S8822

SB-525334

Name: SB-525334
Brand: SIGMA

≥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

UNSPSC Code:

12352200

PubChem Substance ID:

329824610

NACRES:

NA.77

MDL number:

MFCD11045307

Nom du produit

SB-525334, ≥98% (HPLC)

SMILES string

Cc1cccc(n1)-c2[nH]c(nc2-c3ccc4nccnc4c3)C(C)(C)C

InChI key

DKPQHFZUICCZHF-UHFFFAOYSA-N

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)

assay

≥98% (HPLC)

form

solid

color

yellow

solubility

DMSO: ≥20 mg/mL

originator

GlaxoSmithKline

storage temp.

2-8°C

Quality Level

100

Catégories apparentées

Inhibiteurs bioactifs à base de petites molécules

Petites molécules bioactives

Application

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

Biochem/physiol Actions

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.

Features and Benefits

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

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

ppe

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

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Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis.

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

Collagen Biomarkers Quantify Fibroblast Activity In Vitro and Predict Survival in Patients with Pancreatic Ductal Adenocarcinoma.

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

Activin-like kinase 5 (ALK5) mediates abnormal proliferation of vascular smooth muscle cells from patients with familial pulmonary arterial hypertension and is involved in the progression of experimental pulmonary arterial hypertension induced by monocrotaline.

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

Tumor-specific efficacy of transforming growth factor-beta RI inhibition in Eker rats.

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

Optimizing Soluble Cues for Salivary Gland Tissue Mimetics Using a Design of Experiments (DoE) Approach.

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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