OICR-9429

製品コードS7833 バッチS783301

化学情報

	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	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.

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

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：

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

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。