glioblastoma

4-Diethylaminobenzaldehyde, a reversible aldehyde dehydrogenase (ALDH) inhibitor (Ki: 4 nM for ALDH1), exhibits a potent anti-androgenic effect (IC50: 1.71 μM).

Taletrectinib (AB-106) is a new-generation selective inhibitor of ROS1 NTRK including ROS1,NTRK1,NTRK2 and NTRK3 with IC50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM, respectively.

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.

VX-984 (M9831) is an oral, selective DNA-PK inhibitor that can cross the blood-brain barrier. VX-984 inhibited the conjugation of non-homologous terminal NHEJ and acted on DSBs to break DNA double strand. VX-984 is commonly seen in glioblastoma (GBM) and non-small cell lung cancer (NSC-LC) studies.

Bindarit (AF2838)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.

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.

17-AEP-GA is an HSP90 antagonist, a potent inhibitor of glioblastoma cell proliferation, survival, migration, and invasion, and a toxic component of antibody-coupled activated molecules (ADCs), which can be used to study glioblastomas.

K34c hydrochloride is an alpha5β1 integrin antagonist for glioblastoma study.

Vacquinol-1 is an MKK4 activator, which rapidly and selectively induces glioma cell death.

KX2-361 is a orally bioavailable small molecule dual Src tubulin inhibitor that provides long term survival in a murine model of glioblastoma

Levetiracetam (SIB-S1) is a relatively unique anticonvulsant that is typically used in combination with other antiepileptic medications for partial onset seizures. Levetiracetam has been linked to rare instances of serum aminotransferase and alkaline phosphatase elevations during treatment and to rare cases of clinically apparent drug induced liver disease.

Oxcarbazepine (GP 47680) is an Anti-epileptic Agent. The physiologic effect of oxcarbazepine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

Cinnamic acid (β-Phenylacrylic acid) has potential use in cancer intervention,The concentration causing a 50% reduction of cell proliferation (IC50) ranged from 1 to 4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.

CT-179 is a potent and selective inhibitor of oligodendrocyte transcription factor 2 (OLIG2), reduces tumor cell proliferation and induces apoptosis, and enhances efficacy when used in combination with radiotherapy and other agents, showing potential in the treatment of medulloblastoma and glioblastoma.

3-arylisoquinolinamine derivative is a compound with antitumor activity.

Epirubicin hydrochloride (Pharmorubicin) is an adriamycin derivative, a topoisomerase (Topo) inhibitor, and a Forkhead box protein p3 (Foxp3) inhibitor. Epirubicin hydrochloride has antitumor activity.

JR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. It inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM) and exhibits cytotoxicity in glioblastoma [1].

GW280264X (Carbamic acid) is an inhibitor of ADAM17 .

c-Met inhibitor 1 is a c-Met receptor signaling pathway inhibitor, used for the treatment of cancer including glioblastoma, gastric, and pancreatic cancer.

CDK4 6-IN-3, a brain-penetrant CDK4 CDK6 inhibitor (Kis: <0.3 nM and 2.2 nM), is used for the treatment of glioblastoma and inhibits CDK1 with a Ki of 110 nM.

Duocarmycin SA is an extremely potent cytotoxic agent and antitumor antibiotic that induces sequence-selective alkylation of duplex DNA, with an IC50 of 10 pM. It demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells when combined with proton radiation in vitro.

FD 12-9, Anti-glioblastoma activity. is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively.

J22352, a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM, enhances anticancer effects in glioblastoma by promoting HDAC6 degradation. It does so by inhibiting autophagy and stimulating the antitumor immune response, further restoring host antitumor activity through the reduction of PD-L1's immunosuppressive activity.