A selective and potent inhibitor of RSKs (IC50 = 4-13 nM for RSK isoforms 1-3); reduces phosphorylation of YB1 in MDA-MB-231 cells bearing activating mutations in the MAPK signaling pathway (EC50 = 0.21 μM); reduces H358 growth in soft agar and colony forming assays.

LJI308 – 10 mg

Brand:
Cayman
CAS:
1627709-94-7
Storage:
-20
UN-No:
Non-Hazardous - /

LJI308 is a selective and potent inhibitor of the p90 ribosomal S6 kinase (RSK) family with IC50 values ranging from 4 to 13 nM for RSK isoforms 1-3.{33573,39058} In a panel of 442 kinases, LJI308 is selective for RSK1, RSK3, and RSK4. It also inhibits S6K1, MEK4, and HIP in the low micromolar range but had no effect on other kinases tested.{33573} LJI308 also reduces phosphorylation of Y-box-binding protein (YB1) in MDA-MB-231 cells bearing activating mutations in the MAPK signaling pathway (EC50 = 0.21 μM) and reduces H358 growth in soft agar and colony forming assays.  

 

Available on backorder

Add to quotes
SKU: 19924 - Category:

Description

A selective and potent inhibitor of RSKs (IC50 = 4-13 nM for RSK isoforms 1-3); reduces phosphorylation of YB1 in MDA-MB-231 cells bearing activating mutations in the MAPK signaling pathway (EC50 = 0.21 μM); reduces H358 growth in soft agar and colony forming assays. ,

Formal name: 2,6-difluoro-4-[4-[4-(4-morpholinyl)phenyl]-3-pyridinyl]-phenol

Synonyms: 

Molecular weight: 368.4

CAS: 1627709-94-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Kinase Inhibitors|S6K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling||Research Area|Cancer|Cell Signaling|S6K Signaling||Research Area|Cell Biology|Cell Signaling

Related products

  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 50 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 100 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 50 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 50 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 100 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 100 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page