glut-1

STF-31 is an inhibitor of glucose transporter 1 (GLUT1) with IC50 of 1 μM.

BAY-876 is an orally active, selective inhibitor of glucose transporter 1 (GLUT1, IC50= 2 nM), exhibiting over 130-fold greater selectivity for GLUT1 than GLUT2, GLUT3, and GLUT4. It also inhibits glycolytic metabolism and ovarian cancer growth.

WZB117 is a Glucose Transporter 1 (GLUT1) inhibitor. when IC50 of WZB117 approximate 10 μM, it inhibits lung cancer A549 cells and breast cancer MCF7 cells proliferation.

Lavendustin B is a Tyrosine Kinase Inhibitor and an inhibitor of HIV-1 integrase (IN) interaction with its cognate cellular cofactor, lens epithelium-derived growth factor (LEDGF/p75).

Fasentin (N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide) is an inhibitor of GluT1.

GLUT4-IN-2 is a specific GLUT4 inhibitor that inhibits GLUT1 and GLUT4.GLUT4-IN-2 has antitumor activity, induces apoptosis and cell cycle arrest, and can be used for cancer research.

hydrocotarnine is an inhibitor of Cbl.

KL-11743 specifically blocks glucose metabolism, triggering an acute collapse in NADH pools and a striking accumulation of aspartate, indicating a dramatic shift toward oxidative phosphorylation in the mitochondria.

Marein shows neuroprotective effect on PC12 cell damage induced by methylglyoxal, which is due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway, it may be a potent compound for preventing/counteracting diabetic e

GLUT1-IN-1, a glucose transporter 1 (GLUT1) inhibitor, possesses specific inactivation capability for GLUT1. This compound demonstrates concentration-dependent cytotoxicity towards HeLa, A549, and HepG2 cells, with IC50 values of 5.49 μM, 11.14 μM, and 8.73 μM, respectively. It is utilized in the research of photodynamic therapy (PDT) and several cancers [1].

GLUT1-IN-3 (Compd 4b), a compound under investigation for type 1 glucose transporter deficiency syndrome, effectively inhibits seizures [1].

GLUT1/EGFR-IN-1 (compound H) is a potent inhibitor of both GLUT1 and EGFR. It targets the ATP-binding site of the EGFR tyrosine kinase and inhibits GLUT1-mediated energy metabolism, resulting in reduced ATP, MMP, intracellular lactate, and nuclear translocation of EGFR. GLUT1/EGFR-IN-1 is applicable in the research of nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC).

GLUT-1-IN-4 (Compound 13) is an inhibitor of the GLUT-1 glucose transporter that depends on the p53 protein. It suppresses the proliferation of various cancer cells at submicromolar IC50 levels. Additionally, GLUT-1-IN-4 can halt the cell cycle, induce oxidative stress, and promote apoptosis (cell death).

OSS_128167 (SIRT6-IN-1) is a specific SIRT6 inhibitor, and for SIRT6(IC50=89 μM), SIRT1(IC50=1578 μM) and SIRT2(IC50=751 μM).

GLUT inhibitor-1 is an orally active GLUT inhibitor with IC50 s of 242 nM and 179 nM for GLUT1 and GLUT3. GLUT inhibitor-1 can be used in studies about cancers and autoimmune diseases.

Protein O-Glucosyltransferase 1 is a glucosyltransferase that modifies the Notch signaling pathway by attaching glucose to serine residues within Notch.

GLUT4 activator 1 is a potent glucose transporter type 4 (GLUT4) translocation activator (EC50: 0.14 μM).

(Rac)-Glutipyran is a broad-spectrum GLUT inhibitor targeting both GLUT1 and GLUT3. This compound inhibits glucose uptake and significantly impedes the growth of various cancer cells, particularly demonstrating substantial inhibition of PANC-1 cell growth (IC50=1.8 μM) and glucose uptake (IC50=0.13 μM).

PeS-9 is an androgen receptor (AR) degrader that induces the degradation of androgen receptors. It enhances the production of cytotoxic reactive oxygen species (ROS), leading to mitochondrial and endoplasmic reticulum stress, which results in the release of mitochondrial cytochrome C and AIF. PeS-9 activates caspase-9 and caspase-3, causing DNA fragmentation and apoptosis. It exhibits anti-prostate cancer activity and demonstrates antitumor and antimetastatic effects in vivo with minimal side effects. PeS-9 is applicable for targeted therapy research in GLUT-1 overexpressing tumors.

DRB18 is a highly effective pan-class inhibitor of glucose transporter proteins (GLUT). It significantly modulates energy-related metabolism in A549 cells by inducing alterations in the abundance of metabolites associated with glucose-related pathways. DRB18 exerts its effects by promoting G1/S phase arrest, increasing oxidative stress, and prompting necrotic cell death, ultimately displaying notable anti-tumor activity [1].

SSAO/VAP-1 Inhibitor 1 is a potent compound aimed at inhibiting SSAO/VAP-1, a protein involved in facilitating the translocation of Glucose Transport 4 (GLUT 4) to the cell membrane in adipocytes, thus playing a crucial role in glucose regulation. Additionally, in endothelial cells, this enzyme is responsible for mediating the adherence and infiltration of leukocytes, contributing to inflammatory responses. Given these mechanisms, SSAO/VAP-1 Inhibitor 1 holds considerable potential for research into treatments for inflammation, inflammation-related conditions, diabetes, and diabetes-associated diseases[1].

KCN1, a novel synthetic sulfonamide, is a HIF pathway inhibitor with potential anticancer activity in vitro and in vivo anti-pancreatic cancer activities and preclinical pharmacology. KCN1 specifically inhibited HIF reporter gene activity in several glioma cell lines at the nanomolar level. KCN1 also downregulated transcription of endogenous HIF-1 target genes, such as VEGF, Glut-1, and carbonic anhydrase 9, in a hypoxia-responsive element (HRE)-dependent manner. KCN1 potently inhibited the growth of subcutaneous malignant glioma tumor xenografts with minimal adverse effects on the host.

Glutor, a selective GLUT 1/2/3 inhibitor, inhibits glucose uptake, suppresses glycolysis, and effectively induces the death of cancer cells cultured in monolayers and spheroids [1].

1β-Hydroxy-2-oxopomolic acid inhibits adipocyte differentiation through downregulation of various adipocytokines by blocking PPARγ and C/EBPα expression.