U87-MG

CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM, 28-fold greater selectivity for Akt2 than the closely related PKA kinase.

Erastin is an iron death activator that acts on the mitochondrial VDAC in a ROS- and iron-dependent manner. Erastin has anti-tumor activity and acts selectively on tumor cells with RAS-carcinogenic mutations.

Ellipticine (Elliptisine) is a potent antineoplastic agent exhibiting multiple mechanisms of action, IC50 of 0.67±0.06, 1.25±0.13, 1.25±0.13, 0.67±0.06, 0.27±0.02, 0.49±0.04, 0.44±0.03, and 1.48±0.62 μM for Leukemia HL-60, Breast adenocarcinoma MCF-7, Breast adenocarcinoma MCF-7, Leukemia HL-60, Neuroblastoma IMR-32, Neuroblastoma UKF-NB-4, Neuroblastoma UKF-NB-3, and Glioblastoma U87 mg cell, respectively.

ML299 (VU0463568) is a dual PLD1 2 inhibitor (PLD1 and PLD2, IC50 of 6 nM, 20 nM, respectively).

Sertindole (Lu 23-174) is an atypical antipsychotic that binds to dopamine D2 receptors and serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C, with Kds of 2.7, 20, 0.14, and 6 nM, respectively.

VEGF-IN-1 (compound 6) reduces the release of VEGF in U87-MG cells and inhibits angiogenesis in vitro. Additionally, it suppresses cell proliferation by inducing autophagy in tumor cells, with an IC50 value of 28.35 μM against U87-MG cells.

FAK-IN-24 (Compound 9f) is a potent FAK inhibitor with an IC50 of 0.815 nM. It induces DNA damage and apoptosis, and exhibits activity against glioblastoma. FAK-IN-24 effectively inhibits proliferation of glioblastoma cell lines U87-MG (IC50= 15 nM) and U251 (IC50= 20 nM), and suppresses tumor growth in U87-MG xenograft models.

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.

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).

NF-κB-IN-5 (compound 4d) is an orally active NF-κB inhibitor that interacts directly with NF-κB, and exhibits antitumor activity against human cancer cell lines, with IC50 values of 5.35, 2.81, 2.83, 2.02, and 3.90 μM for HCT116, U87-MG, HepG2, BGC823, and PC9, respectively.

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.

Arsthinol is an antiprotozoal agent which may have anti-cancer activity. It was found that arsthinol, a trivalent organoarsenic compound (dithiarsolane), has been active in vitro on leukemia cell lines and offers a better therapeutic index than arsenic trioxide, as estimated by the ratio LD50 IC50. Arsthinol induced growth inhibition of NB4 cells at lower concentration (IC50 (concentration inhibiting growth by 50%) = 0.78 + - 0.08 micromol l after 24 h) than As(2)O(3) (IC50 = 1.60 + - 0.23 micromol l after 24 h) or melarsoprol (IC50 = 1.44 + - 0.08 micromol l after 24 h). Arsthinol-cyclodextrin complex demonstrated to have was more effective than arsenic trioxide (As2O3) and melarsoprol on the U87 MG cell line. Importantly, in the in vivo study, significant antitumor activity against heterotopic xenografts was observed after i.p. administration.

FAK-IN-15 is a highly potent focal adhesion kinase (FAK) inhibitor with antitumor activity.

Tubulin Inhibitor 38 (Compound 14), a tetrazole-based agent, demonstrates significant antiproliferative effects by inducing mitotic arrest and blocking the cell cycle at the G2 M phase, ultimately triggering apoptosis. Administered at 100 nM for 24 hours, it shows considerable cytotoxicity and selectivity within HeLa, MCF7, and U87 MG cell lines [1].

PI3Kα-IN-12 (compound 13), a potent and selective PI3Kα inhibitor (IC50: 1.2 nM), effectively suppresses HCT-116 and U87-MG cell proliferation with IC50 values of 0.83 and 1.25 μM, respectively. Intraperitoneal administration of PI3Kα-IN-12 (40 mg kg) induces tumor regression in a mouse xenograft model bearing U87-MG cells [1].

Sec61-IN-4 (Compound 16b) is a potent inhibitor of Sec61, exhibiting an IC50 value of 0.04 nM in U87-MG cells [1].

PI3Kα-IN-14 (compound F8), a potent PI3Kα inhibitor, exhibits an IC50 value of 0.14 nM and significantly reduces mitochondrial membrane potential, leading to G1 phase cell cycle arrest and apoptosis in U87-MG cells. It also shows substantial antiproliferative effects against various tumor cell lines, including PC-3 (IC50 of 0.28 μM), HCT-116 (IC50 of 0.57 μM), and U87-MG (IC50 of 1.37 μM) [1].

ML-298 (CID53393915) is a potent, specific inhibitor of Phospholipase D2 (PLD2, IC50 of 355 nM).

PP5-IN-2, a selective and orally active inhibitor of protein phosphatase 5 (PP5), exhibits an IC 50 of 0.9 μM. This compound activates p53 and leads to the downregulation of cyclin D1 and MGMT, thereby inducing cell cycle arrest and reversing Temozolomide (TMZ) resistance in the U87 MG cell line. Additionally, PP5-IN-2 has demonstrated effective inhibition of tumor growth in the xenograft mouse model.