JH-RE-06

製品コードS8850 バッチS885002

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₀H₁₆Cl₃N₃O₄
	分子量	468.72	CAS No.	1361227-90-8
Solubility (25°C)*	体外	DMSO	40 mg/mL (85.33 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	JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 of 0.78 μM and Kd value of 0.42 μM, disrupting REV1-POL ζ-mediated mutagenic translesion synthesis (TLS).
in vitro	JH-RE-06 disrupts mutagenic TLS by preventing recruitment of mutagenic POL ζ. Remarkably, JH-RE-06 targets a nearly featureless surface of REV1 that interacts with the REV7 subunit of POL ζ. Binding of JH-RE-06 induces REV1 dimerization, which blocks the REV1-REV7 interaction and POL ζ recruitment. JH-RE-06 inhibits mutagenic TLS and enhances cisplatin-induced-toxicity in cultured human and mouse cell lines.^[1]
in vivo	JH-RE-06 improves tumor cell response to cisplatin in vivo. Co-administration of JH-RE-06 with cisplatin suppresses the growth of xenograft human melanomas in mice, establishing a framework for developing TLS inhibitors as a novel class of chemotherapy adjuvants.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HT1080 cells, A375 cells, KP cells, MEF, LNCap cells, AG01522 cells.
	濃度	1.5 μM
	反応時間	24 h
	実験の流れ	Clonogenic survival assay—300 cells are plated in triplicate in 6-well plates for 24 hours. Cisplatin is added to relevant wells for 24 hours. All plates are incubated at 37℃ for 24 hours. Media are changed the next day and in fresh media JH-RE-06 (at 1.5 μM concentration) is added to untreated or cisplatin-treated cells for another 24 hours. Media are changed at the end of these combination treatments, and cells are allowed to recover for 7 days. To stain the resulting colonies, media are aspirated and the fixative (50% methanol and 10% glacial acetic acid) is added for 10 minutes, followed by the addition of 0.02% Coomassie brilliant blue R-250 stain in methanol: acetic acid: water in a ratio of 46.5:7:46.5 (v/v/v). Colonies that stained blue and contained at least 40 cells are counted. Relative cell survival or colony formation is calculated by dividing colony counts from treated samples by the DMSO or untreated controls.
動物実験	動物モデル	6–8-week-old NCRNU-F (nude) female mice
	投薬量	1.6 mg/kg
	投与方法	intra tumor injection

参考

[1] Jessica L Wojtaszek, et al. Cell. 2019 Jun 27;178(1):152-159.e11.

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：

POLQ seals post-replicative ssDNA gaps to maintain genome stability in BRCA-deficient cancer cells [ Mol Cell, 2022, S1097-2765(22)01070-X]	PubMed: 36455556
Translesion DNA synthesis mediates acquired resistance to olaparib plus temozolomide in small cell lung cancer [ Sci Adv, 2022, 8(19):eabn1229]	PubMed: 35559669

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。