A stable analog of PFT-α

Cyclic Pifithrin-α (hydrobromide) – 50 mg

Brand:
Cayman
CAS:
511296-88-1
Storage:
-20
UN-No:
Non-Hazardous - /

Pifithrin-α (PFT-α; Item No. 13326) is a reversible inhibitor of p53-dependent transcription and apoptosis.{17259} Cyclic PFT-α, also known as PFT-β, is a stable analog of PFT-α, formed by the condensation of pifithrin-α in solution.{23585} It inhibits the growth of the cancer cell lines IGROV-1, A2780, and HCT116 (IC50 = 23, 77, and 103 μM, respectively).{23585,23586} At doses lower than those that inhibit growth, cyclic PFT-α induces autophagy in HCT116 cells and sensitizes IGROV-1 and H460 cells to anti-microtubule agents.{23579,23580} In addition, 10 μM cyclic PFT-α blocks p53-dependent protection from DNA damage, induced by hydrogen peroxide or ultraviolet radiation, in melanocytes.{23581}  

 

Add to quotes
SKU: - Category:

Description

A stable analog of PFT-α, formed by the condensation of PFT-α in solution; inhibits the growth of the cancer cell lines IGROV-1, A2780, and HCT116 (IC50 = 23, 77, and 103 μM, respectively); induces autophagy in HCT116 cells and sensitizes IGROV-1 and H460 cells to anti-microtubule agents

Formal name: 5,6,7,8-tetrahydro-2-(4-methylphenyl)-imidazo[2,1-b]benzothiazole, monohydrobromide

Synonyms:  Cyclic PFT-α|PFT-β|Pifithrin-β

Molecular weight: 349.3

CAS: 511296-88-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer|Autophagy||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|DNA Damage and Repair||Research Area|Cancer|Transcription Factors|p53||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Cell Biology|Cytoskeleton & Motor Proteins||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|Autophagy||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

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 – 10 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 - 10 mg

    Available on backorder

    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
    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 – 5 mg

    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 - 5 mg

    Available on backorder

    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 25 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 - 25 mg

    Available on backorder

    Add to quotes
    View product page