Product Name :
SB505124
Description:
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. SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK 7-dependent activation of downstream cytoplasmic signal transducers, Smad2 and Smad3, and of TGF-beta-induced mitogen-activated protein kinase pathway components but does not alter ALK1, ALK2, ALK3 or ALK6-induced Smad signaling.
CAS:
694433-59-5
Molecular Weight:
335.40
Formula:
C20H21N3O2
Chemical Name:
2-(4-(benzo[d][1,3]dioxol-5-yl)-2-(tert-butyl)-1H-imidazol-5-yl)-6-methylpyridine
Smiles :
CC1=CC=CC(=N1)C1NC(=NC=1C1=CC=C2OCOC2=C1)C(C)(C)C
InChiKey:
WGZOTBUYUFBEPZ-UHFFFAOYSA-N
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)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Belantamab mafodotin} medchemexpress|{Belantamab mafodotin} Antibody-Drug Conjugates (ADCs)|{Belantamab mafodotin} Biological Activity|{Belantamab mafodotin} In Vitro|{Belantamab mafodotin} custom synthesis|{Belantamab mafodotin} Epigenetics}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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. SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK 7-dependent activation of downstream cytoplasmic signal transducers, Smad2 and Smad3, and of TGF-beta-induced mitogen-activated protein kinase pathway components but does not alter ALK1, ALK2, ALK3 or ALK6-induced Smad signaling.|Product information|CAS Number: 694433-59-5|Molecular Weight: 335.40|Formula: C20H21N3O2|Synonym:|SB-505124|SB505124|SB 505124|Chemical Name: 2-(4-(benzo[d][1,3]dioxol-5-yl)-2-(tert-butyl)-1H-imidazol-5-yl)-6-methylpyridine|Smiles: CC1=CC=CC(=N1)C1NC(=NC=1C1=CC=C2OCOC2=C1)C(C)(C)C|InChiKey: WGZOTBUYUFBEPZ-UHFFFAOYSA-N|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)|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO, not in water|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|SB505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC50 value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells.{{Aprocitentan} web|{Aprocitentan} Endothelin Receptor|{Aprocitentan} Technical Information|{Aprocitentan} Purity|{Aprocitentan} manufacturer|{Aprocitentan} Epigenetic Reader Domain} SB505124 (10 µM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro.PMID:23935843 SB505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC.|In Vivo:|SB505124 (5 mg/kg; i.p.) alone has no effect in C57Bl6 mice with A549 xenografts, but administration of SB-505124 with a single dose of Carboplatin (60 mg/kg) results in durable responses without the need for maintenance therapy in five animals.|References:|Onai T, Takai A, Setiamarga DH, Holland LZ. Essential role of Dkk3 for head formation by inhibiting Wnt/β-catenin and Nodal/Vg1 signaling pathways in the basal chordate amphioxus. Evol Dev. 2012 Jul;14(4):338-50. doi: 10.1111/j.1525-142X.2012.00552.x. PubMed PMID: 22765205.Joseph C, Hunter MG, Sinclair KD, Robinson RS. The expression, regulation and function of secreted protein, acidic, cysteine-rich in the follicle-luteal transition. Reproduction. 2012 Sep;144(3):361-72. doi: 10.1530/REP-12-0099. Epub 2012 Jun 25. PubMed PMID: 22733805.Kocic J, Bugarski D, Santibanez JF. SMAD3 is essential for transforming growth factor-β1-induced urokinase type plasminogen activator expression and migration in transformed keratinocytes. Eur J Cancer. 2012 Jul;48(10):1550-7. doi: 10.1016/j.ejca.2011.06.043. Epub 2011 Jul 26. PubMed PMID: 21798735.Products are for research use only. Not for human use.|
