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Purity: ≥98%
OICR-9429 (OICR9429) is a novel, potent and selective antagonist of the interaction between WDR5 and the peptide regions of MLL and Histone 3, disrupting Wdr5-MLL interaction with IC50 of 5 uM. OICR-9429 shows anticancer activity by inhibiting proliferation and inducing differentiation in p30-expressing human AML cells. It can cause a significant decrease in viability in the majority of patient cells with mutations in the N-terminal part of the CEBPA gene. OICR-9429 displays exquisite cellular selectivity and specificity in disrupting critical protein-protein interactions between WDR5. It reduces the viability of primary human AML cells with N-terminal C/EBPα mutations by about 50% (mean value, n = 8) at 5 μM.
| ln Vitro |
T24 and UM-UC-3 exhibit strong sensitivity to OICR-9429 (0-10 μM, 48 h), with IC50 values of 67.74 μM and 70.41 μM, respectively[1]. With an IC50 value of 121.42 μM, OICR-9429 (0-10 μM, 48 hours) exhibits poor sensitivity to TCCSUP[1]. By inhibiting WDR5-mediated H3K4me3, OICR-9429 (70 μM, 120 μM, 140 μM, and 240 μM; 48 hours) lowers BCa cell viability[1]. By controlling the G1/S phase transition, OICR-9429 (70 μM, 120 μM, 140 μM, and 240 μM; 48 hours) prevents BCa cell proliferation [1]. OICR-9429 (70 μM, 120 μM, 140 μM, and 240 μM; 24 h) increases BCa cell apoptosis in a dose- and time-dependent manner while enhancing the cells' chemosensitivity to cisplatin [1]. OICR-9429 (70 μM, 120 μM, 140 μM, and 240 μM; 24 hours, 48 hours) prevents bladder cancer cells from spreading [1]. BCa cells' PD-L1 expression is inhibited by OICR-9429 (70 μM, 120 μM, 140 μM, and 240 μM; 48 h) in response to IFN-γ [1].
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| ln Vivo |
In addition to enhancing the effectiveness of cisplatin on BCa cells in vivo and inhibiting tumor proliferation, OICR-9429 (30 mg/kg or 60 mg/kg, ip) targets WDR5 and lessens the toxic side effects on normal tissues [1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: BCa cell lines (T24, UM-UC-3 and TCCSUP) Tested Concentrations: 70 μM, 120 μM, 140 μM and 240 μM Incubation Duration: 5 days Experimental Results: Had a low proliferation rate and remarkably decreased the number of colonies formed by the three BCa cell lines in a dose-dependent manner. Cell Cytotoxicity Assay[1] Cell Types: BCa cell lines (T24, UM-UC-3 and TCCSUP) Tested Concentrations: 0-10 μM Incubation Duration: 48 h Experimental Results: Inhibited cell viability in a dose-dependent manner in BCa cell lines. Apoptosis Analysis[1] Cell Types: BCa cell lines (T24, UM-UC-3 and TCCSUP) Tested Concentrations: 70 μM, 120 μM, 140 μM and 240 μM Incubation Duration: 24 h Experimental Results: demonstrated no obvious apoptotic cells for 24 h but the apoptotic rate was Dramatically increased at 72 h and upregulated caspase 3/7 activity. Cell Migration Assay [1] Cell Types: BCa cell lines ( T24, UM-UC-3 and TCCSUP) Tested Concentrations: 70 μM, 120 μM, 140 μM and 240 μM Incubation Duration: 24 h, 48 h Experimental Results: decreased the migratory speed and diminished the |
| Animal Protocol |
Animal/Disease Models: xenograft mouse model[1]
Doses: 30 mg/kg, 60 mg/kg Route of Administration: 30 mg/kg, 60 mg/kg, ip Experimental Results: Suppressed tumour growth, small tumours and enhanced tumour sensitivity. |
| References |
[1]. Jingtong Zhang, et al. Targeting WD repeat domain 5 enhances chemosensitivity and inhibits proliferation and programmed death-ligand 1 expression in bladder cancer. J Exp Clin Cancer Res. 2021 Jun 21;40(1):203.
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| Molecular Formula |
C29H32F3N5O3
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| Molecular Weight |
555.59
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| CAS # |
1801787-56-3
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
FC(C1=CC(NC=C1C(NC1C=C(C2=CC=CC(=C2)CN2CCOCC2)C=CC=1N1CCN(C)CC1)=O)=O)(F)F
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7999 mL | 8.9994 mL | 17.9989 mL | |
| 5 mM | 0.3600 mL | 1.7999 mL | 3.5998 mL | |
| 10 mM | 0.1800 mL | 0.8999 mL | 1.7999 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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 16d(OICR-9429) is a potent and selective chemical probe suitable to help dissect the biological role of WDR5.J Med Chem.2016 Mar 24;59(6):2478-96. |
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