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CBR 5884
- Soluble in DMSO
- MF: C14H12N2O4S2
- MW: 336.39
Description
CBR 5884 is a noncompetitive inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH; IC50 value 33 µM) with selective toxicity towards cancer cell lines with high serine biosynthetic activity. CBR-5884 shows no inhibitory effect on two other NAD+-dependent dehydrogenases, lactate dehydrogenase (LDH) and MDH1A.
PHGDH pharmacology is highly relevant to cancer and metabolic reprogramming research; CBR-5884 serves as a potent small-molecule tool that supports mechanistic studies of PHGDH and serine biosynthesis across biochemical, cellular, and disease-model assays.
Key Features
- Non-competitive PHGDH inhibitor
- IC50 value: 33 µM
- Modulates PHGDH-dependent biological activity
- No LDH and MDH1A inhibition
Applications
- PHGDH pharmacology and target-validation studies
- Disease-model research related to cancer
- Compound profiling, assay development and lead-optimization support
More Information
| Parent CAS No. | 681159-27-3 |
|---|---|
| Chemical Name | ethyl 5-(furan-2-carboxamido)-3-methyl-4-thiocyanatothiophene-2-carboxylate |
| SMILES | C1(C(OCC)=O)SC(NC(C2=CC=CO2)=O)=C(SC#N)C=1C |
| MFCD | N.A. |
| InChi | InChI=1S/C14H12N2O4S2/c1-3-19-14(18)11-8(2)10(21-7-15)13(22-11)16-12(17)9-5-4-6-20-9/h4-6H,3H2,1-2H3,(H,16,17) |
| InChiKey | QBVIRPJBDIZKBC-UHFFFAOYSA-N |
| CID | 4674993 |
| Short Description | PHGDH inhibitor |
References
- E Mullarky et al. Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers. Proc Natl Acad Sci U S A. 2016 Feb 16;113(7):1778-83.
- E Mullarky et al. A novel small-molecule inhibitor of 3-phosphoglycerate dehydrogenase. Mol Cell Oncol. 2016 Mar 30;3(4):e1164280.


