CD38 inhibitor 1 (compound 78c)

Catalog No.S8960 Batch:S896006

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Technical Data

Formula

C22H27N3O3S
Molecular Weight 413.53 CAS No. 1700637-55-3
Solubility (25°C)* In vitro DMSO 20 mg/mL (48.36 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.15mg/ml Taking the 1 mL working solution as an example, add 50 μL 83 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description 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.
Targets
mCD38 [1]
(Cell-free assay)		 hCD38 [1]
(Cell-free assay)
1.9 nM 7.3 nM
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]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    HEK293T, MEFs, A549, Jurkat T and AML12 cells

  • Concentrations

    0.5 μM, 0.2 - 0.5 μM

  • Incubation Time

    16 h, 24 h

  • Method

    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.
Animal Study:

[1]
  • Animal Models

    DIO C57Bl6 mice

  • Dosages

    30 mg/kg, 2 mg/kg

  • Administration

    Oral gavage, IV

Selleck's CD38 inhibitor 1 (compound 78c) has been cited by 6 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.