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

Glutaminase

Glutaminase is an amidohydrolase enzyme that generates glutamate from glutamine. Glutamate production by mitochondrial glutaminase is a key process for body homeostasis, and a crucial carbon donor for amino acid and lipid synthesis in tumor cells.

Glutaminase has tissue-specific isoenzymes. Three mammalian glutaminases have been identified: the liver-type [LGA or GLS2], the kidney-type [KGA] and Glutaminase C [GAC] a splice variant of KGA (both usually referred to as GLS1). GLS1 is a therapeutic target for cancer. GLS1 catalyzes the hydrolysis of glutamine to glutamate, which is used in the citric acid cycle (TCA) of cancer cells undergoing an aberrant glycolytic flux as a non-glucose-derived source for anaplerosis. GAC plays an essential role in the transformation of NIH 3T3 fibroblasts by Rho GTPases, as well as in the proliferative and invasive activities of various cancer cells.

Glutaminase 相关产品 (8):

Cat. No. Product Name Effect Purity
  • HY-12248
    Telaglenastat Inhibitor 99.92%
    Telaglenastat (CB-839) 是一种一流的,可逆性的,具有口服生物活性的谷氨酰胺酶 1 (glutaminase 1 (GLS1)) 抑制剂。Telaglenastat (CB-839) 选择性抑制谷氨酰胺酶 1 剪接变异体 KGA 和 GAC,与 GLS2 相比具有更高的选择性。Telaglenastat (CB-839) 在鼠类肾和脑中的内源性谷氨酰胺酶 1 的 IC50 值分别为 23 nM 和 28 nM,而对肝脏中 GLS2 的 IC50>1 μM。Telaglenastat (CB-839) 具有强大的抗肿瘤活性。
  • HY-12683
    BPTES Inhibitor >98.0%
    BPTES是选择性的谷氨酰胺酶变构抑制剂,IC50 为0.16 μM。
  • HY-12682
    Glutaminase C-IN-1 Inhibitor 99.14%
    Glutaminase C-IN-1 (Compound 968) 是 Glutaminase C 变构抑制剂。
  • HY-114334
    Glutaminase-IN-1 Inhibitor 98.05%
    Glutaminase-IN-1 (CB839 derivative) 是CB839 的一个衍生物,是1,3,4-硒二氮基肾型谷氨酰胺酶(KGA) 的变构抑制剂,其IC50 值为1 nM。Glutaminase-IN-1 (CB839 derivative) 具有提高细胞摄取和抗肿瘤的活性。
  • HY-122218
    JHU-083 Inhibitor
    JHU-083 是一种选择性的谷氨酰胺酶 (glutaminase) 拮抗剂,可阻断脑 CD11b+ 细胞和实验性脑疟疾 (ECM) 中的谷氨酰胺酶,导致动物中谷氨酸水平的净降低。
  • HY-108357
    6-Diazo-5-oxo-L-nor-Leucine Antagonist >99.0%
    L-6-Diazo-5-oxonorleucine (L-6-Diazo-5-oxonorleucine) 是一种谷氨酰胺拮抗剂,其Ki 值为 6 μM。L-6-Diazo-5-oxonorleucine 具有镇痛、抗菌、抗病毒和抗癌作用。L-6-Diazo-5-oxonorleucine 在体外表现出遗传毒性。L-6-Diazo-5-oxonorleucine 能降低肿瘤细胞的自我更新能力和转移能力 。
  • HY-119377
    UPGL00004 Inhibitor
    UPGL00004 是一种有效的谷氨酰胺酶 C (GAC) 抑制剂 (IC50=29 nM; Kd=27 nM)。UPGL00004 强烈抑制高度侵袭性三阴性乳腺癌细胞系的增殖。
  • HY-19359
    ZED-1227 Inhibitor
    ZED-1227 是一种特异性的、口服的转谷氨酰胺酶 2 (TG2) 抑制剂,能阻塞炎症诱导的 TG2 表达和激活,有作为治疗乳糜泻药物的前景。
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