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.
Glutaminase 相关产品(17)
- GC19171Glutaminase C-IN-1CAS: 311795-38-7纯度: >98.00%
Glutaminase C-IN-1是一种小分子，可作为谷氨酰胺酶的变构抑制剂，阻断谷氨酰胺分解并影响谷氨酰胺代谢。
- GC25536JHU395CAS: 2079938-92-2
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.
- GC33274Glutaminase-IN-1CAS: 2247127-79-1纯度: >98.00%
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。
- GC36368JHU-083CAS: 1998725-11-3纯度: >98.00%
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.
- GC412246-diazo-5-oxo-L-nor-LeucineCAS: 157-03-9纯度: >98.00%
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。
- GC62285Glutaminase-IN-3CAS: 1439399-45-7纯度: >98.00%
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。
- GC667172-Amino-2-(p-tolyl)acetic acidCAS: 13227-01-5纯度: >96.00%
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。
- GC67898GLS-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。
- GC73547PROTAC TG2 degrader-2纯度: >99.00%
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。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC13958 | BPTES | 314045-39-1 | >98.00% | |
BPTES是一种高效且选择性的肾型谷氨酰胺酶（GLS）变构抑制剂，已被用作分子探针以确定GLS抑制的治疗潜力。 | ||||
| GC15227 | CB-839 | 1439399-58-2 | >99.50% / >99.00% | |
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。 | ||||
| GC19171 | Glutaminase C-IN-1 | 311795-38-7 | >98.00% | |
Glutaminase C-IN-1是一种小分子，可作为谷氨酰胺酶的变构抑制剂，阻断谷氨酰胺分解并影响谷氨酰胺代谢。 | ||||
| GC25536 | JHU395 | 2079938-92-2 | - | |
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. | ||||
| GC33274 | Glutaminase-IN-1 | 2247127-79-1 | >98.00% | |
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。 | ||||
| GC36368 | JHU-083 | 1998725-11-3 | >98.00% | |
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. | ||||
| GC37963 | ZED-1227 | 1542132-88-6 | >99.50% | |
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。 | ||||
| GC41224 | 6-diazo-5-oxo-L-nor-Leucine | 157-03-9 | >98.00% | |
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。 | ||||
| GC62285 | Glutaminase-IN-3 | 1439399-45-7 | >98.00% | |
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。 | ||||
| GC62618 | IPN60090 | 1853164-83-6 | >99.00% | |
IACS-6274 (IPN60090), is a potent, selective and orally active glutaminase inhibitor with potential antineoplastic and immunostimulating activities. | ||||
| GC64531 | KCC009 | 744198-19-4 | >98.00% | |
KCC009是一种高特异性、不可逆的transglutaminase 2 (TG2)抑制剂，可诱导不依赖于p53的放射增敏作用。 | ||||
| GC66717 | 2-Amino-2-(p-tolyl)acetic acid | 13227-01-5 | >96.00% | |
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。 | ||||
| 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。 | ||||
| GC70020 | TG-2-IN-1 | 135273-74-4 | >98.00% | |
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。 | ||||
| GC71455 | TG-2-IN-4 | 2410899-01-1 | 不显示 | |
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。 | ||||
| GC72400 | Zampilimab | 2098280-42-1 | >98.00% | |
Zampilimab（UCB-7858）是一种针对转谷氨酰胺酶2（TG2）的单克隆抗体。 | ||||
| GC73547 | PROTAC TG2 degrader-2 | - | >99.00% | |
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。 | ||||