A cardiac myosin ATPase inhibitor (IC50 = 0.3 µM); selective for cardiac myosin over skeletal myosin (IC50 = 4.7 µM); slows ATPase activity of α- and β-myosin; reduces cardiac contractility

MYK-461 – 1 mg

Brand:
Cayman
CAS:
1642288-47-8
Storage:
-20
UN-No:
Non-Hazardous - /

MYK-461 is an orally bioavailable inhibitor of cardiac myosin ATPase (IC50 = 0.3 µM in purified bovine myosin S1).{30587} It is selective for cardiac myosin over skeletal myosin (IC50 = 4.7 µM) and does not induce skeletal muscle impairments. It slows the rate of ATPase activity in both murine and bovine myofibrils, which are α- and β-myosin-rich, respectively, by reducing the rate of phosphate release during the myosin power stroke. In transgenic mouse models of hypertrophic cardiomyopathy, MYK-461 reduces cardiac contractility, prevents left ventricular hypertrophy, and reverses pathologic remodeling. In cats, it relieves left ventricular outflow tract obstruction.{40089} Formulations containing MYK-461 have been used for the treatment of symptomatic hypertrophic cardiomyopathy in humans and cats.  

 

Available on backorder

Add to quotes
SKU: - Category:

Description

A cardiac myosin ATPase inhibitor (IC50 = 0.3 µM); selective for cardiac myosin over skeletal myosin (IC50 = 4.7 µM); slows ATPase activity of α- and β-myosin; reduces cardiac contractility, prevents left ventricular hypertrophy, and reverses pathologic remodeling in mouse models; relieves left ventricular outflow tract obstruction in cats

Formal name: 3-(1-methylethyl)-6-[[(1S)-1-phenylethyl]amino]-2,4(1H,3H)-pyrimidinedione

Synonyms:  SAR439152

Molecular weight: 273.3

CAS: 1642288-47-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|ATPases||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cardiovascular System|Cardiovascular Diseases|Cardiomyopathy||Research Area|Cardiovascular System|Heart|Myocardial Contractility||Research Area|Cardiovascular System|Heart|Myocardial Hypertrophy

Related products

  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 50 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 - 50 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 – 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
    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 250 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 - 250 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