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AB120839

Src Kinase Inhibitor I (SKI-1)

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(6 Publications)

MW 373.4 Da, Purity >98%. Potent, selective and dual site Src family tyrosine kinase inhibitor (IC50 values are 44 and 88 nM for Src and Lck, respectively). Cell-permeable, reversible and ATP-competitive. Interacts with both ATP and peptide-binding sites. Additionally inhibits VEGFR2 and C-fms (IC50 values are 0.32 and 30 μM, respectively). Induces apoptosis.

View Alternative Names

CARD 3, CARD carrying kinase, CARD containing ICE associated kinase, CARD containing interleukin 1 beta converting enzyme (ICE) associated kinase, CARD-containing IL-1 beta ICE-kinase, CARD-containing interleukin-1 beta-converting enzyme-associated kinase, CARDIAK, CLARP kinase, GIG 30, Growth inhibiting gene 30, RICK, RIP-like-interacting CLARP kinase, RIPK2_HUMAN, Receptor interacting protein (RIP) like interacting caspase like apoptosis regulatory protein (CLARP) kinase, Receptor interacting serine threonine kinase 2, Receptor-interacting protein 2, Receptor-interacting serine/threonine-protein kinase 2, TNFRSF, Tyrosine-protein kinase RIPK2, UNQ277/PRO314/PRO34092

2 Images
Chemical Structure - Src Kinase Inhibitor I (SKI-1) (AB120839)
  • Chemical Structure

Lab

Chemical Structure - Src Kinase Inhibitor I (SKI-1) (AB120839)

2D chemical structure image of ab120839, Src Kinase Inhibitor I (SKI-1)

Functional Studies - Src Kinase Inhibitor I (SKI-1) (AB120839)
  • FuncS

Unknown

Functional Studies - Src Kinase Inhibitor I (SKI-1) (AB120839)

ab11512 staining E cadherin in SW480 cells treated with Src Kinase Inhibitor I (SKI-1) (ab120839), by ICC/IF. Increase of E cadherin expression correlates with increased concentration of Src Kinase Inhibitor I (SKI-1), as described in literature.
The cells were incubated at 37°C for 24h in media containing different concentrations of ab120839 (Src Kinase Inhibitor I (SKI-1)) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab11512 (5 µg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight® 488 anti-rat polyclonal antibody (ab98386) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.

Key facts

CAS number

179248-59-0

Purity

>98%

Form

Solid

form

Molecular weight

373.4 Da

Molecular formula

C<sub>2</sub><sub>2</sub>H<sub>1</sub><sub>9</sub>N<sub>3</sub>O<sub>3</sub>

PubChem

1474853

Nature

Synthetic

Solubility

Soluble in DMSO to 50 mM

Biochemical name

Src Kinase Inhibitor I

Biological description

Potent, selective and dual site Src family tyrosine kinase inhibitor (IC50 values are 44 and 88 nM for Src and Lck, respectively). Cell-permeable, reversible and ATP-competitive. Interacts with both ATP and peptide-binding sites. Additionally inhibits VEGFR2 and C-fms (IC50 values are 0.32 and 30 μM, respectively). Induces apoptosis.

Canonical smiles

COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=C(C=C3)OC4=CC=CC=C4)OC

InChi

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)

InChiKey

DMWVGXGXHPOEPT-UHFFFAOYSA-N

IUPAC Name

6,7-dimethoxy-N-(4-phenoxyphenyl)quinazolin-4-amine

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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
+4°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

RIP2 also known as receptor-interacting serine/threonine-protein kinase 2 or RICK is a protein with roles in signal transduction. It functions mechanically as a kinase which means it adds a phosphate group to other proteins impacting their activity and stability. RIP2 weighs about 61 kDa and is mostly expressed in immune system-related tissues such as spleen thymus peripheral blood leukocytes and bone marrow. As a kinase RIP2 is an action part in the cellular response to external stimuli.
Biological function summary

RIP2 interacts with key components of the immune signaling network. It forms part of a complex with other proteins like nucleotide-binding oligomerization domain (NOD) proteins influencing immune responses. By binding to NOD1 and NOD2 RIP2 modulates inflammatory signaling pathways leading to the activation of NF-kB and the production of inflammatory cytokines. This protein helps regulate the body's defense against bacterial infections and influences inflammation processes.

Pathways

RIP2 plays an integral role in the NOD-like receptor signaling pathway and is also involved in toll-like receptor signaling. In its pathways RIP2 interacts closely with proteins like IKK complexes and the Tak1 complex orchestrating signaling cascades leading to the activation of NF-kB and MAPK pathways. These pathways are essential for instigating the immune response and managing inflammatory signals highlighting how RIP2 acts as a pivotal mediator in these biological routes.

Mutations or dysregulation of RIP2 are linked to inflammatory diseases and immune disorders such as Crohn's disease and Blau syndrome. RIP2's involvement in these conditions often involves its interaction with NOD2 influencing the improper immune response seen in these diseases. Changing RIP2 activity presents a target for developing kinase inhibitors that might help to manage inflammation and immune system disorders by modulating its signaling activity.
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Product protocols

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Publications (6)

Recent publications for all applications. Explore the full list and refine your search

Cell reports 24:987-1000.e7 PubMed30044993

2018

Hypertonic Stress Causes Cytoplasmic Translocation of Neuronal, but Not Astrocytic, FUS due to Impaired Transportin Function.

Applications

Unspecified application

Species

Unspecified reactive species

Eva-Maria Hock,Zuzanna Maniecka,Marian Hruska-Plochan,Stefan Reber,Florent Laferrière,Sonu Sahadevan M K,Helena Ederle,Lauren Gittings,Lucas Pelkmans,Luc Dupuis,Tammaryn Lashley,Marc-David Ruepp,Dorothee Dormann,Magdalini Polymenidou

PloS one 12:e0188645 PubMed29190738

2017

Cervical HSV-2 infection causes cervical remodeling and increases risk for ascending infection and preterm birth.

Applications

Unspecified application

Species

Unspecified reactive species

Devin McGee,Arianna Smith,Sharra Poncil,Amanda Patterson,Alison I Bernstein,Karen Racicot

Journal of immunology (Baltimore, Md. : 1950) 199:3261-3269 PubMed28954885

2017

Green Tea Polyphenol EGCG Upregulates Tollip Expression by Suppressing Elf-1 Expression.

Applications

Unspecified application

Species

Unspecified reactive species

Motofumi Kumazoe,Mai Yamashita,Yuki Nakamura,Kanako Takamatsu,Jaehoon Bae,Shuya Yamashita,Shuhei Yamada,Hiroaki Onda,Takashi Nojiri,Kenji Kangawa,Hirofumi Tachibana

Cell adhesion & migration 12:286-298 PubMed28678601

2017

Adhesion structures in leukemia cells and their regulation by Src family kinases.

Applications

Unspecified application

Species

Unspecified reactive species

Pavla Röselová,Adam Obr,Aleš Holoubek,Dana Grebeňová,Kateřina Kuželová

Journal of medical virology 89:1852-1860 PubMed28480962

2017

Human papillomavirus type 16 E6 oncoprotein promotes proliferation and invasion of non-small cell lung cancer cells through Toll-like receptor 3 signaling pathway.

Applications

BL

Species

Human

Xia Wang,Zhiqiang Zhang,Huimin Cao,Wenyi Niu,Mingying Li,Xiu'e Xi,Jing Wang

Cell death and differentiation 23:1749-1764 PubMed27518433

2016

Transthyretin provides trophic support via megalin by promoting neurite outgrowth and neuroprotection in cerebral ischemia.

Applications

Unspecified application

Species

Unspecified reactive species

J R Gomes,R S Nogueira,M Vieira,S D Santos,J P Ferraz-Nogueira,J B Relvas,M J Saraiva
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