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AB287049

HS-1371

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MW 384.5 Da, Purity >98%. Potent RIP3 kinase inhibitor (IC₅₀ = 20.8 nM). It binds to the ATP binding pocket of RIP3 and inhibits ATP binding to prevent RIP3 enzymatic activity in vitro. It inhibits TNF-induced necroptosis but does not inhibit TNF-induced apoptosis, indicating that HS-1371 has a specific inhibitory effect on RIP3-mediated necroptosis via the suppression of RIP3 kinase activity.

View Alternative Names

ACTR-IB, ACV1B_HUMAN, ACVR 1B, ACVRLK 4, ALK tyrosine kinase receptor, ALK-4, ALK/EML4 fusion gene, included, ALK/NPM1 fusion gene, included, ALK_HUMAN, AUTS9, Activin A receptor type 1B, Activin A receptor type II like kinase 4, Activin A type 1B receptor, Activin A type IB receptor, Activin receptor type IB, Activin receptor type-1B, Activin receptor-like kinase 4, Anaplastic lymphoma kinase, Anaplastic lymphoma kinase Ki1, Angiopoietin-1 receptor, BFGFR, Basic fibroblast growth factor receptor 1, CD 246, CD202b, CD202b antigen, CD246 antigen, CD309, CD309 antigen, CD331, CEK, D249, EC 2.7.10.1, Eag-related protein 1, Endothelial tyrosine kinase, Endothelium specific receptor tyrosine kinase 2, Ether a go go related potassium channel protein, Ether-a-go-go-related gene potassium channel 1, Ether-a-go-go-related protein 1, FGFBR, FGFR1/PLAG1 fusion, FGFR1_HUMAN, FLFL2, FLG, FLJ31474, FLK-1, FLK1, mouse, homolog of, FLT-2, Fetal liver kinase 1, Fms-like gene, Fms-like tyrosine kinase 2, H-ERG, HBGFR, HGF receptor, HGF/SF receptor, HGFR, HH2, HRTFDS, Hepatocyte growth factor receptor, Hyk, KAL2, KCNH2_HUMAN, KI 1, KIAA1387, KRD1, Kdr, Kinase insert domain receptor, Kinase insert domain receptor (a type III receptor tyrosine kinase), Kv11.1, LQT 2, LTK_HUMAN, Leukocyte receptor tyrosine kinase, Leukocyte tyrosine kinase, Leukocyte tyrosine kinase receptor, Ly73, MET proto oncogene, receptor tyrosine kinase, MET_HUMAN, Met proto oncogene tyrosine kinase, Met proto-oncogene, Met proto-oncogene (hepatocyte growth factor receptor), N-SAM, NBLST 3, OGD, Oncogene MET, PP4R3 beta, PP4R3B, PPP4R3 Beta, PPP4R3B, PSY2, Potassium channel HERG, Potassium voltage gated channel subfamily H (eag related) member 2, Potassium voltage-gated channel subfamily H member 2, Protein Phosphatase 4, Regulatory Subunit 3 Beta,, Protein tyrosine kinase 1, Protein-tyrosine kinase receptor flk-1, Proto-oncogene c-Fgr, Proto-oncogene c-Met, RCCP2, SF receptor, SKR 2, SMEK homolog 2, SMEK homolog 2 suppressor of mek1, SMEK homolog 2 suppressor of mek1 (Dictyostelium), SQT1, Scatter factor receptor, Serine(threonine) protein kinase receptor R2, Serine/threonine-protein kinase receptor R2, Serine/threonine-protein phosphatase 4 regulatory subunit 3B, Soluble TIE2 variant 1, Soluble TIE2 variant 2, TCRZ, TEK tyrosine kinase endothelial, TFG/ALK, TIE2_HUMAN, TYK 1, Tek, Tunica interna endothelial cell kinase, Tyrosine kinase growth factor receptor, Tyrosine kinase with Ig and EGF homology domains-2, Tyrosine-protein kinase Met, Tyrosine-protein kinase receptor TEK, Tyrosine-protein kinase receptor TIE-2, VEGFR, VEGFR-2, VGFR2_HUMAN, VMCM, VMCM 1, Vascular endothelial growth factor receptor 2, Venous malformations multiple cutaneous and mucosal, Voltage gated potassium channel, subfamily H, member 2, Voltage-gated potassium channel subunit Kv11.1, anaplastic lymphoma kinase (Ki-1), anaplastic lymphoma receptor tyrosine kinase, bFGF-R-1, c met, eag homolog, fibroblast growth factor receptor 1, fms-related tyrosine kinase 2, hERG-1, hTIE 2, heparin-binding growth factor receptor, hydroxyaryl-protein kinase, mutant anaplastic lymphoma kinase, p140 TEK, smk1, soluble VEGFR2, tek tyrosine kinase

Key facts

CAS number

2158197-70-5

Purity

>98%

Form

Solid

form

Molecular weight

384.5 Da

Molecular formula

C<sub>2</sub><sub>4</sub>H<sub>2</sub><sub>4</sub>N<sub>4</sub>O

PubChem

134817449

Nature

Synthetic

Solubility

>10 mg/ml DMSO

Biochemical name

7-(1-(Piperidin-4-yl)-1h-pyrazol-4-yl)-4-(p-tolyloxy)quinoline

Biological description

Potent RIP3 kinase inhibitor (IC₅₀ = 20.8 nM). It binds to the ATP binding pocket of RIP3 and inhibits ATP binding to prevent RIP3 enzymatic activity in vitro. . It inhibits TNF-induced necroptosis but does not inhibit TNF-induced apoptosis, indicating that HS-1371 has a specific inhibitory effect on RIP3-mediated necroptosis via the suppression of RIP3 kinase activity.

Canonical smiles

CC1=CC=C(C=C1)OC2=C3C=CC(=CC3=NC=C2)C4=CN(N=C4)C5CCNCC5

InChi

InChI=1S/C24H24N4O/c1-17-2-5-21(6-3-17)29-24-10-13-26-23-14-18(4-7-22(23)24)19-15-27-28(16-19)20-8-11-25-12-9-20/h2-7,10,13-16,20,25H,8-9,11-12H2,1H3

InChiKey

VPVLPCIBKVWFDT-UHFFFAOYSA-N

IUPAC Name

4-(4-methylphenoxy)-7-(1-piperidin-4-ylpyrazol-4-yl)quinoline

Product details

This product is manufactured by BioVision, an Abcam company and was previously called B2430 HS-1371. B2430-5 is the same size as the 5 mg size of ab287049.

Properties and storage information

Shipped at conditions
Blue Ice
Appropriate long-term storage conditions
-20°C

Supplementary information

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

ALK (Anaplastic Lymphoma Kinase) LTK (Leukocyte Tyrosine Kinase) VEGF Receptor 2 (Vascular Endothelial Growth Factor Receptor 2) FGFR1 (Fibroblast Growth Factor Receptor 1) Met (c-Met) TIE2 Activin A Receptor Type IB (ALK-4) H-ERG (Human Ether-a-go-go-Related Gene) and SMEK2 are of high importance in various cellular processes. These targets have different alternative names and vary in molecular masses. For example ALK is a receptor tyrosine kinase with a prominent role in neuronal tissue while H-ERG a potassium ion channel primarily contributes to the cardiac tissue. Each target plays important roles in specific signaling pathways and is expressed throughout different tissues impacting diverse cellular functions.
Biological function summary

These targets operate within intricate cellular networks that include signal transduction and ion channel regulation. ALK MET and VEGF Receptor 2 partake in receptor-mediated pathways that guide cell proliferation and angiogenesis while H-ERG controls cardiac repolarization by mediating potassium flow. The SMEK2 protein is part of a protein phosphatase complex influencing various signal transduction pathways. These molecular players interact with cellular machinery to regulate development response to environmental stimuli and maintenance of cellular homeostasis.

Pathways

ALK MET and VEGF Receptor 2 are fundamental in the PI3K-AKT and MAPK signaling pathways influencing cell growth and survival. These proteins often interact with other kinases to transmit extracellular signals into proper cellular responses. MET also integrates within crosstalk of the HGF signaling pathway collaborating with partners like beta-catenin. These pathways illustrate the dynamic role of these targets in cellular signaling linking them to other key proteins and metabolites.

Abnormalities in ALK MET and FGFR1 are associated with cancer while H-ERG dysfunction often leads to cardiac arrhythmias like Long QT syndrome. ALK fusions and mutations trigger tumorigenesis in various cancers including lung cancer where it interacts with EGFR and KRAS mutations. Meanwhile aberrations in H-ERG contribute to lethal cardiac conditions such as Torsades de Pointes through its involvement with ion channel proteins. Understanding these targets aids in addressing disease pathogenesis and guiding therapeutic development.

Product protocols

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