| Name | OICR-9429 |
| Description | OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro. |
| Cell Research | 20,000 viable, actively proliferating primary human AML cells per well were seeded in 96-well plates in triplicates and treated with 0.05% DMSO or OICR-9429. Cell viability was measured using the Cell Titer-Glo luminescent cell viability assay on a VICTOR X4 luminometer after 72 h.(Only for Reference) |
| Kinase Assay | AR binding affinity: AR binding affinities of test compounds are studied in cytosolic lysates obtained from ventral prostates of castrated rats by a competition binding assay. Fresh prostates are minced and homogenized with Buffer A containing protease inhibitors. The homogenates are centrifuged and the resultant supernatants are treated with a dextran-coated charcoal solution to remove endogenous steroids. The dissociation constant of the radio ligand [3H]mibolerone for isolated rat ARs is determined in a saturation binding experiment. For the determination of Ki values, prostate cytosol preparations and 1?nM [3H]mibolerone are incubated with increasing concentrations of test compounds overnight. After the incubation, bound and free steroids are separated by treatment with 100?μL of dextran-coated charcoal suspension. Bound radioactivity is determined by counting 100?μL of supernatant fraction in 200?μL of scintillation fluid using a microbeta counter. All procedures are carried out at 0–4?°C. |
| In vitro | OICR-9429 binds WDR5 with high affinity (Kd=93±28 nM) and competitively disrupts its interaction with a high-affinity Wdr5-interacting (WIN) peptide of MLL (Kdisp=64±4 nM)[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (89.99 mM)
Ethanol : 12 mg/mL (21.6 mM)
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| Keywords | pancreatic | Histone Methyltransferase | MLL | inhibit | colon | prostate cance | OICR9429 | bladder cancer (BCa) | OICR-9429 | Inhibitor | WD repeat domain 5 (WDR5) | Apoptosis | leukaemia | H3K4 |
| Inhibitors Related | Delgocitinib | Deucravacitinib | Fedratinib | Tazemetostat | Ruxolitinib | Piribedil | Tofacitinib Citrate | EPZ015666 | Ruxolitinib phosphate | JAK-IN-10 | Baricitinib | MRTX-1719 |
| Related Compound Libraries | Anti-Lung Cancer Compound Library | Reprogramming Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
