Glutaminase Inhibitor

Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat 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 inuduces autophagy and has antitumor activity.

BPTES is an allosteric and selective glutaminase inhibitor with an IC₅₀ of 0.16 μM.

L-Methionine-DL-sulfoximine (MSX; MSO), a highly specific and irreversible inhibitor of Glutamine synthetase (GS), is also a potent convulsant which metabolically and morphologically primarily affects astroglia. L-Methionine-DL-sulfoximine has been employed to inhibit the Gln-dependent ammonia-stimulated neuronal toxicity in vitro, potentiating Gln deficit-dependent depression. L-Methionine-DL-sulfoximine tremendously increases the rate of release of fixed nitrogen in cyanobacteria. L-Methionine-DL-sulfoximine is a promising candidate for research in biofertilizers and convulsive seizures (CS).

GK921 is a transglutaminase 2 (TGase) inhibitor with an IC₅₀ of 7.71 μM for human recombinant TGase 2.

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.

Cystamine is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC₅₀ value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .

LDN-27219 is a reversible, slow-binding inhibitor of TGase. LDN-27219 inhibits human TGase with an IC₅₀ value of 0.6 μM. LDN-27219 effectively decreases blood pressure and induces vasodilation, it can be used for the research of cardiovascular disease.

Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.

ZED-1227 is a specific and orally active transglutaminase 2 (TG2) inhibitor, with an IC₅₀ of 45 nM. ZED-1227 can block inflammation-induced TG2 expression and activity. ZED-1227 can be used for the research of celiac disease (CeD).

Cystamine (dihydrochloride) is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC₅₀ value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .

TG-2-IN-1 (Compound D003) is a transglutaminase-2 (TGM-2) inhibitor. TG-2-IN-1 can be used for the research of myopia.

Zampilimab (UCB-7858) is a monoclonal antibody against transglutaminase 2 (TG2). Zampilimab inhibits TG2 crosslinking transamidation activity with an IC₅₀ of 0.25 nM and a K_d of <50 pM. Zampilimab improves renal fibrosis.

L-albizziin, as a sulfhydryl group reagent, is a glutamase inhibitor. L-albizziin can be used for the research of cancer.

KCC009, a transglutaminase 2 (TG2) inhibitor, induces p53-independent radiosensitization.

NC9 (Cbz-Lys(Acr)-PEG2-dansyl) is an irreversible transglutaminase (TG) inhibitor. NC9 inhibits osteoblast differentiation and mineralization. NC9 destabilizes microtubules. NC9 can be used for the research of osteoblast differentiation.

BJJF078 is an aminopiperidine derivative. BJJF078 is a potent inhibitor of recombinant human and mouse Transglutaminase enzyme (TG2) activity, IC₅₀ values of 41 and 54 nM, respectively. BJJF078 also inhibits the close related enzyme TG1, with an IC₅₀ of 0.16 μM. BJJF078 can be used for Multiple sclerosis (MS) research.

TG2 inhibitor VA4 (compound VA4) is an irreversible Type 2 transglutaminase (TG2) inhibitor. TG2 inhibitor VA4 reacts exclusively at the TG2 transamidase site, inhibits both transamidase and GTP-binding activities.

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

Glutaminase-IN-3 (compound 657) is a potent glutaminase inhibitor with an IC₅₀ of 0.24 μM for Glutaminase 1 (GLS1). Glutaminase-IN-3 is extracted from patent WO2014089048A1, compound 657.

GLS1 Inhibitor-1 (Compound 27) is an orally active inhibitor for glutaminase 1 (GLS1) with an IC₅₀ of 0.021 μM. GLS1 Inhibitor-1 inhibits the proliferation of PC-3 with an IC₅₀ of 0.3 nM. GLS1 Inhibitor-1 exhibits antitumor efficacy against NCI-H1703 with GI₅₀ of 0.011 μM. GLS1 Inhibitor-1 exhibits moderate pharmacokinetic characteristics.