L6293
LY-364947
≥98% (HPLC)
동의어(들):
4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-quinoline, HTS 466284, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C17H12N4
CAS Number:
Molecular Weight:
272.30
MDL number:
UNSPSC 코드:
51111800
PubChem Substance ID:
NACRES:
NA.77
추천 제품
Quality Level
분석
≥98% (HPLC)
양식
powder
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
2-8°C
SMILES string
c1ccc(nc1)-c2n[nH]cc2-c3ccnc4ccccc34
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)
InChI key
IBCXZJCWDGCXQT-UHFFFAOYSA-N
유전자 정보
human ... TGFBR1(7046)
생화학적/생리학적 작용
LY-364947 is a selective, ATP-competitive inhibitor of Transforming Growth Factor-β Type I receptor kinase (TGF-β RI, ALK5) with IC50 = 59 nM. It is much less potent at related kinases, with IC50 = 400 nM for TGF-β RII and IC50 = 1400 nM for mixed lineage kinase-7 (MLK-7), a kinase in the MAP kinase signal pathway and closely related to TGF-β RII. LY-364947 inhibits TGF-β-dependent cellular growth (IC50 = 81 nM) in NIH 3T3 mouse fibroblasts.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
개인 보호 장비
Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges
이미 열람한 고객
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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