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S8822

Sigma-Aldrich

SB-525334

≥98% (HPLC), solid, ALK5 inhibitor

Sinônimo(s):

6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline

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About This Item

Fórmula empírica (Notação de Hill):
C21H21N5
Número CAS:
356559-20-1
Peso molecular:
343.42
Número MDL:
MFCD11045307
Código UNSPSC:
12352200
ID de substância PubChem:
329824610
NACRES:
NA.77

product name

SB-525334, ≥98% (HPLC)

Ensaio

≥98% (HPLC)

forma

solid

cor

yellow

solubilidade

DMSO: ≥20 mg/mL

originador

GlaxoSmithKline

temperatura de armazenamento

2-8°C

cadeia de caracteres 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)

chave InChI

DKPQHFZUICCZHF-UHFFFAOYSA-N

Aplicação

SB-525334 was used to study TGFβ1-mediated human trophoblast differentiation.7

Ações bioquímicas/fisiológicas

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.

Características e benefícios

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Equipamento de proteção individual

dust mask type N95 (US), Eyeshields, Faceshields, Gloves

Certificados de análise (COA)

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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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