroblast to induced pluripotent stem cells when using the method of ectopic expression of transcriptional factors. In an in vitro model for Alzheimer’s disease, kenpaullone decreased production of amyloid beta peptides Aβ40 and Aβ42.</p>

<p>Inhibitor of EIF2AK3/PERK kinases</p>

<p>(S)-Mephenytoin is a substrate of cytochrome P450 enzyme CYP2C19 (a hydroxylase). It is an effective anticonvulsant that improves control of seizures in patients. According to studies, the drug exhibits a genetic polymorphism in CYP2C19 that results in reduced metabolism in some individuals.</p>

<p>Inhibits YAP/Tead transcriptional activity. Has anti-tumour effects on oesophageal adenocarcinoma with therapeutic potential in combination with 5-FU. Involved in ferroptosis, mediated by iron-dependent ROS.</p>

<p>Analeptic</p>

<p>Etodolac is a non-steroidal anti-inflammatory drug (NSAID) used to treat osteoarthritis and rheumatoid arthritis. It is also used to treat acute pain. This drug works by inhibiting prostaglandin synthesis from the inhibition of the enzyme cyclooxygenase.</p>

<p>Inhibitor of protein kinase CK2</p>

<p>6-Thioguanine is a purine analog used in the therapy for leukemia and for remission consolidation in patients with acute nonlymphocytic anemia. This drug also has antimetabolite action. It replaces guanine during DNA replication. This substitution disrupts the accurate pairing of DNA bases, leading to errors in DNA replication and hinders cell division.</p>

<p>Inhibitor of glutathione peroxidase GPX4</p>

<p>Inhibits RNAPII-mediated trasncription; immunosuppressant; anti-inflammatory</p>

<p>A small molecule inhibitor with high selectivity for CDK8 over CDK19. Increases IL-10 production in stimulated human and murine macrophages and dendritic cells. Modulatory action on inflammatory responses has therapeutic potential.</p>

<p>Allosteric activator of AMP-activated protein kinase (AMPK) acting on the AMPK-β subunit with therapeutic potential in metabolic disorders such as diabetes, obesity, etc. A769662 also blocks the differentiation of mouse embryonic stem cells (mESCs) and maintains the mESCs in naïve state even in the absence of leukemia inhibitory factor (2i/L).</p>

<p>Tacrolimus is a calcineurin inhibitor drug that is used for the prevention of rejection after an organ transplant. This drug can also be used in the treatment of severe atopic dermatitis. Tacrolimus’ mechanism of action is not well known however it is understood that this drug inhibits T-lymphocyte activation by binding to an intracellular protein called FKBP-12. This drug also has anti-inflammatory properties.</p>

<p>A potent inhibitor of EGFR with sensitizing and T790M resistance mutations, selective over the wild-type form of the receptor. Causes tumour regression in EGFR mutant T790M transgenic and xenograft models in vivo.</p>

<p>Ramipril is an angiotensin-converting enzyme (ACE) inhibitor. It is used in the treatment of high blood pressure, congestive heart failure and other cardiovascular diseases. Ramipril inhibits the conversion of angiotensin I to angiotensin II by blocking ACE, which lowers blood pressure and reduces fluid retention.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&amp;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.</p>

<p>Inhibitor of PDE4 enzyme; anti-inflammatory</p>

<p>Inhibitor of the Bruton tyrosine kinase</p>

<p>Anti-inflammatory; inducer of P450 II B family</p>

<p>Diacerein is a slow-onset anthraquinone IL-1 inhibitor that is used in the treatment of joint diseases such as osteoarthritis. This drug is also being studied for the treatment of insulin resistance and diabetes mellitus. Diacerein works to decrease inflammation and cartilage destruction by reducing the level of interleukin-1.</p>