CD38 inhibitor 1 (compound 78c)

For research use only.

Catalog No.S8960 Synonyms: CD38-IN-78c, MDK-7553

CD38 inhibitor 1 (compound 78c) Chemical Structure

CAS No. 1700637-55-3

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.

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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

Cell Research:

[2]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: DIO C57Bl6 mice
  • Dosages: 30 mg/kg, 2 mg/kg
  • Administration: Oral gavage, IV
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL (200.71 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 413.53
Formula

C22H27N3O3S

CAS No. 1700637-55-3
Storage powder
in solvent
Synonyms CD38-IN-78c, MDK-7553
Smiles CN1C2=C(C=C(C=C2)C3=CN=CS3)C(=CC1=O)NC4CCC(CC4)OCCOC

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID