2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. OICR-9429

OICR-9429 is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) .

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OICR-9429 Chemical Structure

OICR-9429 Chemical Structure

CAS No. : 1801787-56-3

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Customer Review

Based on 10 publication(s) in Google Scholar

OICR-9429 Related Antibodies

Top Publications Citing Use of Products

    OICR-9429 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 21;10(1):3761.  [Abstract]

    WDR5 inhibitor OICR-9429 enhances the sensitivity of ovarian cancer to genotoxic chemotherapeutics in vivo. Representative images and the apoptotic rate the indicated chemotherapy-treated xenograft tumors.

    OICR-9429 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 21;10(1):3761.  [Abstract]

    IB analysis of the level of cleaved-caspase 3 and cleaved-PARP1 in the indicated chemotherapy-treated xenograft tumors. GAPDH served as the loading control.

    View All Histone Methyltransferase Isoform Specific Products:

    View All Isoforms
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    OICR-9429 is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) [1].

    IC50 & Target

    IC50: 67.74 μM (T24 cell); 0.41 μM (UM-UC-3 cell); 121.42 μM (TCCSUP) [1]
    In Vitro

    OICR-9429 (0-10 μM, 48 h) shows high sensitivity for T24, UM-UC-3 with IC50 values of 67.74 μM and 70.41 μM, respectively[1].
    OICR-9429 (0-10 μM, 48 h) shows low sensitivity for TCCSUP with IC50 values of 121.42 μM[1].
    OICR-9429 (70 μM, 120 μM, 140 μM and 240 μM; 48 h) reduces BCa cell viability by decreasing WDR5-mediated H3K4me3[1].
    OICR-9429 (70 μM, 120 μM, 140 μM and 240 μM; 48 h) inhibits the proliferation of BCa cells by regulating the G1/S phase transition[1].
    OICR-9429 (70 μM, 120 μM, 140 μM and 240 μM; 24 h) enhances apoptosis of BCa cells in a time-dependent and dose-dependent manner and promotes cisplatin chemosensitivity in BCa cells[1].
    OICR-9429 (70 μM, 120 μM, 140 μM and 240 μM; 24 h, 48 h) suppresses the metastatic behaviour of bladder cancer cells[1].
    OICR-9429 (70 μM, 120 μM, 140 μM and 240 μM; 48 h) suppresses PD-L1 expression induced by IFN-γ in BCa cells[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    OICR-9429 Related Antibodies

    Cell Proliferation Assay[1]

    Cell Line: BCa cell lines (T24, UM-UC-3 and TCCSUP)
    Concentration: 70 μM, 120 μM, 140 μM and 240 μM
    Incubation Time: 5 days
    Result: Had a low proliferation rate and remarkably reduced the number of colonies formed by the three BCa cell lines in a dose-dependent manner.

    Cell Cytotoxicity Assay[1]

    Cell Line: BCa cell lines (T24, UM-UC-3 and TCCSUP)
    Concentration: 0-10 μM
    Incubation Time: 48 h
    Result: Inhibited cell viability in a dose-dependent manner in BCa cell lines.

    Apoptosis Analysis[1]

    Cell Line: BCa cell lines (T24, UM-UC-3 and TCCSUP)
    Concentration: 70 μM, 120 μM, 140 μM and 240 μM
    Incubation Time: 24 h
    Result: Showed no obvious apoptotic cells for 24 h but the apoptotic rate was significantly increased at 72 h and upregulated caspase 3/7 activity.

    Cell Migration Assay [1]

    Cell Line: BCa cell lines (T24, UM-UC-3 and TCCSUP)
    Concentration: 70 μM, 120 μM, 140 μM and 240 μM
    Incubation Time: 24 h, 48 h
    Result: Reduced the migratory speed and decreased the migration of the three BCa cell lines.

    Cell Invasion Assay[1]

    Cell Line: BCa cell lines (T24, UM-UC-3 and TCCSUP)
    Concentration: 70 μM, 120 μM, 140 μM and 240 μM
    Incubation Time: 24 h, 48 h
    Result: Decreased the invasion of the three BCa cell lines.

    Western Blot Analysis[1]

    Cell Line: BCa cell lines (T24, UM-UC-3 and TCCSUP)
    Concentration: 70 μM, 120 μM, 140 μM and 240 μM
    Incubation Time: 48 h
    Result: Showed significant downregulation of H3K4me3 in treated cells but not WDR5 or total H3.
    Reduced the expression of PD-L1 induced by IFN-γ in a dose-dependent manner at both the RNA and protein levels.

    RT-PCR[1]

    Cell Line: BCa cell lines (T24, UM-UC-3 and TCCSUP)
    Concentration: 70 μM, 120 μM, 140 μM and 240 μM
    Incubation Time: 48 h
    Result: Downregulated some genes related to the cell cycle, such as CDK1, PLK1, CCNE2, CCNB1, CCNA2, AURKA, and E2F1, genes related to apoptosis and DNA repair, such as BIRC5, XRCC2, AURKA, E2F1, and MCM2, and genes related to metastasis, such as AURKA and FOXM1.

    Cell Cycle Analysis[1]

    Cell Line: BCa cell lines (T24, UM-UC-3 and TCCSUP)
    Concentration: 70 μM, 120 μM, 140 μM and 240 μM
    Incubation Time: 48 h
    Result: Increased the cell population in the G0/G1 phase of three BCa cells and reduced cell population in the S and G2/M phases.
    In Vivo

    OICR-9429 (30 mg/kg or 60 mg/kg, i.p) targeting WDR5 not only suppressed tumour proliferation and enhance the efficacy of cisplatin for BCa cells in vivo but also reduced the toxicity and side effects for normal tissues[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: xenograft mouse model[1]
    Dosage: 30 mg/kg, 60 mg/kg
    Administration: 30 mg/kg, 60 mg/kg, i.p.
    Result: Suppressed tumour growth, small tumours and enhanced tumour sensitivity.
    Molecular Weight

    555.59

    Formula

    C29H32F3N5O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CNC(C=C1C(F)(F)F)=O)NC2=CC(C3=CC(CN4CCOCC4)=CC=C3)=CC=C2N5CCN(C)CC5
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 32 mg/mL (57.60 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.71%

    SDS (392 KB)

    COA (256 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7999 mL 8.9994 mL 17.9989 mL 44.9972 mL
    5 mM 0.3600 mL 1.7999 mL 3.5998 mL 8.9994 mL
    10 mM 0.1800 mL 0.8999 mL 1.7999 mL 4.4997 mL
    15 mM 0.1200 mL 0.6000 mL 1.1999 mL 2.9998 mL
    20 mM 0.0900 mL 0.4500 mL 0.8999 mL 2.2499 mL
    25 mM 0.0720 mL 0.3600 mL 0.7200 mL 1.7999 mL
    30 mM 0.0600 mL 0.3000 mL 0.6000 mL 1.4999 mL
    40 mM 0.0450 mL 0.2250 mL 0.4500 mL 1.1249 mL
    50 mM 0.0360 mL 0.1800 mL 0.3600 mL 0.8999 mL
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    OICR-9429 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    OICR-94291801787-56-3OICR9429OICR 9429Histone MethyltransferaseApoptosisWD repeat domain 5 (WDR5)MLLH3K4leukaemiacolonpancreaticprostate cancebladder cancer (BCa)Inhibitorinhibitorinhibit

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