Glutaminase Inhibitor

UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC₅₀=29 nM; K_d=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.

Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC₅₀ of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.

N-Carbobenzoxytyramine (N-CBZ-Tyramine), a carbobenzoxy derivatives of amino acid, is a competitive inhibitor of glutaminase activity.

TG53 is a potent inhibitor of tissue transglutaminase (TG2) and fibronectin (FN) protein-protein interaction. TG53 inhibits formation of a complex with integrin β1 and activation of FAK and c-Src during SKOV3 cell attachment onto FN. TG53 can be used for ovarian cancer research.

2-Amino-2-(p-tolyl)acetic acid is used for optimizing azide skeleton, and is the intermediate in the synthesis of 1,3, 4-thiadiazole compounds. 1,3,4-thiadiazole compounds exhibit potential anti-cancer activity, and inhibit glutaminase (GLSI).

MD102 is an orally active transglutaminase 2 (TG2) inhibitor with an IC₅₀ of 0.35 μM. MD102 binds to the β-sandwich domain of TG2, disrupts the interaction between TG2 and p53, stabilizes p53, and reduces the activity of p-AKT and p-mTOR signaling pathways. MD102 induces cell apoptosis and inhibits tumor growth. MD102 can be used for the research of renal cell carcinoma.

Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC₅₀s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity.

IPN-60090 dihydrochloride is an orally active and highly selective inhibitor of glutaminase 1 (GLS1; IC₅₀=31 nM), with no activity observed against GLS-2. IPN-60090 dihydrochloride exhibits excellent physicochemical and pharmacokinetic properties in vivo. IPN-60090 dihydrochloride can be used for solid tumors research, such as lung and ovarian cancers.

GLS-1-IN-1 (compound 1d) is a GLS-1 inhibitor. GLS-1-IN-1 shows inhibitory effect against Hep G2, MCF 7, and MCF 10A cells.

Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy.

TG-2-IN-4 (compound 8) is a transglutaminase 2 (TG2) inhibitor with an IC₅₀ <0.5 mM. TG-2-IN-4 can be used for the research of inflammatory disorder.

GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selective glutaminase 1 (GLS1) inhibitor (IC₅₀=68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis.

α-Glucosidase-IN-5 (compound 8) is a potent α-glucosidase inhibitor with an IC₅₀ of 57.9 µM. α-Glucosidase-IN-5 has the potential for the research of diabetes mellitus.

GLS1 Inhibitor-7 (compound 4d) is a GLS1 inhibitor (IC₅₀=46.7 μM), with potential anti-cancer, anti-aging and anti-obesity properties.

TG-2-IN-5 (Compound CP4d) is a reversible TG2 inhibitor with a K_i of 1.0 μM for human TG2. TG-2-IN-5 can be used to study diseases associated with upregulation of TG2-mediated acyl transfer, such as fibrosis and cancer.

GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor with an IC₅₀ of 27.98 nM. GLS1 Inhibitor-3 shows antiproliferative activity.

TG2-IN-3h (Compound 3h) is a transglutaminase (TG2) inhibitor (hTG2: IC₅₀ = 6nM). TG2-IN-3h inhibits endothelial cell migration and angiogenesis. TG2-IN-3h alleviates renal fibrosis in a mouse model of hypertensive nephropathy. TG2-IN-3h can be used in research on metabolic diseases such as hypertensive nephropathy and cardiovascular and cerebrovascular diseases such as pathological angiogenesis.

TRG-192 is a potent and selective glutaminase (GLS) inhibitor with an IC₅₀ of 68 nM. TRG-192 inhibits intracellular glutamate levels. TRG-192 is applicable to related research on non-small cell lung cancer.

AA9 is a potent Transglutaminase 2 (TG2) inhibitor. AA9 strongly impacts HIF-mediated hypoxia in MDA-MB-231 cells.

Glutaminase C-IN-3 is a potent allosteric inhibitor of Glutaminase C (GAC) with an EC₅₀ of 116 nM. Glutaminase C-IN-3 regulates cellular metabolites and increases reactive oxygen species (ROS) production by blocking glutamine metabolism. Glutaminase C-IN-3 exhibits strong antitumor activity in an A549 xenograft mouse model. Glutaminase C-IN-3 can be used for the research of non-small cell lung cancer (NSCLC).