A Cdk9 inhibitor (IC50 = 44 nM); selective for Cdk9 over Cdk1

LDC000067 – 10 mg

Brand:
Cayman
CAS:
1073485-20-7
Storage:
-20
UN-No:
Non-Hazardous - /

LDC000067 is a cyclin-dependent kinase 9 (Cdk9) inhibitor (IC50 = 44 nM).{46601} It is selective for Cdk9 over Cdk1, -2, -4, -6, and -7 (IC50s = 5.5, 2.44, 9.24, >10, and >10 μM, respectively), as well as a panel of 28 additional kinases at 10 μM. LDC000067 (10 μM) inhibits transcription dependent on the Cdk9-cyclin T complex positive transcription elongation factor b (P-TEFb) in vitro and de novo RNA synthesis in A549 cells. It induces apoptosis in A549 and MCF-7 cancer cells. LDC000067 prevents IL-1β-induced production of matrix metalloproteinase-3 (MMP-3), MMP-9, MMP-13, IL-6, IL-8, and TNF-α and NF-κB activation in SW 1353 chondrocytes.{46602} In vivo, LDC000067 (7.5 mg/kg) delays cartilage degeneration in a mouse model of anterior cruciate ligament transection (ACLT). It also prevents bone resorption in mouse models of ACLT- or LPS-induced osteoarthritis.{46603}  

 

Available on backorder

Add to quotes
SKU: 29419 - 10 mg Category:

Description

A Cdk9 inhibitor (IC50 = 44 nM); selective for Cdk9 over Cdk1, -2, -4, -6, and -7 (IC50s = 5.5, 2.44, 9.24, >10, and >10 μM, respectively) and a panel of 28 additional kinases at 10 μM; inhibits P-TEFb-dependent transcription in vitro and de novo RNA synthesis in A549 cells at 10 μM; induces apoptosis in A549 and MCF-7 cancer cells; prevents IL-1β-induced production of MMP-3, MMP-9, MMP-13, IL-6, IL-8, and TNF-α and NF-κB activation in SW 1353 chondrocytes; delays cartilage degeneration in a mouse model of ACLT at 7.5 mg/kg; prevents bone resorption in mouse models of ACLT- or LPS-induced osteoarthritis

Formal name: 3-[[6-(2-methoxyphenyl)-4-pyrimidinyl]amino]-benzenemethanesulfonamide

Synonyms:  LDC067

Molecular weight: 370.4

CAS: 1073485-20-7

Purity: ≥98%

Formulation: A crystalline solid

Related products

  • 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 – 50 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 - 50 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
  • 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