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S8822

SB-525334

Name: SB-525334
Brand: SIGMA

≥98% (HPLC), solid, ALK5 inhibitor

别名:

6-[2-叔-丁基-5-(6-甲基吡啶-2-基)-1H-咪唑-4-基]-喹喔啉

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About This Item

经验公式（希尔记法）:

C₂₁H₂₁N₅

CAS号:

356559-20-1

分子量:

343.42

MDL编号:

MFCD11045307

UNSPSC代码:

12352200

PubChem化学物质编号:

329824610

NACRES:

NA.77

product name

SB-525334, ≥98% (HPLC)

质量水平

100

检测方案

≥98% (HPLC)

形式

solid

颜色

yellow

溶解性

DMSO: ≥20 mg/mL

创始人

GlaxoSmithKline

储存温度

2-8°C

SMILES字符串

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)

InChI key

DKPQHFZUICCZHF-UHFFFAOYSA-N

应用

SB-525334已被用于研究TGFβ1介导的人滋养细胞分化。⁷

生化/生理作用

SB-525334在肾近端小管细胞中可阻断TGFβ1诱导的Smad2/3的激活。⁴ SB-525334可降低TGFβ1的敏感性，从而通过逆转肺动脉压而有益于肺动脉高血压。⁵ SB-525334可降低子宫平滑肌瘤等间充质肿瘤的发生率和大小。⁶

SB-525334是一种有效的激活素受体样激酶（ALK5）/I型TGFβ-受体激酶抑制剂，其 IC₅₀ = 14.3 nM。

特点和优势

该化合物由GlaxoSmithKline开发。要浏览其他药物开发化合物和批准的药物/候选药物列表，单击此处。

WGK

WGK 3

个人防护装备

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

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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

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

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

A high content, phenotypic 'scar-in-a-jar' assay for rapid quantification of collagen fibrillogenesis using disease-derived pulmonary fibroblasts.

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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