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S8822
SB-525334
≥98% (HPLC), solid, ALK5 inhibitor
Synonim(y):
6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline
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About This Item
Wzór empiryczny (zapis Hilla):
C21H21N5
Numer CAS:
Masa cząsteczkowa:
343.42
Numer MDL:
Kod UNSPSC:
12352200
Identyfikator substancji w PubChem:
NACRES:
NA.77
Polecane produkty
Nazwa produktu
SB-525334, ≥98% (HPLC)
Próba
≥98% (HPLC)
Formularz
solid
kolor
yellow
rozpuszczalność
DMSO: ≥20 mg/mL
inicjator
GlaxoSmithKline
temp. przechowywania
2-8°C
ciąg SMILES
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)
Klucz InChI
DKPQHFZUICCZHF-UHFFFAOYSA-N
Zastosowanie
SB-525334 was used to study TGFβ1-mediated human trophoblast differentiation.7
Działania biochem./fizjol.
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.
Cechy i korzyści
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
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Kod klasy składowania
11 - Combustible Solids
Klasa zagrożenia wodnego (WGK)
WGK 3
Środki ochrony indywidualnej
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
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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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