Home Metabolism Dehydrogenase inhibitor CBR-5884 For research use only.

CBR-5884

CBR-5884 is a selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and was selectively toxic to cancer cell lines with high serine biosynthetic activity.

CBR-5884 Chemical Structure

CBR-5884 Chemical Structure

CAS No. 681159-27-3

Purity & Quality Control

Batch: S964501 DMSO]67 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.81%
99.81

CBR-5884 Related Products

Signaling Pathway

Dehydrogenase Signaling Pathways

Dehydrogenase Signaling Pathway

Biological Activity

Description CBR-5884 is a selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and was selectively toxic to cancer cell lines with high serine biosynthetic activity.
Targets
PHGDH [1]
(Cell-free assay)
33 μM
In vitro
In vitro

CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. Biochemical characterization of the inhibitor reveals that it is a noncompetitive inhibitor that shows a time-dependent onset of inhibition and disrupts the oligomerization state of PHGDH.[1]
Cell Research Cell lines Carney cells
Concentrations 1 μM, 15 μM, 30 μM; 1 μM to 40 μM
Incubation Time 1 h; 3 h
Method

Acute Toxicity Assay. Carney cells acclimated to growth in MEM media are plated in a 96-well plate at 6,000 cells per well. The next day, cells are treated with CBR-5884 from 1 μM to 40 μM for 3 h. Drug containing media are then removed, fresh drug-free media added, and cell viability is determined via a CellTiter-Glo or Alamar Blue assay according to the manufacturer’s protocol.

Chemical Information & Solubility

Molecular Weight 336.39 Formula

C14H12N2O4S2
CAS No. 681159-27-3 SDF --
Smiles CCOC(=O)C1=C(C(=C(S1)NC(=O)C2=CC=CO2)SC#N)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 67 mg/mL ( (199.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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