Name | LDC000067 |
Description | LDC000067 (LDC067) is a highly specific and selective CDK9 inhibitor with an IC50 value of 44±10 nM. |
Kinase Assay | 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]. |
In vitro | LDC000067 reduces Ser2-P, induces p53 activation and leads to apoptosis in mESCs. In addition, LDC067 also dose-dependently inhibits P-TEFb-dependent de novo?RNA synthesis of cellular genes.[1] |
Storage | store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 69 mg/mL (186.3 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
|
Keywords | LDC-067 | LDC-000067 | LDC000067 | LDC 067 | LDC 000067 | Inhibitor | inhibit | Cyclin dependent kinase | CDK | Apoptosis |
Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Myricetin | Dextran sulfate sodium salt (MW 4500-5500) | Sodium 4-phenylbutyrate | L-Ascorbic acid | Metronidazole | Sorafenib | Tributyrin | Salicylic acid | Oleic acid |
Related Compound Libraries | Highly Selective Inhibitor Library | Apoptosis Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |