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

OICR-9429 

Cat. No.: HY-16993 Purity: 99.91%
COA Handling Instructions

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) .

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

OICR-9429 Chemical Structure

OICR-9429 Chemical Structure

CAS No. : 1801787-56-3

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10 mM * 1 mL in DMSO USD 129 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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Estimated Time of Arrival: December 31
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10 mg USD 140 In-stock
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25 mg USD 320 In-stock
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50 mg USD 530 In-stock
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100 mg USD 850 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    OICR-9429 purchased from MCE. 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 MCE. 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.
    • 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].

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

    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].

    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.
    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 32 mg/mL (57.60 mM)

    *"≥" 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
    10 mM 0.1800 mL 0.8999 mL 1.7999 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.91%

    References
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    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.

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    Product Name:
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    Cat. No.:
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