RI-1

製品コードS8077 バッチS807701

印刷

化学情報

Synonyms

RAD51 inhibitor 1

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₄H₁₁Cl₃N₂O₃

分子量

361.61

CAS No.

415713-60-9

Solubility (25°C)*

体外

DMSO

50 mg/mL (138.27 mM)

Water

Insoluble

Ethanol

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.250mg/ml (3.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.250mg/ml (3.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	RI-1 (RAD51 inhibitor 1) is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM.
in vitro	RI-1 sensitizes cells to DNA damage by directly and specifically disrupting HsRAD51 and inhibiting the ability of RAD51 to form filaments on ssDNA. In addition, this compound alone generates single-agent toxicity in all three cancer cell lines (HeLa, MCF-7 and U2OS) with LD50 values in the 20–40 µM range. ^[1] It decreases the rejoining of γ-H2AX foci in G2 phase cells and results in a higher level of unrepaired DSBs 6 hours after irradiation. ^[2]
特徴	A selective recombinant RAD51 protein inhibitor discovered in 2012. Valuable tool for mechanistic studies of DNA repair and potential for use in many cancers.

プロトコル(参考用のみ)

キナーゼアッセイ	DNA binding assays
キナーゼアッセイ	All reactions are performed in black non-binding polystyrene 384-well plates with reaction volumes of 30–100 μL. Purified DNA strand exchange proteins and chemical compounds are pre-incubated at room temperature for 5 minutes; they are then further incubated at 37°C for 30 min with 100 nM of ssDNA substrate, consisting of a 45-mer poly-dT tagged with Alexa 488 at the 5’ terminus (synthesized and purified by Integrated DNA Technologies). Reactions are performed in 20 mM HEPES pH 7.5, 10 mM MgCl₂, 0.25 μM BSA, 2% glycerol, 30 mM NaCl, 4% DMSO and 2 mM ATP. Some conditions included DTT or TCEP (tris(2-carboxyethyl)phosphine) as indicated. DNA binding is measured as a function of fluorescence polarization (FP) with a Safire2 plate reader, using the following settings: excitation 470±5nm, emission 530±5nm, 10 reads/well, Z height and G factor auto-calibrated from control wells. Displayed error bars represent standard deviation. For experiments involving a titration of protein concentrations, data are fit to an equation that accounts for the cooperative nature by which recombinase proteins bind DNA. For experiments involving a titration of this compound, protein concentrations are selected to give an ∼80% saturation of the FP signal in the absence of this chemical.
細胞アッセイ	細胞株	HeLa, MCF-7 and U2OS cells
	濃度	~35 μM
	反応時間	24 hours
	実験の流れ	Cytotoxicity is determined by loss of colony-forming ability. Experiments are performed in triplicate. Crystal violet stained colonies are imaged with a CCD camera and counted using NIH Image software. Error bars denote standard error.

参考

https://pubmed.ncbi.nlm.nih.gov/22573178/
https://pubmed.ncbi.nlm.nih.gov/23874869/
[4] Pereira M, et al. Prog Neuropsychopharmacol Biol Psychiatry. 2011, 35(7), 1636-1644.

カスタマーフィードバック

: Data from [Data independently produced by , , Biomed Pharmacother, 2017, 94:165-168]

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：

Combined MEK and PARP inhibition enhances radiation response in rectal cancer [ Cell Rep Med, 2025, 6(8):102284]	PubMed: 40782795
Low-dose ionizing radiation-induced RET/PTC1 rearrangement via the non-homologous end joining pathway to drive thyroid cancer [ MedComm (2020), 2024, 5(8):e690]	PubMed: 39135916
Amodiaquine ameliorates stress-induced premature cellular senescence via promoting SIRT1-mediated HR repair [ Cell Death Discov, 2024, 10(1):434]	PubMed: 39394181
Short-Term Starvation Weakens the Efficacy of Cell Cycle Specific Chemotherapy Drugs through G1 Arrest [ Int J Mol Sci, 2023, 24(3)2498]	PubMed: 36768821
Short-Term Starvation Weakens the Efficacy of Cell Cycle Specific Chemotherapy Drugs through G1 Arrest [ Int J Mol Sci, 2023, 24(3)2498]	PubMed: 36768821
DNA‑PKcs phosphorylation specific inhibitor, NU7441, enhances the radiosensitivity of clinically relevant radioresistant oral squamous cell carcinoma cells [ Biomed Rep, 2023, 18(4):28]	PubMed: 36926187
U2AF1 mutation connects DNA damage to the alternative splicing of RAD51 in lung adenocarcinomas [ Clin Exp Pharmacol Physiol, 2022, 10.1111/1440-1681.13646]	PubMed: 35434831
CRIP1 cooperates with BRCA2 to drive the nuclear enrichment of RAD51 and to facilitate homologous repair upon DNA damage induced by chemotherapy [ Oncogene, 2021, 10.1038/s41388-021-01932-0]	PubMed: 34262130
A non-genetic, cell cycle-dependent mechanism of platinum resistance in lung adenocarcinoma [ Elife, 2021, 10e65234]	PubMed: 33983115
The Valproate Mediates Radio-Bidirectional Regulation Through RFWD3-Dependent Ubiquitination on Rad51 [ Front Oncol, 2021, 11:646256]	PubMed: 33842359

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。