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S2075

Src Inhibitor-1

Name: Src Inhibitor-1
Brand: SIGMA

≥98% (HPLC), Src kinase inhibitor, powder

Synonym(s):

4-(4′-Phenoxyanilino)-6,7-dimethoxyquinazoline, 6,7-Dimethoxy-N-(4-phenoxyphenyl)-4-quinazolinamine, SKI-1, Src-l1

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About This Item

Empirical Formula (Hill Notation):

C₂₂H₁₉N₃O₃

CAS Number:

179248-59-0

Molecular Weight:

373.40

UNSPSC Code:

12352200

PubChem Substance ID:

329824504

NACRES:

NA.77

MDL number:

MFCD01815300

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Storage condition:

desiccated

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Product Name

Src Inhibitor-1, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white

solubility

DMSO: >10 mg/mL

storage temp.

2-8°C

SMILES string

COc1cc2ncnc(Nc3ccc(Oc4ccccc4)cc3)c2cc1OC

InChI

1S/C22H19N3O3/c1-26-20-12-18-19(13-21(20)27-2)23-14-24-22(18)25-15-8-10-17(11-9-15)28-16-6-4-3-5-7-16/h3-14H,1-2H3,(H,23,24,25)

InChI key

DMWVGXGXHPOEPT-UHFFFAOYSA-N

Related Categories

Bioactive Small Molecule Inhibitors

Bioactive Small Molecules

Application

Src Inhibitor-1 may be used in Src kinase-mediated cell signaling studies.

Biochem/physiol Actions

Src Inhibitor-1 is a potent, competitve dual site (both the ATP- and peptide-binding) Src kinase inhibitor.

Apart from Src kinase, some Src inhibitors also inhibit the activity of Abl kinase, Lck, Csk and Yes proteins and are therefore being explored as viable anti-cancer drug options.

Src Inhibitor-1 is a potent, competitve dual site (both the ATP- and peptide-binding) Src kinase inhibitor. Src Inhibitor-1 is one of the "gold standards" for Src kinase inhibition. It has been shown to use PP1 or PP2 in parallel with Src-I1 to inhbit Src family kinases. Src Inhibitor-1 is a selective, competitive inhibitor of Src family of tyrosine kinases (IC₅₀ = 44 nM and 88 nM for Src and Lck, respectively). Src Inhibitor-1 Inhibits VEGFR2 and c-fms tyrosine kinases at much higher concentrations (IC₅₀ = 0.32 μM and 30 μM, respectively).

Features and Benefits

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Storage Class

11 - Combustible Solids

wgk

WGK 3

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7-Alkoxy-4-phenylamino-3-quinolinecar-bonitriles as dual inhibitors of Src and Abl kinases.

Diane H Boschelli et al.

Journal of medicinal chemistry, 47(7), 1599-1601 (2004-03-19)

We previously reported that several 7-alkoxy-4-phenylamino-3-quinolinecarbonitriles were potent inhibitors of Src kinase activity. We disclose here a new highly efficient and versatile route to these compounds, which are also potent inhibitors of Abl kinase.

uPAR isoform 2 forms a dimer and induces severe kidney disease in mice.

Changli Wei et al.

The Journal of clinical investigation, 129(5), 1946-1959 (2019-02-08)

Soluble urokinase plasminogen activator receptor (suPAR) is an immune-derived circulating signaling molecule that has been implicated in chronic kidney disease, such as focal segmental glomerulosclerosis (FSGS). Typically, native uPAR (isoform 1) translates to a 3-domain protein capable of binding and

Altering microtubule dynamics is synergistically toxic with spindle assembly checkpoint inhibition.

Klaske M Schukken et al.

Life science alliance, 3(2) (2020-01-26)

Chromosomal instability (CIN) and aneuploidy are hallmarks of cancer. As most cancers are aneuploid, targeting aneuploidy or CIN may be an effective way to target a broad spectrum of cancers. Here, we perform two small molecule compound screens to identify

Periplocin promotes wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase.

Lei Chen et al.

Phytomedicine : international journal of phytotherapy and phytopharmacology, 57, 72-83 (2019-01-23)

Periploca forrestii(PF) is mainly utilized for treatment of arthritis and traumatic injury historically. We had previously demonstrated that a fraction rich in cardiotonic steroids isolated from PF had the potential to facilitate wound healing. However, the exact material basis and

Cysteine-Mediated Redox Regulation of Cell Signaling in Chondrocytes Stimulated With Fibronectin Fragments.

Scott T Wood et al.

Arthritis & rheumatology (Hoboken, N.J.), 68(1), 117-126 (2015-09-01)

Oxidative posttranslational modifications of intracellular proteins can potentially regulate signaling pathways relevant to cartilage destruction in arthritis. In this study, oxidation of cysteine residues to form sulfenic acid (S-sulfenylation) was examined in osteoarthritic (OA) chondrocytes and investigated in normal chondrocytes

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Articles

Src Family Kinases Overview

Src is the original member of a group of non-receptor protein-tyrosine kinases termed the Src family kinases (SFKs). Learn about the SFKs that, in humans, consist of eight members, a small group of atypical members, and two related kinases.

Discover Bioactive Small Molecules for Kinase Phosphatase Biology

Global Trade Item Number

SKU	GTIN
S2075-5MG	04061836917388
S2075-25MG	04061833221266

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