u87 glioblastoma cells

BAY-218 is an aryl hydrocarbon receptor (AHR) antagonist with IC50 of 39.9 nM in the human glioblastoma U87 cell line. BAY-218 inhibition of AhR stimulates pro-inflammatory monocyte and T cell responses in vitro and drives anti-tumor immune responses, leading to reduced tumor growth in vivo.

Tubulin-IN-51 is an orally active tubulin inhibitor with an IC50 of 31 nM. It promotes tubulin polymerization in vitro and does not competitively bind with Paclitaxel. Tubulin-IN-51 inhibits the binding of Vinblastine to tubulin and suppresses tumor growth in various nude mouse xenograft models, including those using A549 human non-small cell lung cancer (NSCLC) cells and U87-MG human glioblastoma.

OLIG2-IN-1 is a potent and selective inhibitor of the oligodendrocyte transcription factor 2 (OLIG2). It directly and dose-dependently reduces nuclear OLIG2 levels with an IC50 of 0.88 μM. In U87 and U251 cells, OLIG2-IN-1 exhibits significant antiproliferative activity with IC50 values of 7.02 μM and 6.43 μM, respectively. OLIG2-IN-1 is applicable in cancer research, particularly for studying glioblastoma multiforme.

K-TMZ is a DNA alkylating agent. It increases the concentration of O6-methylated deoxyguanosine in U87 glioblastoma multiforme (GBM) cells in a concentration-dependent manner. K-TMZ reduces cell viability of GBM cell lines lacking (IC50s = 18-44 μM) or expressing O6-methylguanine DNA methyltransferase (MGMT; IC50s = 115-240 μM). K-TMZ can cross the blood-brain barrier and increases survival in a Br23c mouse xenograft model of GBM when administered at a dose of 14.9 mg/kg.

Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecaidine propargyl ester decreases mean arterial blood pressure in normotensive cats (ED25= 1.9 nmol/kg).3It is toxic to house flies (Musca) when administered at a dose of 75 μg/fly.4 1.Scapecchi, S., Matucci, R., Bellucci, C., et al.Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonistJ. Med. Chem.49(6)1925-1931(2006) 2.Di Bari, M., Tombolillo, B., Conte, C., et al.Cytotoxic and genotoxic effects mediated by M2 muscarinic receptor activation in human glioblastoma cellsNeurochem. Int.90261-270(2015) 3.Porsius, A.J., and Van Zwieten, P.A.Central action of some cholinergic drugs (arecaidine esters) and nicotine on blood pressure and heart rate of catsProg. Brain Res.47131-135(1977) 4.Honda, H., Tomizawa, M., and Casida, J.E.Insect muscarinic acetylcholine receptor: Pharmacological and toxicological profiles of antagonists and agonistsJ. Agric. Food Chem.55(6)2276-2281(2007)

ML-309 is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). It reversibly and selective inhibits IDH1R132H over wild-type IDH1 (IC50s = 96 and 36,500 nM, respectively). ML-309 reduces 2-hydroxyglutarate production in U87 MG glioblastoma cells (EC50 = 55 nM).

Exatecan-amide-cyclopropanol is an anticancer agent that potently inhibits the proliferation of SK-BR-3 breast cancer cells with an IC50 value of 0.12 nM, and it also suppresses the growth of U87 glioblastoma cells with an IC50 value of 0.23 nM,Exatecan-amide-cyclopropanol demonstrate robust cytotoxic potential across distinct cancer cell lines. Exatecan-amide-cyclopropanol is primarily used in research aimed at understanding DNA-topoisomerase inhibition mechanisms and their therapeutic implications in oncology.

ML309 is a potent inhibitor of R132H mutant IDH1 capable of reducing 2-hydroxyglutarate production in U87 MG glioblastoma cells. ML309 is capable of potent and selective inhibition of mutant IDH1 and effectively lowers cell-based production of 2-HG in a U87MG mutant glioblastoma cell line.

EGFR-IN-86 (compound 4i), an EGFR inhibitor (IC50: 1.5 nM), demonstrates potent activity against glioblastoma by inducing apoptosis and causing G2/M phase cell cycle arrest in U87 cells [1].

Tubulin inhibitor 41 (Compd D19) is a promising lead compound for glioblastoma treatment, known for its ability to penetrate the blood-brain barrier (BBB). It functions as a tubulin inhibitor, inducing G2/M phase arrest, leading to cell apoptosis, and inhibiting the migration of U87 cells [1].

Ecdysoside B (compound 6b) is a pregnane glycoside isolated from the plant Ecdysanthera rosea. This compound and its derivatives and isomers exhibit anticancer, immunosuppressive, and anti-inflammatory activities. Ecdysoside B demonstrates cytotoxicity against various human tumor cell lines, including PANC-1 (human pancreatic cancer cells), A375 (human melanoma cells), and U87 (glioblastoma U87 cells). It is a valuable compound for research in cancer, immunomodulation, and anti-inflammation.