Chemical Property of 2-(4-(benzo[d][1,3]dioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl)-6-methylpyridine
Chemical Property:
- Melting Point:168 °C
- Boiling Point:509.7±50.0 °C(Predicted)
- PKA:11.26±0.10(Predicted)
- PSA：60.03000
- Density:1.202
- LogP:4.47330
- Storage Temp.:2-8°C
- Solubility.:DMSO: >10mg/mL
- XLogP3:4.3
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:4
- Rotatable Bond Count:3
- Exact Mass:335.16337692
- Heavy Atom Count:25
- Complexity:466
- Purity/Quality:
-
99%, *data from raw suppliers
SB-505124 *data from reagent suppliers
Safty Information:
- Pictogram(s):
Xi
- Hazard Codes:Xi
- Statements:
36/37/38
- Safety Statements:
26-36
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CC1=NC(=CC=C1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=C(C=C3)OCO4
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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.
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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. 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. SB-505124 hydrochloride hydrate was used to study the role of TGF-β pathway in development and differentiation studies.3,4
