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
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.
* <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, this compound 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 CD38 inhibitor 1 (compound 78c), A549 cells were treated with vehicle or 0.5 μM 78c for 16 hours. Then, cells were washed and incubated with (this compound) or without (this compound+release) this compound 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

参考

  • https://pubmed.ncbi.nlm.nih.gov/25828863/
  • https://pubmed.ncbi.nlm.nih.gov/29719225/

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:

CD38 in the pathobiology of cutaneous T-cell lymphoma and the potential for combination therapeutic intervention [ Leukemia, 2025, 10.1038/s41375-025-02551-4] PubMed: 40057636
Bionic bearing-inspired lubricating microspheres with Immunomodulatory effects for osteoarthritis therapy [ J Nanobiotechnology, 2025, 23(1):457] PubMed: 40542398
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。

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