Glutaminase

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Glutaminase is the initial enzyme in glutamine metabolism, which catalyzes the hydrolysis of glutamine to glutamate in cells. Glutaminase plays a key role in cancer cell metabolism, growth, and proliferation. In mammalian cells, there are two paralogous GLS genes, GLS1 (or GLS) and GLS2. GLS1 encodes two alternatively spliced isozymes: kidney glutaminase (KGA) and glutaminase C (GAC). GLS2 also encodes two isozymes: liver glutaminase (LGA) and glutaminase B.

GLS1 is ubiquitously expressed in various tissues, and its expression can be induced by the oncogene MYC. GLS1 is frequently activated and/or overexpressed in various types of cancer, including hepatocellular carcinoma (HCC). GLS1 has been reported to promote tumorigenesis in different types of cancer, including HCC, which is mainly attributable to its glutaminase activity and role in promoting glutamine metabolism. GLS has emerged as a critical enzyme in a number of cancer types. Elevated GLS2 enzymatic activity has also been correlated with tumor cell growth in vitro and in vivo. N-Myc activates GLS2 to promote conversion of glutamine to glutamate in MYCN-amplified neuroblastoma cells. Abrogation of GLS2 function profoundly inhibits glutaminolysis and dramatically decreases cell proliferation and survival in vitro and in vivo. However, there is controversy over the role of GLS2 as a tumor suppressor. Enzymatic activity independent of GLS2 is up-regulated via p53 or p63 and plays a role of tumor suppressor.

Glutaminase Related Products (45)
Antibodies (6)

By Effects:	Inhibitors (41) Degrader (1) Antagonists (2)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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	98.98%
BPTES is an allosteric and selective glutaminase inhibitor with an IC₅₀ of 0.16 μM.

HY-108357

6-Diazo-5-oxo-L-nor-Leucine	Antagonist	99.95%
6-Diazo-5-oxo-L-nor-Leucine (L-6-Diazo-5-oxonorleucine; DON) is a glutamine antagonist that irreversibly inhibits the catabolic effect of glutamine. 6-Diazo-5-oxo-L-nor-Leucine shows good anticancer activity (especially in pancreatic cancer) and reduces the self-renewal potential and metastatic capacity of tumour cells. 6-Diazo-5-oxo-L-nor-Leucine also possesses antibacterial and antiviral activity.

HY-122218

JHU-083	Antagonist	≥98.0%
JHU-083, a proagent of 6-diazo-5-oxo-L-norleucine (DON; HY-108357), is an orally active and selective glutaminase antagonist. JHU-083 blocks glutaminase activity in brain CD11b⁺ cells and experimental cerebral malaria (ECM) resulting in a net decrease of glutamate levels in the animals.

HY-12682

Glutaminase C-IN-1	Inhibitor	99.88%
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-158378

Trivalent hydroxyarsinothricn	Inhibitor
Trivalent hydroxyarsinothricn (R-AST-OH) is a covalent and irreversible kidney-type glutaminase (KGA) inhibitor. Trivalent hydroxyarsinothricn binds to the glutamine binding site and forms a covalent bond with an active site cysteine residue. Trivalent hydroxyarsinothricn selectively kills triple-negative breast cancer (TNBC) cells and is not cytotoxic to the control cell line. KGA is the enzyme that controls glutamine metabolism and is correlated with tumor malignancy.

HY-157975

LM11	Inhibitor
LM11 is an inhibitor of transglutaminase 2 (TG2) with an activity of killing glioblastoma cells by maintaining TG2 in a cytotoxic conformational state.

HY-162141

MD102	Inhibitor
MD102 is a potent TG2 inhibitor with an IC₅₀ value of 0.35 μM. MD102 stabilizes p53 by inhibiting TG2, inducing a decrease in p-AKT and p-mTOR downstream signaling, leading to tumor cell apoptosis.

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 prevent the Gln-dependent aspect of stimulation of neuronal networks in vitro by ammonia, potentiating Gln deficit-dependent aspects of 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 eco-friendly biofertilizers and convulsive seizures (CS).

HY-19359

ZED-1227	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-12337

GK921	Inhibitor	99.93%
GK921 is a transglutaminase 2 (TGase) inhibitor with an IC₅₀ of 7.71 μM for human recombinant TGase 2.

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	99.79%
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-123290

KCC009	Inhibitor	98.98%
KCC009, a transglutaminase 2 (TG2) inhibitor, induces p53-independent radiosensitization.

HY-W020050

Cystamine (dihydrochloride）	Inhibitor	≥98.0%
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-114334

Glutaminase-IN-1	Inhibitor	98.65%
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.

HY-103671

IPN60090	Inhibitor	99.47%
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.

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-79583

Glutaminase-IN-3	Inhibitor	98.47%
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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Glutaminase

Glutaminase

Glutaminase Related Products (45)

Antibodies (6)

Glutaminase Related Products (45):