YU238259

製品コードS8379 バッチS837902

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	C₂₂H₂₂ClN₃O₄S
	分子量	459.95	CAS No.	1943733-16-1
Solubility (25°C)*	体外	DMSO	91 mg/mL (197.84 mM)
		Water	Insoluble
		Ethanol	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	YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays.
in vitro	YU238259 exhibits potent synthetic lethality in the setting of DNA damage response and DNA repair defects. Treatment with YU238259 is not only synergistic with ionizing radiation (IR), etoposide, and PARP inhibition, but this synergism is heightened by BRCA2-deficiency. Synthetic lethality of YU238259 in HDR-deficient cells results from accumulation of unresolved DSBs following additional inhibition of residual HDR pathway activity. Inhibition of HDR activity by YU238259 has little to no effect on the NHEJ pathway. YU238259 sensitizes tumor cells to radiation therapy and DSB-inducing chemotherapy ^[1].
in vivo	Growth of BRCA2-deficient human tumor xenografts in nude mice is significantly delayed by YU238259 treatment even in the absence of concomitant DNA-damaging therapy^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	U2OS cells
	濃度	25 μM
	反応時間	1 h
	実験の流れ	U2OS cells were pretreated with 25 μM YU238259 or DMSO vehicle for 1 h and cells were then irradiated with 10 Gy IR. Cells were fixed at 8 h post-IR, stained with antibodies and Hoechst dye, and imaged. Foci were quantified using the InCell Analyzer algorithm developed by YCMD. Cells were scored as foci-positive if they contained ≥15 foci (BRCA1, pDNA-PK) or ≥20 foci (53BP1).
動物実験	動物モデル	069(nu)/070(nu/+) athymic nude mice
	投薬量	3 mg/kg
	投与方法	i.p

参考

[1] Stachelek GC, et al. Mol Cancer Res. 2015, 13(10):1389-97.

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：

Human papillomavirus E6/E7 oncoproteins promote radiotherapy-mediated tumor suppression by globally hijacking host DNA damage repair [ Theranostics, 2023, 13(3):1130-1149]	PubMed: 36793865
Suppression of SHROOM1 Improves In Vitro and In Vivo Gene Integration by Promoting Homology-Directed Repair [ Int J Mol Sci, 2020, 21(16)E5821]	PubMed: 32823670

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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