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S8822

Sigma-Aldrich

SB-525334

≥98% (HPLC), solid, ALK5 inhibitor

Synonyme(s) :

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

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About This Item

Formule empirique (notation de Hill):
C21H21N5
Numéro CAS:
356559-20-1
Poids moléculaire :
343.42
Numéro MDL:
MFCD11045307
Code UNSPSC :
12352200
ID de substance PubChem :
329824610
Nomenclature NACRES :
NA.77

product name

SB-525334, ≥98% (HPLC)

Pureté

≥98% (HPLC)

Forme

solid

Couleur

yellow

Solubilité

DMSO: ≥20 mg/mL

Auteur

GlaxoSmithKline

Température de stockage

2-8°C

Chaîne 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)

Clé InChI

DKPQHFZUICCZHF-UHFFFAOYSA-N

Application

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

Actions biochimiques/physiologiques

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.

Caractéristiques et avantages

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Équipement de protection individuelle

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

Certificats d'analyse (COA)

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Neel I Nissen et al.
Cancers, 14(3) (2022-02-16)
The use of novel tools to understand tumour-fibrosis in pancreatic ductal adenocarcinoma (PDAC) and novel anti-fibrotic treatments are highly needed. We established a pseudo-3D in vitro model including humane pancreatic fibroblasts (PFs) and pancreatic cancer-associated fibroblasts (CAFs) in combination with
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
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
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
Robert B Good et al.
BMC biomedical engineering, 1, 14-14 (2019-06-28)
Excessive extracellular matrix (ECM) deposition is a hallmark feature in fibrosis and tissue remodelling diseases. Typically, mesenchymal cells will produce collagens under standard 2D cell culture conditions, however these do not assemble into fibrils. Existing assays for measuring ECM production
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