1. Cell Cycle/DNA Damage
  2. CDK

LDC000067 (Synonyms: LDC067)

Cat. No.: HY-15878 Purity: 98.14%
Handling Instructions

LDC000067 is a highly specific CDK9 inhibitor with an IC50 value of 44±10 nM in vitro.

For research use only. We do not sell to patients.

LDC000067 Chemical Structure

LDC000067 Chemical Structure

CAS No. : 1073485-20-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 124 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 113 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 458 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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    LDC000067 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363.

    LAPC-4 cells are grown in charcoal-stripped serum medium (CSS) for 24 hours and then stimulated by R1881 alone or with different doses of Palbociclib (PD). Palbociclib is added 30 min before androgen treatment. Cellular expression of all proteins is detected by immunoblotting analysis. β-actin is included as a control for protein loading.

    LDC000067 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363.

    LAPC-4 cells are grown in charcoal-stripped serum medium (CSS) for 24 hours and then stimulated by R1881 alone or with different doses of LDC000067. LDC000067 is added 30 min before androgen treatment. Cellular expression of all proteins was detected by immunoblotting analysis. β-actin was included as a control for protein loading.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    LDC000067 is a highly specific CDK9 inhibitor with an IC50 value of 44±10 nM in vitro.

    IC50 & Target[1]

    CDK9- Cyclin T1

    44 nM (IC50)

    cdk2-cyclin A

    2441 nM (IC50)

    cdk1-cyclin B1

    5513 nM (IC50)

    cdk4-cyclin D1

    9242 nM (IC50)

    GSK3A

    1460 nM (IC50)

    HGK/MAP4K4

    820 nM (IC50)

    ABL2/ARG

    3640 nM (IC50)

    In Vitro

    The selectivity of LDC000067 for CDK9 over other CDKs exceeds that of the known inhibitors flavopiridol and DRB. LDC000067 displayed 55/125/210/ >227/ >227-fold selectivity for CDK9 versus CDK2/1/4/6/7. LDC000067 inhibits in vitro transcription in an ATP-competitive and dose-dependent manner. Gene expression profiling of cells treated with LDC000067 demonstrates a selective reduction of short-lived mRNAs, including important regulators of proliferation and apoptosis[1].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.6996 mL 13.4978 mL 26.9957 mL
    5 mM 0.5399 mL 2.6996 mL 5.3991 mL
    10 mM 0.2700 mL 1.3498 mL 2.6996 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    The fluorescence resonance energy transfer (FRET)-based LANCE Ultra KinaSelect Ser/Thr kit is used to determine IC50 values for various CDK inhibitors. Briefly, a specific ULight MBP peptide substrate (50 nM final concentration) is phosphorylated by a CDK-cyclin pair in buffer (50 mM HEPES-KOH pH 7.5, 10 mM MgCl2, 1 mM EGTA, 2 mM dithiothreitol) containing ATP at the concentration of the Km values of the individual kinases for 1 h at room temperature. Subsequently, phosphorylation is detected by addition of specific Eu-labelled anti-phospho-antibodies (2 nM), which upon binding to the phosphopeptide give rise to a FRET signal. FRET signals are then recorded[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    370.43

    Formula

    C₁₈H₁₈N₄O₃S

    CAS No.

    1073485-20-7

    SMILES

    O=S(CC1=CC=CC(NC2=NC=NC(C3=CC=CC=C3OC)=C2)=C1)(N)=O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 47 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    LDC000067
    Cat. No.:
    HY-15878
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