Glioma

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

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.

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.

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 specific and non-competitive inhibitor of CcO (cytochrome c oxidase) that inhibits the proliferation of chemically sensitive and chemically resistant glioma cells and blocks cell proliferation and neurosphere formation in glioma stem cell cultures.

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 an orally active, irreversible, and cell-permeable proteasome inhibitor (IC50 = 4.8 μM) that also inhibits the lysosomal enzyme cathepsin A. It induces apoptosis and cell cycle arrest, possesses anticancer, antiviral, and antioxidant activities, can penetrate the blood-brain barrier, and is commonly used in the construction of Parkinson’s disease and dementia models.

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.

Compound BPP (HDGFRP2 PSIP1-IN-1) is a dual inhibitor targeting the PWWP domains of Hepatoma-derived Growth Factor Related Protein 2 (HDGFRP2) and its homologue PSIP1. This compound effectively hinders the occurrence and progression of Diffuse Intrinsic Pontine Glioma (DIPG). It demonstrates binding affinity with a Kd value of 7 μM for HDGFRP2, indicative of its efficient ligand efficacy at 0.47. Additionally, Compound BPP exhibits a Kd value of 27 μM when binding to the PSIP1 PWWP domain, and a Kd value of 14 μM against HDGFRP3, confirming its potency as an inhibitor within the HDGFRP2 PWWP subfamily.

TLBC, a borane-chalcone derivative, exhibits dose-dependent inhibitory effects across various glioma cell lines with IC50 values ranging from 5.5 to 25.5 μM. TLBC induces apoptosis independently of alterations in the tumor suppressor factor p53.

JQ dS-4 is a degrader of Brahma-related gene 1 (BRG1) BRM SMARCA4 (PROTAC®; DC50 range = 9 - 390 nM in glioma models and cell lines), featuring a BRG1 inhibitor connected through a linker to a cereblon (CRBN) E3 ligase ligand. It effectively degrades BRG1 completely over 48 and 72 hours in HSJD-DIPG007 and SU-DIPGXIIIP cells. Additionally, it lessens the viability of various cancer cell lines, including those of H3K27M glioma, prostate, thyroid, and salivary gland.

M4K2308, a selective ALK2 ether-linked inhibitor, demonstrates an IC50 of 2 nM and exhibits greater specificity for ALK2 over ALK5, with an IC50 of 224 nM for ALK5. This compound holds potential for research into Diffuse Intrinsic Pontine Glioma (DIPG).