CBR-5884

SKU: orb1219562

Description

CBR-5884 is an selective, active of phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis. Biochemical characterization of the inhibitor revealed that it was a noncompetitive inhibitor that showed a time-dependent onset of inhibition and disrupted the oligomerization state of PHGDHCBR-5884 (15 or 30 μM; 3-5 days) selectively inhibits breast cancer lines that have a high propensity for serine synthesis. CBR-5884 (15 or 30 μM; 3-5 days) also selectively inhibits the proliferation of melanoma.

Research Area

Metabolism Research

Key Properties

• CAS Number: 681159-27-3
• MW: 336.39
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₂N₂O₄S₂
• SMILES: CCOC(=O)c1sc(NC(=O)c2ccco2)c(SC#N)c1C
• Target: Dehydrogenase
• Solubility: DMSO:47 mg/mL (139.72 mM; Need ultrasonic);H2O:< 0.1 mg/mL (insoluble)

Bioactivity

• In Vitro:
  CBR-5884 (15 or 30 μM; 3-5 days) selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis. Cell Proliferation Assay Cell line: Breast and melanoma cell lines. Concentration: 15 or 30 μM. Incubation time: 3-5 days. Result: Inhibited the proliferation of melanoma and breast cancer lines.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Dehydrogenase