OICR-9429

製品コードS7833 バッチS783304

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C29H32F3N5O3
分子量 555.59 CAS No. 1801787-56-3
Solubility (25°C)* 体外 DMSO 100 mg/mL (179.98 mM)
Ethanol 100 mg/mL (179.98 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Primary human AML cells
濃度 5 μM
反応時間 72 h
実験の流れ

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.
動物実験 動物モデル Male BALB/c nude mice
投薬量 30 or 60 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/26167872/
  • https://pubmed.ncbi.nlm.nih.gov/34154613/

カスタマーフィードバック

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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Targeting MLL1/WDR5-Mediated Epigenetic Regulation Mitigates Peritoneal Fibrosis by Reducing p16INK4a [ FASEB J, 2025, 39(8):e70543] PubMed: 40232893
Transcription elongation defects link oncogenic SF3B1 mutations to targetable alterations in chromatin landscape [ Mol Cell, 2024, 84(8):1475-1495.e18] PubMed: 38521065
MYCN drives oncogenesis by cooperating with the histone methyltransferase G9a and the WDR5 adaptor to orchestrate global gene transcription [ PLoS Biol, 2024, 22(3):e3002240] PubMed: 38547242
The COMPASS complex maintains the metastatic capacity imparted by a subpopulation of cells in UPS [ iScience, 2024, 27(7):110187] PubMed: 38989451
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
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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