Background
CBR-5884 is a small-molecule inhibitor of phosphoglycerate dehydrogenase (PHGDH), which catalyzes the first step in the serine biosynthesis pathway. An increase in serine biosynthesis supports growth and proliferation of cancer cells, which is seen by amplification and overexpression of PHGDH in some melanoma and breast cancers (1). CBR-5884 inhibited the proliferation of melanoma and breast cancers that displayed increased levels of serine synthesis, but had no effect on cells that rely on extracellular serine uptake. CBR-5884 disrupted PHGDH oligomerization and decreased serine biosynthesis by 30% in cancer cells (2). CBR-5884 treatment of teratocarcinoma cells significantly decreased the growth rate in a dose-dependent manner (3). Inhibition of PHGDH and serine biosynthesis caused accumulation of reactive oxygen species, DNA damage, and apoptosis in leukemic cells (4). Treating human myeloma cells with CBR-5884 reduced proliferation, while inhibition of PHGDH by CBR-5884 reduced proliferation and sensitized glioblastoma cells to hypoxia-induced cell death (5,6).
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- Mullarky, E. et al. (2016) Proc Natl Acad Sci U S A 113, 1778-83.
- Sharif, T. et al. (2018) Cell Death Dis 9, 990.
- Garcia-Cuellar, M.P. et al. (2020) Blood Adv 4, 3626-3638.
- Elsaadi, S. et al. (2021) Exp Hematol Oncol 10, 3.
- Engel, A.L. et al. (2020) Br J Cancer 122, 1391-1398.
Molecular Formula
C14H12N2O4S2
Molecular Weight
336.4 g/mol
Purity
>98%
CAS
681159-27-3
Solubility
Soluble in DMSO at 50 mg/mL or DMF at 50 mg/mL.
Storage
Directions for Use
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
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