An orally bioavailable helicase-primase inhibitor; inhibits the ATPase activity of HSV helicase-primase (IC50 = 30 nM); inhibits HSV replication in Vero cells (IC50 = 20 nM for both HSV-1 and HSV-2); active against porcine and bovine HSV strains (IC50s = 5 and 0.12 μM

BAY 57-1293 – 1 mg

Brand:
Cayman
CAS:
348086-71-5
Storage:
-20
UN-No:
De Minimis - 3077 / 9

BAY-57-1293 is an orally bioavailable helicase-primase inhibitor.{39314} It inhibits the ATPase activity of herpes simplex virus (HSV) helicase-primase (IC50 = 30 nM). It inhibits HSV replication in Vero cells (IC50 = 20 nM for both HSV-1 and HSV-2) and is also active against porcine and bovine HSV strains (IC50s = 5 and 0.12 μM, respectively). In vivo, oral administration of BAY-57-1293 is effective against HSV-1 and HSV-2 in a lethal challenge model (ED50 = 0.5 mg/kg in mice and rats) and in a zosteriform spread model, at a dose of 15 mg/kg, in mice and Lewis rats.{39314,39315} It is also effective in a guinea pig model of genital herpes and a mouse model of ocular herpes. BAY-57-1293 reduces levels of amyloid-beta (Aβ) and phosphorylated Tau in HSV-1 infected Vero cells.{39316}  

 

Out of stock

Add to quotes
SKU: 22129 - Category:

Description

An orally bioavailable helicase-primase inhibitor; inhibits the ATPase activity of HSV helicase-primase (IC50 = 30 nM); inhibits HSV replication in Vero cells (IC50 = 20 nM for both HSV-1 and HSV-2); active against porcine and bovine HSV strains (IC50s = 5 and 0.12 μM, respectively); effective against HSV-1 and HSV-2 in a lethal challenge model (ED50 = 0.5 mg/kg in mice and rats) and in a zosteriform spread model, at a dose of 15 mg/kg, in mice and Lewis rats; reduces levels of Aβ and phosphorylated Tau production in HSV-1 infected Vero cells

Formal name: N-[5-(aminosulfonyl)-4-methyl-2-thiazolyl]-N-methyl-4-(2-pyridinyl)-benzeneacetamide

Synonyms: 

Molecular weight: 402.5

CAS: 348086-71-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Antivirals|Helicase-primase Inhibitors||Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Product Type|Biochemicals|Small Molecule Inhibitors|Nucleic Acid Turnover/Signaling||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Viral Diseases|HSV

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 – 25 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 - 25 mg

    Available on backorder

    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
    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 – 1 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 - 1 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