An inhibitor of Cdk8 and Cdk19; inhibits Cdk8 (IC50s = 24-50 nM

Senexin B – 1 mg

Brand:
Cayman
CAS:
1449228-40-3
Storage:
-20
UN-No:
Non-Hazardous - /

Senexin B is an inhibitor of Cdk8 and Cdk19.{42922} It inhibits Cdk8 with IC50 values ranging from 24 to 50 nM, depending on the assay used. It selectively inhibits Cdk19 and Cdk8 by 98.6 and 97.8%, respectively, in a panel of greater than 450 kinases at 2 μM but does inhibit MAP4K2 and YSK4 by 69 and 59%, respectively. Senexin B (1.25-5 μM) inhibits cell growth in MCF-7, BT474, and T47D-ER/Luc breast cancer cells in estrogen-containing media in a concentration-dependent manner.{42923} It reduces tumor growth in an MCF-7 mouse xenograft model when administered at a dose of 100 mg/kg twice per day. Senexin B (1 and 1.5 μM) also inhibits RANKL-induced differentiation of murine bone marrow-derived macrophages (BMDMs) into osteoclasts.{42924} It increases the bone volume fraction and bone mineral density in injured tibiae in a rat model of cancellous bone injury and regeneration when administered locally at a dose of 1 μg.  

 

Available on backorder

Add to quotes
SKU: 28459 - 1 mg Category:

Description

An inhibitor of Cdk8 and Cdk19; inhibits Cdk8 (IC50s = 24-50 nM, depending on assay); selectively inhibits Cdk19 and Cdk8 by 98.6 and 97.8%, respectively, in a panel of >450 kinases at 2 μM but does inhibit MAP4K2 and YSK4 by 69 and 59%, respectively; inhibits cell growth in MCF-7, BT474, and T47D-ER/Luc breast cancer cells in estrogen-containing media at 1.25-5 μM; reduces tumor growth in an MCF-7 mouse xenograft model at 100 mg/kg twice per day; inhibits RANKL-induced differentiation of murine BMDMs into osteoclasts at 1 and 1.5 μM; increases the bone volume fraction and bone mineral density in injured tibiae in a rat model of cancellous bone injury and regeneration when administered locally at 1 μg

Formal name: 4-[[2-[6-[(4-methyl-1-piperazinyl)carbonyl]-2-naphthalenyl]ethyl]amino]-6-quinazolinecarbonitrile

Synonyms:  SNX2-1-165

Molecular weight: 450.5

CAS: 1449228-40-3

Purity: ≥98%

Formulation: A crystalline solid

Related products

  • 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 zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 250 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 - 250 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 – 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
    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 50 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 - 50 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page