UNC0379

製品コードS7570 バッチS757002

印刷

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

C₂₃H₃₅N₅O₂

分子量

413.56

CAS No.

1620401-82-2

Solubility (25°C)*

体外

DMSO

83 mg/mL (200.69 mM)

Ethanol

30 mg/mL (72.54 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.
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。	2.500mg/ml (6.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 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.

* <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	UNC0379 is a selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.3 μM, high selectivity over 15 other methyltransferases.
in vitro	UNC0379 is competitive with the peptide substrate and noncompetitive with the cofactor SAM. ^[1]
in vivo	UNC0379, a specific inhibitor of SET8 (a histone H4 lysine 20 (H4K20) , resulted in myofibroblast dedifferentiation may partly mitigate lung fibrosis without affecting the inflammatory responses.

プロトコル(参考用のみ)

キナーゼアッセイ	Microfluidic Capillary Electrophoresis Assay
キナーゼアッセイ	Inhibition of SETD8 methyltransferase activity is analyzed by monitoring decrease in methylation of the labeled peptide, TW21. The test compounds are solubilized in 100% DMSO to 10 mM and then plated in Greiner 384-well polypropylene plates using 3-fold dilution scheme over 10 points spanning the concentration range from 3 mM to 0.15 μM using TECAN Genesis liquid handler. Then 1 μL of the serial dilution is transferred into compound dilution plate using Nanoscreen MultiMek liquid handling robot. Prior to performing the assay the compounds are diluted 10-fold in 1× assay buffer (20 mM Tris, pH 8.0, 25 mM NaCl, 2 mM DTT, and 0.05% Tween-20), and an amount of 2.5 μL of the resulting dilution is transferred into assay plate by Nanoscreen MultiMek liquid handling robot. To this plate 20 μL of 50 nM SETD8 and 2 μM TW21 peptide cocktail in 1× assay buffer are added using multidrop liquid dispenser. Following a 10 min incubation of the compounds with the enzyme/peptide mix, the reaction is initiated by adding 2.5 μL of 150 μM SAM in 1× buffer. For 100% inhibition controls 1× buffer is added instead of SAM. The reaction is allowed to proceed at room temperature for 120 min, and then the reaction is terminated by adding 35 μL of 0.08 ng/μL Endo-LysC protease solution. Following an additional 1 h incubation the plate is read on a Caliper Life Sciences EZ reader II using upstream voltage −500 V, downstream voltage −1800 V, and pressure of −1.5 psi. The IC50 values are determined using Screenable Solutions software.
細胞アッセイ	細胞株	HEK293T cells
	濃度	10 μM
	反応時間	24 h
	実験の流れ	Cells were treated with indicated concentration of drug for 24 h.
動物実験	動物モデル	Mice
	投薬量	1 mg/kg
	投与方法	i.t.

参考

https://pubmed.ncbi.nlm.nih.gov/25032507/
https://pubmed.ncbi.nlm.nih.gov/32111740/
https://pubmed.ncbi.nlm.nih.gov/32850975/

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：

C1Q+ TPP1+ macrophages promote colon cancer progression through SETD8-driven p53 methylation [ Mol Cancer, 2025, 24(1):102]	PubMed: 40165182
SET8 inhibition preserves PTEN to attenuate kidney cell apoptosis in cisplatin nephrotoxicity [ Cell Death Dis, 2025, 16(1):226]	PubMed: 40164578
SET8 inhibition preserves PTEN to attenuate kidney cell apoptosis in cisplatin nephrotoxicity [ Res Sq, 2024, rs.3.rs-4603170]	PubMed: 39184108
Targeted inhibition of the methyltransferase SETD8 synergizes with the Wee1 inhibitor adavosertib in restraining glioblastoma growth [ Cell Death Dis, 2023, 10.1038/s41419-023-06167-3]	PubMed: 37758718
Targeted inhibition of the methyltransferase SETD8 synergizes with the Wee1 inhibitor adavosertib in restraining glioblastoma growth [ Cell Death Dis, 2023, 14(9):638]	PubMed: 37758718
SETD8, a frequently mutated gene in cervical cancer, enhances cisplatin sensitivity by impairing DNA repair [ Cell Biosci, 2023, 13(1):107]	PubMed: 37308924
SETD8, a frequently mutated gene in cervical cancer, enhances cisplatin sensitivity by impairing DNA repair [ Cell Biosci, 2023, 13(1):107]	PubMed: 37308924
CDC20 Is Regulated by the Histone Methyltransferase, KMT5A, in Castration-Resistant Prostate Cancer [ Cancers (Basel), 2023, 15(14)3597]	PubMed: 37509260
H4K20me1 plays a dual role in transcriptional regulation of regeneration and axis patterning in Hydra [ Life Sci Alliance, 2023, 6(5)e202201619]	PubMed: 36944423
SETD8 induces stemness and epithelial-mesenchymal transition of pancreatic cancer cells by regulating ROR1 expression [ Acta Biochim Biophys Sin (Shanghai), 2021, gmab140]	PubMed: 34599596

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。