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S8822
SB-525334
≥98% (HPLC), solid, ALK5 inhibitor
Synonym(e):
6-[2-tert-butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline
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About This Item
Empirische Formel (Hill-System):
C21H21N5
CAS-Nummer:
Molekulargewicht:
343.42
MDL-Nummer:
UNSPSC-Code:
12352200
PubChem Substanz-ID:
NACRES:
NA.77
Empfohlene Produkte
Produktbezeichnung
SB-525334, ≥98% (HPLC)
Assay
≥98% (HPLC)
Form
solid
Farbe
yellow
Löslichkeit
DMSO: ≥20 mg/mL
Ersteller
GlaxoSmithKline
Lagertemp.
2-8°C
SMILES String
Cc1cccc(n1)-c2[nH]c(nc2-c3ccc4nccnc4c3)C(C)(C)C
InChI
1S/C21H21N5/c1-13-6-5-7-16(24-13)19-18(25-20(26-19)21(2,3)4)14-8-9-15-17(12-14)23-11-10-22-15/h5-12H,1-4H3,(H,25,26)
InChIKey
DKPQHFZUICCZHF-UHFFFAOYSA-N
Anwendung
SB-525334 was used to study TGFβ1-mediated human trophoblast differentiation.7
Biochem./physiol. Wirkung
SB-525334 blocks the activation of Smad2/3 induced by TGFβ1 in renal proximal tubule cells.4 The sensitivity of TGFβ1 is decreased by SB-525334 that benefits the pulmonary arterial hypertension condition by reversing the pulmonary arterial pressure.5 SB-525334 is reduces the tumor incidence and size of mesenchymal tumors such as uterine leiomyoma.6
SB-525334 is a potent activin receptor-like kinase (ALK5)/ type I TGFβ-receptor kinase inhibitor with IC50 = 14.3 nM.
SB-525334 is an ALK5/type I TGFβ-R kinase inhibitor.
Leistungsmerkmale und Vorteile
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
Lagerklassenschlüssel
11 - Combustible Solids
WGK
WGK 3
Persönliche Schutzausrüstung
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
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Eugene T Grygielko et al.
The Journal of pharmacology and experimental therapeutics, 313(3), 943-951 (2005-03-17)
SB-525334 (6-[2-tert-butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline) has been characterized as a potent and selective inhibitor of the transforming growth factor-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). The compound inhibited ALK5 kinase activity with an IC(50) of 14.3 nM and was approximately 4-fold less potent
Nicholas J Laping et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 13(10), 3087-3099 (2007-05-17)
Transforming growth factor beta (TGF-beta), which generally stimulates the growth of mesenchymally derived cells but inhibits the growth of epithelial cells, has been proposed as a possible target for cancer therapy. However, concerns have been raised that whereas inhibition of
Hiroyuki Higashiyama et al.
Experimental and molecular pathology, 83(1), 39-46 (2007-02-06)
Activin receptor-like kinase 5 (ALK5) is a type I receptor of transforming growth factor (TGF)-beta. ALK5 inhibition has been reported to attenuate the tissue fibrosis including pulmonary fibrosis, renal fibrosis and liver fibrosis. To elucidate the inhibitory mechanism of ALK5
Matthew Thomas et al.
The American journal of pathology, 174(2), 380-389 (2009-01-01)
Mutations in the gene for the transforming growth factor (TGF)-beta superfamily receptor, bone morphogenetic protein receptor II, underlie heritable forms of pulmonary arterial hypertension (PAH). Aberrant signaling via TGF-beta receptor I/activin receptor-like kinase 5 may be important for both the
Lindsay R Piraino et al.
Cells, 11(12) (2022-06-25)
The development of therapies to prevent or treat salivary gland dysfunction has been limited by a lack of functional in vitro models. Specifically, critical markers of salivary gland secretory phenotype downregulate rapidly ex vivo. Here, we utilize a salivary gland
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