LJH685 - 10mM in DMSO, high purity , CAS No.1627710-50-2

  • 10mM in DMSO
Item Number
L421986
Grouped product items
SKUSizeAvailabilityPrice Qty
L421986-1ml
1ml
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$233.90

S6 Kinase Inhibitors

Basic Description

SynonymsLJH685 | 1627710-50-2 | LJH-685 | 2,6-difluoro-4-[4-[4-(4-methylpiperazin-1-yl)phenyl]pyridin-3-yl]phenol | CHEMBL3604793 | 27CZQ807C1 | 2,6-Difluoro-4-{4-[4-(4-Methylpiperazin-1-Yl)phenyl]pyridin-3-Yl}phenol | Phenol, 2,6-difluoro-4-(4-(4-(4-methyl-1-piperazinyl)pheny
Specifications & Purity10mM in DMSO
Biochemical and Physiological MechanismsLJH685 is a potent pan-RSK inhibitor with IC50 of 6 nM, 5 nM and 4 nM for RSK1, RSK2, and RSK3, respectively.
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
Product Description

Information

LJH685 LJH685 is a potent pan- RSK inhibitor with IC50 of 6 nM, 5 nM and 4 nM for RSK1, RSK2, and RSK3, respectively.

Targets

RSK3 (Cell-free assay); RSK2 (Cell-free assay); RSK1 (Cell-free assay) 4 nM; 5 nM; 6 nM

In vitro

LJH685 modulates YB1 phosphorylation by potently and selectively inhibiting RSK in cells. In MAPK pathway–dependent cancer cell lines, LJH685 shows antiproliferative effects, and causes cell-cycle regulation and apoptosis induction.

Cell Research(from reference)

Cell lines:Calu6, NCI-H2122, NCI-H358, NCI-H727, NCI-H2087, SW620, SW480, HT29, Capan-2, MiaPaCa2, SW1990, Panc02.03, MDA-MB-231, A375, G361, Colo205, Malme3M, WM1799, WM983B and WM266-4 cells 

Concentrations:~100 μM 

Incubation Time:72 h 

Associated Targets(Human)

RPS6KA1 Tchem Ribosomal protein S6 kinase alpha-1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RPS6KA2 Tchem Ribosomal protein S6 kinase alpha-2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RPS6KA3 Tchem Ribosomal protein S6 kinase alpha-3 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha 1 (2796 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RPS6KA2 Tchem Ribosomal protein S6 kinase alpha 2 (2184 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RPS6KA3 Tchem Ribosomal protein S6 kinase alpha 3 (4284 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK293 (82097 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HCC1806 (544 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MOLM-13 (2241 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver microsome (341 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rps6ka3 Ribosomal protein S6 kinase alpha-3 (39 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 2,6-difluoro-4-[4-[4-(4-methylpiperazin-1-yl)phenyl]pyridin-3-yl]phenol
INCHI InChI=1S/C22H21F2N3O/c1-26-8-10-27(11-9-26)17-4-2-15(3-5-17)18-6-7-25-14-19(18)16-12-20(23)22(28)21(24)13-16/h2-7,12-14,28H,8-11H2,1H3
InChi Key IKUFKDGKRLMXEX-UHFFFAOYSA-N
Canonical SMILES CN1CCN(CC1)C2=CC=C(C=C2)C3=C(C=NC=C3)C4=CC(=C(C(=C4)F)O)F
Isomeric SMILES CN1CCN(CC1)C2=CC=C(C=C2)C3=C(C=NC=C3)C4=CC(=C(C(=C4)F)O)F
PubChem CID 73010393
Molecular Weight 381.42

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