Key Documents

LY-364947

Name: LY-364947
Brand: SIGMA

≥98% (HPLC), Transforming Growth Factor-β Type I receptor kinase (ALK5) inhibitor, powder

Synonym(s):

4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-quinoline, HTS 466284, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor

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About This Item

Empirical Formula (Hill Notation):

C₁₇H₁₂N₄

CAS Number:

396129-53-6

Molecular Weight:

272.30

UNSPSC Code:

51111800

PubChem Substance ID:

24724526

NACRES:

NA.77

MDL number:

MFCD00800758

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Pricing and availability is not currently available.

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Properties

Product Name

LY-364947, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

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

Gene Information

human ... TGFBR1(7046)

Description

Biochem/physiol Actions

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.

Transforming Growth Factor-β Type I receptor kinase (ALK5) inhibitor

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This Item	616454	SML2851	SML1643
Sigma-Aldrich L6293 LY-364947	Sigma-Aldrich 616454 TGF-β RI Kinase Inhibitor IV	Sigma-Aldrich SML2851 Galunisertib	Sigma-Aldrich SML1643 AS2444697
assay ≥98% (HPLC)	assay ≥97% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)
form powder	form solid	form powder	form powder
Quality Level 100	Quality Level 200	Quality Level 100	Quality Level 100
storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C	storage temp. 2-8°C
solubility DMSO: 2 mg/mL, clear	solubility DMSO: 20 mg/mL	solubility DMSO: 2 mg/mL, clear	solubility DMSO: 5 mg/mL, clear (warmed)
color white to beige	color pale yellow	color white to beige	color white to beige

Storage Class

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

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Certificates of Analysis (COA)

Lot/Batch Number

0000523219

0000331153

0000220801

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Expressed repeat elements improve RT-qPCR normalization across a wide range of zebrafish gene expression studies.

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

Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.

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

A TGF-β receptor 1 inhibitor for prevention of proliferative vitreoretinopathy.

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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Global Trade Item Number

SKU	GTIN
L6293-25MG	04061832434094
L6293-5MG	04061833958728

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