Dihydroorotate Dehydrogenase Inhibitor, Brequinar-CAS 96201-88-6-Calbiochem

C₂₃H₁₄F₂NNaO₂

397.35

A quinolinecarboxylic acid derivative with immunosuppressive and anti-neoplastic properties. Inhibits pyrimidine synthesis by blocking the activity of mammalian mitochondrial dihydroorotate dehydrogenase (DHODH; IC₅₀ = 12 nM). Does not affect DHODH in non-mammalian species. Also reported to inhibit glycosylation of adhesion molecules. Potentiates the sensitivity of U1690 small cell lung cancer cells to TRAIL-induced apoptosis and synergistically enhances the anti-tumor effects of doxorubicin ( ~100 µM).

Cell permeable: yes
Primary Target
DHODH

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

He, T. et al. 2013. Oncogene32, in press.
Hurt, D.E., et al. 2006. Bioorg. Med. Chem. Lett.16, 1610.
Schnellrath, L. et al. 2011. Int. J. Antimicrob. Agents.38, 435.
Batt, D.G., et al. 1995. Bioorg. Med. Chem. Lett.14, 1549.
Allison, A., et al. 1993. Transplantation Proc.25, 67.
Cramer, D. et al. 1992. Transplantation.53, 303.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥98% (HPLC)

solid

12 nM IC₅₀

Calbiochem^®

OK to freeze
protect from light

off-white

DMSO: 50 mg/mL

2-8℃

1S/C23H15F2NO2.Na/c1-13-21(23(27)28)18-12-16(24)10-11-20(18)26-22(13)15-8-6-14(7-9-15)17-4-2-3-5-19(17)25;/h2-12H,1H3,(H,27,28);/q;+1/p-1

PZOHOALJQOFNTB-UHFFFAOYSA-M

Packaged under inert gas

11 - Combustible Solids

WGK 3