L6293
LY-364947
≥98% (HPLC), Transforming Growth Factor-β Type I receptor kinase (ALK5) inhibitor, powder
別名:
4-[3-(2-ピリジニル)-1H-ピラゾール-4-イル]-キノリン, HTS 466284, トランスフォーミング増殖因子-β I型受容体キナーゼ阻害剤
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この商品について
実験式（ヒル表記法）:
C17H12N4
CAS番号:
分子量:
272.30
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
製品名
LY-364947, ≥98% (HPLC)
SMILES string
c1ccc(nc1)-c2n[nH]cc2-c3ccnc4ccccc34
InChI key
IBCXZJCWDGCXQT-UHFFFAOYSA-N
InChI
1S/C17H12N4/c1-2-6-15-13(5-1)12(8-10-19-15)14-11-20-21-17(14)16-7-3-4-9-18-16/h1-11H,(H,20,21)
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Gene Information
human ... TGFBR1(7046)
Biochem/physiol Actions
LY-364947は、IC50 = 59 nMのトランスフォーミング増殖因子-β I型受容体キナーゼ（TGF-β RI、ALK5）の選択的ATP競合阻害剤です。関連キナーゼでははるかに効力が低く、TGF-β RIIではIC50 = 400 nM、MAPキナーゼシグナル経路のキナーゼであり、TGF-β RIIと密接に関連する混合系統キナーゼ-7（MLK-7）ではIC50 = 1400 nMです。LY-364947は、NIH 3T3マウス線維芽細胞のTGF-β-依存性細胞増殖（IC50 = 81 nM）を阻害します。
トランスフォーミング増殖因子-β I型受容体キナーゼ（ALK5）阻害剤
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges
Hong-yu Li et al.
Journal of medicinal chemistry, 49(6), 2138-2142 (2006-03-17)
Novel dihydropyrrolopyrazole-substituted benzimidazoles were synthesized and evaluated in vitro as inhibitors of transforming growth factor-beta type I receptor (TGF-beta RI), TGF-beta RII, and mixed lineage kinase-7 (MLK-7). These compounds were found to be potent TGF-beta RI inhibitors and selective versus
J Scott Sawyer et al.
Journal of medicinal chemistry, 46(19), 3953-3956 (2003-09-05)
Pyrazole-based inhibitors of the transforming growth factor-beta type I receptor kinase domain (TbetaR-I) are described. Examination of the SAR in both enzyme- and cell-based in vitro assays resulted in the emergence of two subseries featuring differing selectivity versus p38 MAP
Sheng-Ru Shiou et al.
The Journal of biological chemistry, 281(45), 33971-33981 (2006-09-09)
Metastasis is a primary cause of mortality due to cancer. Early metastatic growth involves both a remodeling of the extracellular matrix surrounding tumors and invasion of tumors across the basement membrane. Up-regulation of extracellular matrix degrading proteases such as urokinase
Suzanne Vanhauwaert et al.
PloS one, 9(10), e109091-e109091 (2014-10-14)
The selection and validation of stably expressed reference genes is a critical issue for proper RT-qPCR data normalization. In zebrafish expression studies, many commonly used reference genes are not generally applicable given their variability in expression levels under a variety
Khaled Nassar et al.
Experimental eye research, 123, 72-86 (2014-04-20)
This study evaluates the use of the TGF-β receptor 1 inhibitor LY-364947 (LY) to prevent proliferative vitreoretinopathy (PVR). For the in vitro experiments Human Tenon's Fibroblasts (HTFs) and retinal pigment epithelial (RPE) cells were treated with different concentrations of LY
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