CD38 inhibitor 1 (compound 78c)

製品コードS8960 バッチS896005

印刷

化学情報

 Chemical Structure Synonyms CD38-IN-78c, MDK-7553 Storage
(From the date of receipt)
3 years -20°C powder
化学式

C22H27N3O3S

分子量 413.53 CAS No. 1700637-55-3
Solubility (25°C)* 体外 DMSO 14 mg/mL (33.85 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 CD38 inhibitor 1 (compound 78c, CD38-IN-78c, MDK-7553) is a potent inhibitor of CD38 with IC50 of 7.3 nM and 1.9 nM for human CD38 and mouse CD38, respetively.
in vitro

CD38 inhibitor 1 (compound 78c) increases NAD+ levels, resulting in activation of pro-longevity and health span-related factors including sirtuins, AMPK, and PARPs.[2]

in vivo

CD38 inhibitor 1 (compound 78c) is found to not only be a very potent inhibitor, but also had suitable physiochemical properties to serve as a robust tool for in vivo studies. In addition, CD38 inhibitor 1 (compound 78c) is able to elevate NAD in both liver and gastrocnemius tissue when dosed orally in a DIO mouse.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HEK293T, MEFs, A549, Jurkat T and AML12 cells
濃度 0.5 μM, 0.2 - 0.5 μM
反応時間 16 h, 24 h
実験の流れ

To test the reversibility of the CD38i, A549 cells were treated with vehicle or 0.5 μM 78c for 16 hours. Then, cells were washed and incubated with (78c) or without (78c+release) 78c for another 8 hours.

動物実験 動物モデル DIO C57Bl6 mice
投薬量 30 mg/kg, 2 mg/kg
投与方法 Oral gavage, IV

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:

Inhibition of CD38 enzymatic activity enhances CAR-T cell immune-therapeutic efficacy by repressing glycolytic metabolism [ Cell Rep Med, 2024, 5(2):101400] PubMed: 38307031
Boosting NAD preferentially blunts Th17 inflammation via arginine biosynthesis and redox control in healthy and psoriasis subjects [ Cell Rep Med, 2023, S2666-3791(23)00310-5] PubMed: 37586364
Boosting NAD preferentially blunts Th17 inflammation via arginine biosynthesis and redox control in healthy and psoriasis subjects [ Cell Rep Med, 2023, 4(9):101157] PubMed: 37586364
Comprehensive Proteomics Analysis Identifies CD38-Mediated NAD+ Decline Orchestrating Renal Fibrosis in Pediatric Patients With Obstructive Nephropathy [ Mol Cell Proteomics, 2023, 22(3):100510] PubMed: 36804530
eIF3i promotes colorectal cancer cell survival via augmenting PHGDH translation [ J Biol Chem, 2023, 299(9):105177] PubMed: 37611825
Role of Integrin β1 in the progression and chemo-resistance of esophageal squamous cell carcinoma [ Orthop Surg, 2022, 10.1111/os.13258] PubMed: 35441488

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。