An inducer of ferroptosis; inhibits glutamate release in human CCF-STTG1 astrocytoma cells (IC50 = 30 nM)

Imidazole Ketone Erastin – 1 mg

Brand:
Cayman
CAS:
1801530-11-9
Storage:
-20
UN-No:
Non-Hazardous - /

Imidazole ketone erastin is an inducer of ferroptosis.{50040} It inhibits glutamate release in human CCF-STTG1 astrocytoma cells (IC50 = 30 nM), indicating inhibition of the system xc- cystine/glutamate transporter.{43385} Imidazole ketone erastin increases production of lipid reactive oxygen species (ROS) in SUDHL6 diffuse large B cell lymphoma (DLBCL) cells in a concentration-dependent manner, as well as reduces glutathione (GSH) levels in these cells (IC50 = 34 nM).{50040} It inhibits the growth of HT-1080 fibrosarcoma cells (GI50 = 310 nM) as well as HRASG12V-overexpressing BJeLR cells (IC50 = 3 nM).{43385} Imidazole ketone erastin (23 and 40 mg/kg) reduces tumor growth in an SUDHL6 mouse xenograft model.{50040}  

 

Available on backorder

Add to quotes
SKU: 27088 - 1 mg Category:

Description

An inducer of ferroptosis; inhibits glutamate release in human CCF-STTG1 astrocytoma cells (IC50 = 30 nM), indicating inhibition of the system xc- cystine/glutamate transporter; increases production of lipid ROS in SUDHL6 DLBCL cells in a concentration-dependent manner, as well as reduces GSH levels in these cells (IC50 = 34 nM); inhibits the growth of HT-1080 fibrosarcoma cells (GI50 = 310 nM) as well as HRASG12V-overexpressing BJeLR cells (IC50 = 3 nM); reduces tumor growth in an SUDHL6 mouse xenograft model at 23 and 40 mg/kg

Formal name: 2-[[4-[2-(4-chlorophenoxy)acetyl]-1-piperazinyl]methyl]-3-[5-[2-(1H-imidazol-1-yl)acetyl]-2-(1-methylethoxy)phenyl]-4(3H)-quinazolinone

Synonyms:  IKE

Molecular weight: 655.1

CAS: 1801530-11-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ox Stress Reagents||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cancer|Tumor Microenvironment||Research Area|Cell Biology|Cell Death|Ferroptosis||Research Area|Oxidative Stress & Reactive Species|Lipid Peroxidation||Research Area|Oxidative Stress & Reactive Species|Pro-oxidant Activity||Research Area|Oxidative Stress & Reactive Species|Reactive Oxygen||Research Area|Oxidative Stress & Reactive Species|Reactive Sulfur|Glutathione

Related products

  • 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 – 100 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 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 1 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 1 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 500 µg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 500 µg

    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) – 500 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 - 500 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page