694433-59-5 Usage
Description
2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride, also known as SB-505124 hydrochloride hydrate, is a chemical compound that functions as a selective inhibitor of the transforming growth factor-beta (TGF-β) type I receptor ALK5. It is characterized by its ability to inhibit the TGF-β1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM, making it a potent antagonist. Additionally, it acts as a less potent inhibitor of ALK4 and ALK7, selectively and concentration-dependently inhibiting the activation of downstream SMAD2 and SMAD3, as well as TGF-β-induced MAP kinase pathway components.
Uses
Used in Pharmaceutical Research:
2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride is used as a research tool for studying the role of the TGF-β pathway in development and differentiation processes. Its ability to selectively inhibit ALK5, ALK4, and ALK7 makes it valuable in understanding the intricate mechanisms of TGF-β signaling.
Used in Cancer Research:
In the field of cancer research, 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride is utilized as a selective inhibitor of TGF-β type I receptors, which play a crucial role in tumor growth, metastasis, and immune evasion. It has been shown to block TGF-β-induced apoptosis of FaO cells and NRP 154 cells in a concentration-dependent manner and to suppress the migration and invasion of breast cancer MCF-7-M5 cells, making it a potential therapeutic agent for cancer treatment.
Used in Drug Development:
2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride is employed in the development of drugs targeting the TGF-β pathway. Its high potency and selectivity for ALK5, along with its ability to inhibit ALK4 and ALK7, make it a promising candidate for the creation of targeted therapies that can modulate TGF-β signaling, potentially leading to novel treatments for various diseases, including cancer and fibrosis.
Used in Assay Development:
In the development of assays to determine the in vitro phosphorylation of SMAD3, 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride serves as a benchmark compound. It is more potent than SB-431452, with IC50 values of 47 versus 94 nM, respectively, providing a reference point for evaluating the effectiveness of other compounds in inhibiting TGF-β signaling pathways.
Biochem/physiol Actions
SB-505124 selectively inhibits TGF-β type I receptors, activin receptor-like kinases (ALK) 4, 5 and 7. It inhibits ALK4-, 5- and 7-mediated activation of Smad2, Smad3 and MAPK pathway induced by TGF-β.1 SB-505124 inhibits the human fibroblast trans-differentiation induced by the co-culture with Esophageal squamous cell carcinoma.2
Check Digit Verification of cas no
The CAS Registry Mumber 694433-59-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 6,9,4,4,3 and 3 respectively; the second part has 2 digits, 5 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 694433-59:
(8*6)+(7*9)+(6*4)+(5*4)+(4*3)+(3*3)+(2*5)+(1*9)=195
195 % 10 = 5
So 694433-59-5 is a valid CAS Registry Number.
