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694433-59-5 (SB-505124)

1

Identification

SB-505124 SB-505124
Name SB-505124
Formula C20H21N3O2
MW 335.4
CAS No. 694433-59-5
EINECS
Smiles CC1=CC=CC(C2=C(C3=CC=C(OCO4)C4=C3)N=C(C(C)(C)C)N2)=N1
Synonyms SB 505124;SB505124; 2-(4-(benzo[d][1,3]dioxol-5-yl)-2-(tert-butyl)-1H-imidazol-5-yl)-6-methylpyridine
InChI InChI=1S/C20H21N3O2/c1-12-6-5-7-14(21-12)18-17(22-19(23-18)20(2,3)4)13-8-9-15-16(10-13)25-11-24-15/h5-10H,11H2,1-4H3,(H,22,23)
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Introduction

SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6. IC50 Value: 47 ± 5 nM (ALK5); 129 ± 11 nM (ALK4) [1] Target: ALK4/5 in vitro: SB-505124 was identified as a potent inhibitor of the in vitro kinase activity of ALK5 for its substrate Smad3 with an IC50 of 47 ± 5 nM.

Background Information

SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6. IC50 Value: 47 ± 5 nM (ALK5); 129 ± 11 nM (ALK4) [1] Target: ALK4/5 in vitro: SB-505124 was identified as a potent inhibitor of the in vitro kinase activity of ALK5 for its substrate Smad3 with an IC50 of 47 ± 5 nM. This compound was determined to be a reversible ATP competitive inhibitor, because prior incubation of the ALK5 kinase with high concentrations of the inhibitor, followed by dilution to a sub-IC50concentration had no effect on the kinetics of Smad3 phosphorylation (data not shown). SB-505124 demonstrated no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. Selectivity of the SB-505124 inhibitor for type I receptors other than ALK5 was first evaluated against ALK4 and ALK2 in vitro. SB-505124 inhibited the closely related ALK4 with an IC50value of 129 ± 11 nM (about 2.5-fold less sensitive than ALK5) but did not inhibit ALK2 at concentrations up to 10 μM [1]. The in vitro drug release study demonstrated 100% drug release within 12 h. The gel did not show cytotoxicity to the cultured rabbit subconjunctival cells by MTT assay [2]. Suppression of pSmad2, CTGF, and α-SMA by SB-505124 was observed in cultured fibroblasts [3]. in vivo: In the in vivo rabbit GFS model, the drug was successfully delivered by injection and no severe post-surgical complications were observed [2]. Filtering blebs in the GFS with SB-505124 group were maintained for more than 10 days, and the period of bleb survival was significantly longer than that in controls. IOP levels after surgery seemed to be related to bleb survival. Histologically, subconjunctival cell infiltration and scarring at the surgical site in the GFS with SB-505124 and mitomycin C (MMC) groups were much subsided compared to controls. Suppression of CTGF and α-SMA by SB-505124 was also observed by immunofluorescence [3]. Toxicity: N/A Clinical trial: N/A ......by MedChemexpress Co., Ltd.
SB505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5, ALK4 and ALK7) with potential anticancer activity. SB505124 selectively inhibits signaling from TGF-β and activin; does not inhibit other ALK family members. Shelf life: >2 years if stored properly. Drug formulation: ......by MedKoo Biosciences, Inc.
SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6. ......by Selleck Chemicals LLC
SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM in cell-free assays, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6. ......by Target Molecule Corp.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000016855

Storage condition

Solubility

DMSO 67 mg/mL; Water <1 mg/mL; Ethanol 67 mg/mL by MedChemexpress Co., Ltd.
DMSO 67 mg/mL (199 mM) ; Water <1 mg/mL (<1 mM) ; Ethanol 67 mg/mL (199 mM) by Selleck Chemicals LLC
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Mechanism and Indication

Signaling Pathways TGF-beta/Smad
Target TGF-β Receptor
Research Area Cancer
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
SB-505124 - Not Found
SB-505124 - No Development Reported
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Safety Data of SB-505124

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
Abcam 25mg/USD315() USA
Axon Medchem BV 5mg/USD114(In Stock) Netherlands
CHEMSCENE, LLC USA
Carbosynth Limited 5mg/USD140()
Cayman Chemical Company 1mg/USD18() USA
MedChemexpress Co., Ltd. 10mg/USD120(In stock);50mg/USD420(In stock) USA
MedKoo Biosciences, Inc. 10mg/USD150() USA
Santa Cruz Biotechnology, Inc. 10mg/USD205() USA
Selleck Chemicals LLC 10mg/USD170(In stock);10mM/1mLIn DMSO/USD220(In stock);10mM(in 1mL DMSO)/USD277(in 1mL DMSO);50mg/USD570(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD120(In stock);50mg/USD420(In stock) China
Target Molecule Corp. 10mg/USD112();25mg/USD213();50mg/USD382() USA
Tocris Bioscience Inc. 10mg/USD219() USA
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Related Products

Other Forms of 694433-59-5

Name CAS No Formula MW
SB-505124 (hydrochloride) 356559-13-2 C20H22ClN3O2 371.86

Recommended Compounds in TGF-β Receptor

Name CAS No Formula MW
K 02288 1431985-92-0 C20H20N2O4 352.38
ML347 1062368-49-3 C22H16N4O 352.39
DMH-1 1206711-16-1 C24H20N4O 380.44
LDN-212854 1432597-26-6 C25H22N6 406.48
SB-505124 (hydrochloride) 356559-13-2 C20H22ClN3O2 371.86
A 77-01 607737-87-1 C18H14N4 286.33
LY-364947 396129-53-6 C17H12N4 272.3
LDN193189 (Hydrochloride) 1062368-62-0 C25H26Cl4N6 552.33
SD-208 627536-09-8 C17H10ClFN6 352.75
RepSox 446859-33-2 C17H13N5 287.32
LDN193189 1062368-24-4 C25H22N6 406.48
A 83-01 909910-43-6 C25H19N5S 421.52
LY2109761 700874-71-1 C26H27N5O2 441.52
LY2157299 700874-72-2 C22H19N5O 369.42
GW788388 452342-67-5 C25H23N5O2 425.48
SB 525334 356559-20-1 C21H21N5 343.42
SB-431542 301836-41-9 C22H16N4O3 384.39
EW-7197 1352608-82-2 C22H18FN7 399.42
R-268712 879487-87-3 C20H18FN5O 363.39
ITD-1 1099644-42-4 C27H29NO3 415.52

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

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More Information

SB-505124

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