BW-1370U87 is a reversible competitive monoamine oxidase-A inhibitor for the study of depression and other CNS disorders.

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).

Topotecan (NSC-609669) is a Topoisomerase I inhibitor,and is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.

Sec61-IN-4 (Compound 16b) is a potent Sec61 inhibitor with 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 markedly diminishes mitochondrial membrane potential, resulting in cell cycle arrest at the G1 phase and apoptosis in U87-MG cells. Additionally, it demonstrates significant antiproliferative effects against various tumor cell lines, including PC-3 with an IC50 of 0.28 μM, HCT-116 with an IC50 of 0.57 μM, and U87-MG with an IC50 of 1.37 μM [1].

Compound 2, or 15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide, is an ent-kaurene diterpenoid extracted from Rubescens rubescens. This compound exhibits cytotoxic activity against various cell lines, including EC-1, U87, A549, MCF-7, and HeLa, with IC50 values of 37.69 μM, 79.362 μM, 80.07 μM, 197.35 μM, and 462.13 μM, respectively, as well as 180.09 μM against another unspecified line [1].

Theaflavin 3,3'-digallate (8-Gingerol) , a major polyphenol found in black tea, is an inducer of oxidative stress which has anti-inflammatory and cancer chemopreventive actions, it reduces tumor angiogenesis by downregulating HIF-1αand VEGF.

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].

IDO/Tubulin-IN-2 (HT2) is a powerful inhibitor of both TDO and tubulin. This compound demonstrates significant efficacy against various cancer cell lines, including U87, HepG2, A549, HCT-116, and LO2, with respective IC50 values of 0.43, 0.036, 0.041, 0.095, and 1.04 μM. Additionally, IDO/Tubulin-IN-2 markedly enhances antitumor activity [1].

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

Hematoporphyrin dihydrochloride (Hematoporphyrin IX dihydrochloride) is a substrate for affinity chromatography of heme-binding proteins.

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].

SA-PA, a self-assembled intracellular PROTAC leveraging azide-alkyne click chemistry, selectively degrades VEGFR-2, PDGFR-β, and EphB4 proteins within U87 cells. In the presence of endogenous copper in tumor tissues, SA-PA undergoes in situ conversion to active PROTAC through a click reaction [1].

HPOB is an effective and specific HDAC6 inhibitor (IC50: 56 nM), >30-fold selectivity over other HDACs.

L-Kynurenine ((S)-Kynurenine) is a key intermediate in the breakdown pathway of tryptophan. L-Kynurenine is a substrate of kynureninase, KMO, and KAT associated with the suppression of antitumor immune responses. It has been shown to inhibit allogeneic T-cell proliferation and to increase malignant U87 glioma cell invasion into a collagen matrix.

LIH383 is a peptide agonist specifically designed to activate the chemokine (C-X-C motif) receptor 7 (CXCR7), which functions both as a chemokine and an opioid peptide scavenger receptor. Demonstrating a high selectivity, LIH383 activates CXCR7 with an effective concentration (EC50) of 0.61 nM, showing significantly lower affinity towards μ-, δ-, and κ-opioid receptors, as well as the nociceptin opioid peptide (NOP) receptor, even at concentrations of 3 µM in β-arrestin recruitment assays. Furthermore, at a concentration of 3 µM, LIH383 effectively inhibits the uptake of opioid peptides by CXCR7, a process normally induced by dynorphin A, a non-selective opioid receptor agonist, in U87-ACKR3 cells.

5-Hydroxyflavone is a natural product

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)

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.

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

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].

SA-VA, an intracellular self-assembled PROTAC featuring azide and alkyne groups, selectively degrades VEGFR-2 and EphB4 proteins within U87 cells. This compound undergoes in situ conversion to active PROTAC via a copper-catalyzed click reaction utilizing endogenous copper present in tumor tissues. Additionally, SA-VA induces apoptosis and arrests cell cycle progression in the S phase [1].

Exatecan-amide-cyclopropanol is an anticancer agent that inhibits the proliferation of SK-BR-3 cells (IC50: 0.12 nM) and U87 cells (IC50: 0.23 nM).

MT477 is PKC-α inhibitor. MT477 interfered with PKC activity as well as phosphorylation of Ras and ERK1/2 in H226 human lung carcinoma cells. It also induced poly-caspase-dependent apoptosis. MT477 had a dose-dependent (0.006 to 0.2 mM) inhibitory effect on cellular proliferation of H226, MCF-7, U87, LNCaP, A431 and A549 cancer cell lines as determined by in vitro proliferation assays.

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. NF-κB-IN-5 interacts directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines, with IC 50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM for HCT116, U87-MG, HepG2, BGC823, PC9, respectively.

BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist , has an IC50 of 39.9 nM in human cell line.

ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM).

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.

L-Kynurenine-d4 is a deuterated compound of L-Kynurenine. L-Kynurenine has a CAS number of 2922-83-0. L-Kynurenine is a key intermediate in the breakdown pathway of tryptophan. L-Kynurenine is a substrate of kynureninase, KMO, and KAT associated with the suppression of antitumor immune responses. It has been shown to inhibit allogeneic T-cell proliferation and to increase malignant U87 glioma cell invasion into a collagen matrix.

L-Kynurenine-d4-1 is a deuterated compound of L-Kynurenine. L-Kynurenine has a CAS number of 2922-83-0. L-Kynurenine is a key intermediate in the breakdown pathway of tryptophan. L-Kynurenine is a substrate of kynureninase, KMO, and KAT associated with the suppression of antitumor immune responses. It has been shown to inhibit allogeneic T-cell proliferation and to increase malignant U87 glioma cell invasion into a collagen matrix.

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.