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

Glutaminase (谷氨酰胺酶)

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 相关产品 (14):

目录号 产品名 作用方式 纯度
  • HY-12248
    Telaglenastat Inhibitor ≥98.0%
    Telaglenastat (CB-839) 是一种首创的,选择性的,可逆性的,口服活性的谷氨酰胺酶 1 (GLS1) 抑制剂。Telaglenastat 抑制 GLS1 剪接变异体 KGAGAC,比 GLS2 具有更高的选择性。Telaglenastat 对小鼠类肾和脑中的内源性谷氨酰胺酶的 IC50 值分别为 23 nM 和 28 nM。Telaglenastat 还可诱导细胞自噬 (autophagy),并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-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-122218
    JHU-083 Antagonist
    JHU-083 是 6-diazo-5-oxo-L-norleucine (DON; HY-108357) 的前药,是一种口服有效的,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-12682
    Glutaminase C-IN-1 Inhibitor 99.61%
    Glutaminase C-IN-1 (Compound 968) 是 Glutaminase C 变构抑制剂。
  • HY-121167
    L-Albizziin Inhibitor ≥98.0%
    L-albizziin 为一种巯基试剂,是谷氨酰胺酶抑制剂。L-albizziin 可用于癌症研究。
  • HY-12248A
    Telaglenastat hydrochloride Inhibitor
    Telaglenastat (CB-839) hydrochloride 是一种首创的,选择性的,可逆性的,口服活性的谷氨酰胺酶 1 (GLS1) 抑制剂。Telaglenastat hydrochloride 抑制 GLS1 剪接变异体 KGAGAC,比 GLS2 具有更高的选择性。Telaglenastat hydrochloride 对小鼠类肾和脑中的内源性谷氨酰胺酶的 IC50 值分别为 23 nM 和 28 nM。Telaglenastat hydrochloride 还可诱导细胞自噬 (autophagy),并具有强大的抗肿瘤活性。
  • 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-19359
    ZED-1227 Inhibitor 99.97%
    ZED-1227 是一种特异性的,具有口服活性的转谷氨酰胺酶 2 (TG2) 抑制剂,IC50值为 45 nM。ZED-1227 能阻塞炎症诱导的 TG2 表达和激活,可用于乳糜泻的研究。
  • HY-12337
    GK921 Inhibitor 99.92%
    GK921是转谷氨酰胺酶2 (TGase2) 抑制剂,对人类重组TGase2的IC50值为7.71 μM。
  • HY-103671
    IPN60090 Inhibitor 99.14%
    IPN-60090 是一种具有口服活性和高选择性的谷氨酰胺酶 1 GLS1 的抑制剂 (IC50=31 nM),对 GLS-2 无活性。IPN-60090 在体内表现出优良的物理化学和药代动力学特性。IPN-60090 可用于实体肿瘤的研究,如肺癌和卵巢癌。
  • HY-103671A
    IPN60090 dihydrochloride Inhibitor 99.05%
    IPN-60090 dihydrochloride 是一种具有口服活性和高选择性的谷氨酰胺酶 1 GLS1 的抑制剂 (IC50=31 nM),对 GLS-2 无活性。IPN-60090 dihydrochloride 在体内表现出优良的物理化学和药代动力学特性。IPN-60090 dihydrochloride 可用于实体肿瘤的研究,如肺癌和卵巢癌。
  • HY-79583
    Glutaminase-IN-3 Inhibitor
    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。
  • HY-119377
    UPGL00004 Inhibitor ≥98.0%
    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。
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