Glutaminase Inhibitor

Glutaminase Inhibitors (61):

Cat. No.	Product Name	Effect	Purity

HY-12248

Telaglenastat	Inhibitor	99.82%
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.

HY-12683

BPTES	Inhibitor	98.75%
BPTES is an allosteric and selective glutaminase inhibitor with an IC₅₀ of 0.16 μM.

HY-B1692

L-Methionine-DL-sulfoximine	Inhibitor	≥98.0%
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).

HY-12337

GK921	Inhibitor	99.91%
GK921 is a transglutaminase 2 (TGase) inhibitor with an IC₅₀ of 7.71 μM for human recombinant TGase 2.

HY-W353728

N-Carbobenzoxytyramine	Inhibitor	98.62%
N-Carbobenzoxytyramine (N-CBZ-Tyramine), a carbobenzoxy derivatives of amino acid, is a competitive inhibitor of glutaminase activity.

HY-180322

TG2-IN-3h	Inhibitor
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.

HY-181890

TRG-192	Inhibitor
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.

HY-W015309

Decanoic acid	Inhibitor	98.0%
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.

HY-124476

Cystamine	Inhibitor	99.85%
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) .

HY-16693

LDN-27219	Inhibitor	99.76%
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.

HY-12682

Glutaminase C-IN-1	Inhibitor	99.89%
Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.

HY-19359

Vilagletistat	Inhibitor	99.97%
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).

HY-W020050

Cystamine dihydrochloride	Inhibitor	99.92%
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) .

HY-P99512

Zampilimab	Inhibitor	≥99.0%
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.

HY-117678

TG-2-IN-1	Inhibitor	98.0%
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.

HY-121167

L-Albizziin	Inhibitor	98.0%
L-albizziin, as a sulfhydryl group reagent, is a glutamase inhibitor. L-albizziin can be used for the research of cancer.

HY-123290

KCC009	Inhibitor	98.06%
KCC009, a transglutaminase 2 (TG2) inhibitor, induces p53-independent radiosensitization.

HY-129126

NC9	Inhibitor	99.98%
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.

HY-145933

BJJF078	Inhibitor	99.66%
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.

HY-79583

Glutaminase-IN-3	Inhibitor	99.88%
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.

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