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HomeProduct name list2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride

2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride

Synonym(s):2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrochloride hydrate

2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine  hydrate  hydrochloride Structural

What is 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride?

Description

SB-505124 inhibits the TGF-β1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM. Though it is a less potent antagonist of ALK4 (IC50 = 129 nM) and ALK7, SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK7-dependent activation of downstream SMAD2 and SMAD3 and TGF-β–induced MAP kinase pathway components without altering ALK1-3 or ALK6-induced SMAD signaling. In an assay determining in vitro phosphorylation of SMAD3, SB-505124 is more potent than SB-431452 with IC50 values of 47 versus 94 nM, respectively.

The Uses of 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride

SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptor ALK5 and as well as being a selective inhibitor of ALK4 but with less potency. SB-505124 blocks TGF-β–induced apoptosis of FaO cells and NRP 154 cells in a concentration-dependent manner. SB-505124 has been shown to suppress the migration and invasion of breast cancer MCF-7-M5 cells.

The Uses of 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride

SB-505124 inhibits the TGF-β1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM. Though it is a less potent antagonist of ALK4 (IC50 = 129 nM) and ALK7, SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK7-dependent activation of downstream SMAD2 and SMAD3 and TGF-β–induced MAP kinase pathway components without altering ALK1-3 or ALK6-induced SMAD signaling. In an assay determining in vitro phosphorylation of SMAD3, SB-505124 is more potent than SB-431452 with IC50 values of 47 versus 94 nM, respectively.

The Uses of 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride

SB-505124 hydrochloride hydrate was used to study the role of TGF-β pathway in development and differentiation studies.3,4

What are the applications of Application

SB-505124 is an inhibitor of Activin receptor-like kinase 5

Definition

ChEBI: SB 505124 is a member of the class of imidazoles carrying tert-butyl, 1,3-benzodioxol-5-yl and 6-methylpyridin-2-yl substituents at positions 2, 4 and 5 respectively. It has a role as a TGFbeta receptor antagonist. It is a member of imidazoles, a benzodioxole and a member of methylpyridines.

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

storage

Store at -20°C

Properties of 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride

Melting point: 168 °C
Boiling point: 509.7±50.0 °C(Predicted)
Density  1.202
storage temp.  Sealed in dry,2-8°C
solubility  DMSO: >10mg/mL
form  powder
pka 11.26±0.10(Predicted)
color  yellow

Safety information for 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P264:Wash hands thoroughly after handling.
P264:Wash skin thouroughly after handling.
P271:Use only outdoors or in a well-ventilated area.
P280:Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352:IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride

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