Glioma

NG 52 (NG-52) is a cell-permeable, reversible, and ATP-compatible inhibitor of the cell cycle-regulating kinase Cdc28p and the related Pho85p kinase.

U-83836E (lazaroid ) has neuroprotective activity and anti-tumor activity, inhibits glioma cell proliferation, inhibits tumor necrosis factor and reverses endotoxin-induced shock.

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

SMBA1 is a highly potent Bax agonist with antitumor activity that induces cell cycle arrest and apoptosis in malignant glioma cells. SMBA1 can be used to study triple-negative breast cancer.

Phenoxybenzamine hydrochloride (NCI-c01661) is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen.

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

(±)-α-Bisabolol (Bisabolol) isa sesquiterpenol extracted from essential oils of chamomile, candida and other plants. It isa natural antiseptic with soothing, antiirritating, anti-inflammatory, antioxidant and anticancer activities. (±)-α-Bisabolol has anticancer effects on A549 NSC-LC cells by inducing cell cycle arrest, mitochondrial death and inhibiting PI3K Akt signaling (IC50 = 15 μM). (±)-α-Bisabolol can induce apoptosis of glioma cells.

DL-Tryptophan ((±)-Tryptophan) containing dipeptides are interesting ingredients for functional foods as a natural prevention for hypertension with reduced side effects due to its selective inhibition of the C-domain. Low thalamic Tryptophan uptake appears to be a strong, independent predictor of long survival in patients with previous glioma treatment.

NIK-250 is a P-glycoprotein inhibitor. NIK250 could reverse multidrug resistance in human glioma cells.

Germacrone is extracted from Curcuma zedoaria and has anti-inflammatory, anti-androgenic and antiviral activities. It also inhibits the proliferation of glioma cells by promoting apoptosis.

Eflornithine (DFMO) is a selective and orally available ornithine decarboxylase inhibitor that delays hair overgrowth.Eflornithine is used in the study of African trypanosomiasis, malignant glioma, and sleeping sickness.

1. Gycitein has weak estrogenic activity. 2. Glycitein (Glycetein) inhibits glioma cell invasion through down-regulation of MMP-3 and MMP-9 gene expression.

Tricin can inhibit human cytomegalovirus (HCMV) replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells via the upregulation of focal-adhesion-finase (FAK)-targeting microRNA-7.

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).

JAK2 inhibitor G5-7 (JAK2 inhibitor G5-7) is an orally active JAK2 inhibitor, selectively inhibits JAK2–mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 has the potential for glioma study

Cycloartenol (Handianol) is a plant sterol compound found widely in plants with anti-inflammatory, anti-tumor, antioxidant, and antibacterial properties. It inhibits glioma cell migration and p38 MAPK phosphorylation, and is used in plant growth and development studies.

ADDA 5 hydrochloride is a partial non-competitive inhibitor of cytochrome c oxidase (CcO), with IC50 values of 18.93 μM for purified CcO from human glioma and 31.82 μM for CcO from bovine heart.

AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks (Kis of 4 nM, 6 nM, 2 nM, and 1 nM for PI3Kα, β, δ, and γ, respectively), exhibiting anti-tumor activity in a mouse glioblastoma xenograft model[1]. AMG 511 significantly suppresses PI3K signaling as indicated by a decrease in p-Akt (Ser473).

Lactacystin is a natural non-peptide proteasome inhibitor and highly specific anticancer drug that controls the UPS of cellular protein turnover and inhibits alkaline cell proliferation, and is able to be used as a model for studying dementia, induces neurite outgrowth and transiently elevated levels of cAMP, inhibits angiogenesis, triggers apoptosis in glioma cells, and can penetrate the blood-brain barrier (BBB).

trans-AUCB (t-AUCB) is an effective and selective soluble epoxide hydrolase inhibitor, with IC50 values of 1.3 nM for hsEH, 8 nM for mouse sEH, and 8 nM for rat sEH.

USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4. USL311 inhibits CXCR4 activation and decreases proliferation and migration of CXCR4-expressing tumor cells, with anti-tumor activ

LDN-214117 is a potent and selective ALK2 inhibitor.

Gentiakochianin (Swertianine), an anthrone from Gentianaceae, has vasodilatory activity, induces glioma cell cycle arrest in the G(2) M phase and inhibits proliferation, significantly reduces oxLDL-induced cell damage in EA.hy926 cells, inhibits ROS levels and up-regulated the activity of Akt CREB eNOS signaling pathway inhibited by oxLDL.

Imipramine (Dimipressin) is an orally active Fascin1 inhibitor with antidepressant and antitumor activity.Imipramine inhibits the 5-hydroxytryptamine transporter (IC50: 32 nM), induces apoptosis, and induces autophagy in U-87MG glioma cells.Imipramine has neuroprotective and immunomodulatory activities, inhibits TNT, and is used to label brain blood vessels.Imipramine is a neuroprotective and immunomodulatory compound. Imipramine has neuroprotective and immunomodulatory activities, inhibits invasion and migration of TNBC cells, and can be used to study breast cancer and epilepsy.