1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Glutaminase
  4. Glutaminase Inhibitor

Glutaminase Inhibitor

Glutaminase Inhibitors (48):

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-159962
    TGase2-IN-1
    Inhibitor
    TGase2-IN-1 (Compound 22) is an orally active inhibitor for TGase2 with an IC50 of 1.12 μM. TGase2-IN-1 inhibits TGase2 in human retinal microvascular endothelial cells with an IC50 of 0.07 μM. TGase2-IN-1 exhibits 74.6% oral bioavailability. TGase2-IN-1 inhibits retinal vascular leakage in mouse Streptozotocin (HY-13753)-induced diabetic model.
  • 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-16693
    LDN-27219
    Inhibitor 99.64%
    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-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-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-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-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-123290
    KCC009
    Inhibitor 98.06%
    KCC009, a transglutaminase 2 (TG2) inhibitor, induces p53-independent radiosensitization.
  • 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-114334
    Glutaminase-IN-1
    Inhibitor 98.09%
    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-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.
  • HY-P99512
    Zampilimab
    Inhibitor 98.81%
    Zampilimab (UCB-7858) is a monoclonal antibody against transglutaminase 2 (TG2). Zampilimab has potential application in renal transplant.
  • HY-119377
    UPGL00004
    Inhibitor ≥98.0%
    UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.
  • HY-145933
    BJJF078
    Inhibitor 99.34%
    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.