OICR-9429

Catalog No.S7833 Batch:S783301

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Technical Data

Formula

C29H32F3N5O3
Molecular Weight 555.59 CAS No. 1801787-56-3
Solubility (25°C)* In vitro DMSO 38 mg/mL (68.39 mM)
Ethanol 15 mg/mL (26.99 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description OICR-9429 is a potent antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3 and reduces viability of acute myeloid leukemia cells in vitro. It binds to WDR5 with high affinity (KD = 93 ± 28 nM.
Targets
Wdr5-MLL interaction [1] WDR5 [1]
93 nM(Kd)
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].
In vivo

OICR-9429, a potent WDR5 inhibitor, suppressed proliferation, metastasis and PD-L1-based immune evasion while enhancing apoptosis and chemosensitivity to cisplatin in bladder cancer by blocking the WDR5-MLL complex mediating H3K4me3 in target genes.

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Primary human AML cells

  • Concentrations

    5 μM

  • Incubation Time

    72 h

  • Method

    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.
Animal Study:

[2]
  • Animal Models

    Male BALB/c nude mice

  • Dosages

    30 or 60 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Theranostics, 2018, 8(18):5143-5158]

Selleck's OICR-9429 has been cited by 10 publications

Therapeutic targeting of metabolic vulnerabilities in cancers with MLL3/4-COMPASS epigenetic regulator mutations [ J Clin Invest, 2023, 133(13)e169993] PubMed: 37252797
Priming therapy by targeting enhancer-initiated pathways in patient-derived pancreatic cancer cells [ EBioMedicine, 2023, 92:104602] PubMed: 37148583
Unannotated microprotein EMBOW regulates the interactome and chromatin and mitotic functions of WDR5 [ Cell Rep, 2023, 42(9):113145] PubMed: 37725512
MYCN driven oncogenesis involves cooperation with WDR5 to activate canonical MYC targets and G9a to repress differentiation genes [ bioRxiv, 2023, 2023.07.11.548643] PubMed: 37781575
Recruitment of MLL1 complex is essential for SETBP1 to induce myeloid transformation [ iScience, 2022, 25(1):103679] PubMed: 35036869
ecDNA hubs drive cooperative intermolecular oncogene expression [ Nature, 2021, 10.1038/s41586-021-04116-8] PubMed: 34819668
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, 40(1):203] PubMed: 34154613
Inhibition of the H3K4 methyltransferase MLL1/WDR5 complex attenuates renal senescence in ischemia reperfusion mice by reduction of p16INK4a [ Kidney Int, 2019, 96(5):1162-1175] PubMed: 31570196
Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity [ Cell Rep, 2019, 26(11):2916-2928.e13] PubMed: 30865883
Overexpression of HOXC10 promotes angiogenesis in human glioma via interaction with PRMT5 and upregulation of VEGFA expression [Tan Z, et al. Theranostics, 2018, 8(18):5143-5158] PubMed: 30429891

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.