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Home >> Signaling Pathways >> Proteases >> Glutaminase

Glutaminase(谷氨酰胺酶)

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.

Products for  Glutaminase

  1. Cat.No. 产品名称 Information
  2. GC73547 PROTAC TG2 degrader-2 PROTAC TG2 degrader-2（化合物7）是靶向转谷氨酰胺酶2 （TG2）的选择性竞争性降解物，Kd为100 μM。
  3. GC72400 Zampilimab Zampilimab（UCB-7858）是一种针对转谷氨酰胺酶2（TG2）的单克隆抗体。
  4. GC71455 TG-2-IN-4 TG-2-IN-4（化合物8）是一种转谷氨酰胺酶2（TG2）抑制剂，IC50＜0.5mM。
  5. GC70020 TG-2-IN-1 TG-2-IN-1 (Compound D003) 是一种转谷氨酰胺酶-2 (TGM-2) 抑制剂。TG-2-IN-1 可用于近视研究。
  6. GC25536 JHU395 JHU395 is a novel orally bioavailable GA (glutamine antagonists) prodrug designed to circulate inert in plasma, but permeate and release active GA within target tissues. JHU395 delivers active GA to malignant peripheral nerve sheath tumor (MPNST), and significantly inhibits tumor growth without observed toxicity.
  7. GC67898 GLS-1-IN-1 GLS-1-IN-1 (compound 1d) 是一种 GLS-1 抑制剂。GLS-1-IN-1 对 Hep G2、MCF 7 和 MCF 10A 细胞有抑制作用。
  8. GC66717 2-Amino-2-(p-tolyl)acetic acid 2-Amino-2-(p-tolyl)acetic acid 可用于优化叠氮骨架，是 1,3,4- 噻二唑类化合物的中间体。1,3,4- 噻二唑类化合物具有出潜在的抗癌活性，并对谷氨酰胺酶有抑制作用。
  9. GC64531 KCC009 KCC009 是转谷氨酰胺酶 2 的抑制剂，可诱导 p53 途径依赖的放疗敏感性。
  10. GC62618 IPN60090 IACS-6274 (IPN60090), is a potent, selective and orally active glutaminase inhibitor with potential antineoplastic and immunostimulating activities.
  11. GC62285 Glutaminase-IN-3

    N-[6-[4-(5-氨基-1,3,4-噻二唑-2-基)丁基]-3-哒嗪基]-3-(三氟甲氧基)苯乙酰胺

     Glutaminase-IN-3 (compound 657) 是一种有效的 glutaminase 抑制剂，对GLS1的 IC50 值为0.24 μM。详细情况请参见专利 WO2014089048A1，compound 657。
  12. GC37963 ZED-1227 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。
  13. GC36368 JHU-083 JHU-083 (Ethyl 2-(2-Amino-4-methylpentanamido)-DON) is a novel prodrug of DON.JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress.Solutions are best fresh-prepared.
  14. GC41224 6-diazo-5-oxo-L-nor-Leucine

    6-重氮-5-氧代-L-正亮氨酸; L-6-Diazo-5-oxonorleucine; DON

     6-Diazo-5-oxo-L-nor-Leucine (DON)是一种抑制谷氨酰胺酶的谷氨酰胺类似物,是一种选择性的、基于机制的谷氨酰胺酶失活剂。
  15. GC33274 Glutaminase-IN-1

    CB839 derivative

     Glutaminase-IN-1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1nM.Glutaminase-IN-1具有提高细胞摄取和抗肿瘤的活性。
  16. GC19171 Glutaminase C-IN-1

    5-[3-溴-4-(二甲胺基)苯基]-2,3,5,6-四氢-2,2-二甲基苯并[A]菲啶-4(1H)-酮,Compound 968

     An inhibitor of glutaminase C
  17. GC13958 BPTES An allosteric inhibitor of GLS1
  18. GC15227 CB-839

    Telaglenastat

     Telaglenastat (CB-839) 是一流的、可逆的和具有口服生物利用度的谷氨酰胺酶 1 (GLS1) 抑制剂。

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