LY-364947, also known as LY364947, is a TGF-β (transforming growth factor-beta) receptor I kinase inhibitor. It is a small-molecule compound with the chemical formula C22H19N3O2S and a molecular weight of 393.47 g/mol. Its CAS (Chemical Abstracts Service) number is 396129-53-6.
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LY364947 is also known by other names such as N-(2-(6-Methylpyridin-2-yl)-1H-benzo[d]imidazol-5-yl)-3-(3-pyridinyl)urea, TGF beta RI kinase inhibitor IV, and 4-(4-(benzo[d]imidazole-5-yl)-pyrimidin-2-ylamino)-N-methylpyridine-2-sulfonamide.
Health Benefits of LY-364947:
LY-364947 has shown potential health benefits in various preclinical and clinical studies. Some of these are detailed below:
Cancer Therapy: LY-364947 exhibits anticancer properties by inhibiting the TGF-β signaling pathway, which plays a vital role in tumor growth, invasion, and metastasis. Studies have shown that LY-364947 suppresses the growth and migration of cancer cells, making it a promising candidate for cancer therapy.
Fibrosis: LY-364947 helps to reduce the progression of fibrosis, a condition where there is an excessive deposition of extracellular matrix leading to organ damage. The drug inhibits the differentiation of fibroblasts into myofibroblasts, which are responsible for the production of collagen.
Anti-inflammatory Agent: LY-364947 can help in reducing inflammation caused by chronic diseases such as arthritis, asthma, and inflammatory bowel disease. It does so by inhibiting the TGF-β signaling pathway, which plays a crucial role in inflammation.
LY-364947 has been shown to have various potential effects. Some of these are:
Anticancer Effect: LY-364947 has shown potent anticancer effects, especially in breast, colon, liver, and pancreatic cancers. It inhibits tumor cell proliferation, migration, and metastasis.
Reduces Fibrosis Progression: LY-364947 has been found to be effective in reducing the progression of fibrosis, which is a significant contributor to various chronic diseases.
Anti-inflammatory Effect: LY-364947 has been shown to have anti-inflammatory effects, which could be useful in treating various chronic inflammatory conditions.
The mechanism of action of LY-364947 is via inhibition of the TGF-β signaling pathway. TGF-β is a cytokine that regulates many cellular processes, including cell proliferation, differentiation, and apoptosis. Dysregulation of the TGF-β signaling pathway has been implicated in several diseases, including cancer and fibrosis. LY-364947 selectively binds to and inhibits the activity of TGF-β receptor I kinase, thereby blocking downstream signaling events.
LY-364947 has been shown to be well-tolerated in preclinical and clinical studies. However, like all drugs, it can cause side effects, which are discussed below. Patients should always consult their healthcare provider before starting any new medication.
Some of the common side effects of LY-364947 include:
The dosing information for LY-364947 varies depending on the condition being treated, patient factors, and other medications the patient may be taking. In phase 1 clinical trials, doses ranged from 25 mg to 1000 mg per day.
LY-364947 is a promising small-molecule inhibitor of the TGF-β signaling pathway, which plays a crucial role in various diseases such as cancer and fibrosis. Preclinical and clinical studies have shown its potential as a therapeutic agent for cancer, fibrosis, and chronic inflammatory conditions. Although generally well-tolerated, LY-364947 can cause side effects, and patients should always consult their healthcare provider before starting any new medication. Further research is needed to determine its full therapeutic potential and optimize dosing regimens