| Identification | Back Directory | [Name]
2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride | [CAS]
694433-59-5 | [Synonyms]
CS-872
SB505124;SB505124
SB-505124 hydrochloride hydrate
SB-505124 hydrate hydrochloride
SB-505124, 98%, a selective inhibitor of TGFβR for ALK4, ALK5
2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-iMidazol-4-yl)-6-Methylpyridine
2-[4-(1,3-Benzodioxol-5-yl)-2-(tert-butyl)-1H-imidazol-5-yl]-6-methylpyridine
2-(4-(benzo[d][1,3]dioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl)-6-methylpyridine
2-[5-(Benzo[d][1,3]dioxol-5-yl)-2-(tert-butyl)-1H-imidazol-4-yl]-6-methylpyridine
2-[4-(1,3-Benzodioxol-5-yl)-2-(1,1- diMethylethyl)-1H-iMidazol-5-yl]-6-Methyl-pyridine
Pyridine, 2-[4-(1,3-benzodioxol-5-yl)-2-(1,1-dimethylethyl)-1H-imidazol-5-yl]-6-methyl-
2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrochloride hydrate
2-[4-(1,3-Benzodioxol-5-yl)-2-(tert-butyl)-1H-imidazol-5-yl]-6-methylpyridine SB505124
2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride | [Molecular Formula]
C20H21N3O2 | [MDL Number]
MFCD11045901 | [MOL File]
694433-59-5.mol | [Molecular Weight]
335.41 |
| Chemical Properties | Back Directory | [Melting point ]
168 °C | [Boiling point ]
509.7±50.0 °C(Predicted) | [density ]
1.202 | [storage temp. ]
2-8°C | [solubility ]
DMSO: >10mg/mL | [form ]
powder | [pka]
11.26±0.10(Predicted) | [color ]
yellow |
| Hazard Information | Back Directory | [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. | [Uses]
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. | [Uses]
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. | [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 |
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