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20

抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T3964 Glutaminase C-IN-1

Compound 968,Glutaminase Inhibitor Compound 968

Glutaminase Proteases/Proteasome
Glutaminase C-IN-1 (Compound 968) 是一种 Glutaminase C 变构抑制剂。
T37385 Glutaminase-IN-3

Glutaminase Proteases/Proteasome
Glutaminase-IN-3 是一种有效的的 Glutaminase 1 抑制剂,具有潜在的抗肿瘤活性,对 GLS1 具有抑制作用,可用于研究癌症。
T11421 Glutaminase-IN-1

CB839 derivative

transporter Metabolism
Glutaminase-IN-1 (CB839 derivative),是一种新型 1,3,4-硒二氮基肾型谷氨酰胺酶(KGA) 的变构抑制剂,在侵袭性 H22 肝癌异种移植模型中显示出抗肿瘤活性。
T6791 BPTES

transporter; Glutaminase Metabolism; Proteases/Proteasome
BPTES 是一种特异性 GlutamiN/Ase GLS1 (KGA) 抑制剂,IC50=0.16 μM。
T63137 Glutaminase-IN-4

Glutaminase-IN-4 (compound 2a) 是一种谷氨酰胺酶 (GLS) 抑制剂 (IC50: 2.3 μM)。
T83914 Glutaminase C Inhibitor 11

Glutaminase C inhibitor 11是一种glutaminase C (GAC)的抑制剂。它能够抑制GAC酶的活性(EC50 = 10.64 nM),降低A549非小细胞肺癌(NSCLC)细胞的活力(IC50 = 4.025 nM)。在A549细胞中,Glutaminase C inhibitor 11(0.1和1 µM)能减少细胞集落形成并降低细胞内谷氨酸水平。在体内,Glutaminase C inhibitor 11(100 mg/kg)能够减缓A549小鼠异位瘤模型中的肿瘤生长。
T78892 Glutaminase C-IN-2

Glutaminase Proteases/Proteasome
GlutaminaseC-IN-2(compound 11)为GAC变构抑制剂,IC50值为10.64 nM。该化合物通过干扰谷氨酰胺代谢,调控细胞代谢产物,进而提高ROS水平,并展现出抗癌活性。
T3968 GK921

Glutaminase Proteases/Proteasome
GK921 是一种转谷氨酰胺酶2 抑制剂,对人类重组TGase2的IC50=为7.71 μM。
T6797 Telaglenastat

CB 839,CB839,CB-839

transporter; Glutaminase; Autophagy Autophagy; Metabolism; Proteases/Proteasome
Telaglenastat (CB 839) 是一种选择性可逆的,有口服活性的谷氨酰胺酶 1 (GLS1) 抑制剂,抑制 GLS1剪接变异体 KGA 和 GAC,比 GLS2 具有更高的选择性。它可诱导细胞自噬 ,具有抗肿瘤活性。它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。
T20121 L-Albizziin

NSC-132089,L-beta-Ureidoalanine,L-Albizziine,Albizzine,NSC 132089,Albizziin,L-脲基丙氨酸

Glutaminase Proteases/Proteasome
L-Albizziin (L-beta-Ureidoalanine) 是一种巯基试剂,是一种谷氨酰胺酶抑制剂,可用于研究癌症。
T78362 Transglutaminase

TG

Transglutaminase (TG) 是一种硫醇酶,促使蛋白质分子间交联,通过催化谷氨酰胺残基的γ-羧酰胺基团与其他化合物的一级ε-胺基团形成异肽键。该酶在包括凝血、抗菌免疫反应和光合作用在内的多种生理过程中发挥作用。
T17206 UPGL00004

Others; Glutaminase Others; Proteases/Proteasome
UPGL00004 是一种有效的谷氨酰胺酶 C (GAC) 抑制剂 ,其 IC50为29 nM。UPGL00004 对 GAC 的 Kd 为27 nM。UPGL00004 对高度侵袭性三阴性乳腺癌细胞系的增殖具有很强的抑制作用 。
T11412 IPN60090

GLS1-IN-1

Others; transporter Metabolism; Others
IPN60090是一种新型、强效、口服生物利用度高的 肾型谷氨酰胺酶(GLS1)特异性抑制剂,对GLS1的IC50值为31 nM。IPN60090 具有潜在的抗癌和免疫刺激/免疫调节活性,可选择性地靶向、结合并抑制人谷氨酰胺酶,可用于研究 GLS1 介导的疾病。
T39309 Telaglenastat hydrochloride

CB-839 hydrochloride

Telaglenastat (CB-839) hydrochloride is a first-in-class, reversible, and orally active inhibitor of glutaminase 1 (GLS1). It selectively inhibits the splice variants of GLS1, specifically KGA (kidney-type glutaminase) and GAC (glutaminase C), as compared to GLS2. Telaglenastat hydrochloride has an IC50 of 23 nM for endogenous glutaminase in mouse kidney and 28 nM in the brain. In addition, it induces autophagy and exhibits antitumor activity.
T15613 JHU-083

Others Others
JHU-083 is a selective glutaminase antagonist. JHU-083 blocks glutaminase activity in brain CD11b+ cells. JHU-083 also experimental cerebral malaria (ECM) resulting in a net decrease of glutamate levels in the animals.
T28961 THDP-17

THDP 17,THDP17

THDP-17 is a inhibitor of glutaminase. THDP-17 shows a partial uncompetitive inhibition in vitro.
T37222 GLS1 Inhibitor

GLS1 inhibitor is an inhibitor of glutaminase 1 (GLS1; IC50= 0.021 μM).1It inhibits the growth of NCI H1703 non-small cell lung cancer (NSCLC) cellsin vitro(GI50= 0.011 μM). GLS1 inhibitor (100 mg/kg) reduces tumor growth, increases tumor levels of glutamine, and decreases tumor levels of glutamate and aspartate in an NCI H1703 mouse xenograft model. 1.Finlay, M.R.V., Anderton, M., Bailey, A., et al.Discovery of a thiadiazole-pyridazine-based allosteric glutaminase 1 inhibitor series that demons...
T39544 IPN60090 dihydrochloride

IPN60090 dihydrochloride

IPN-60090 dihydrochloride is a potent and specific inhibitor of glutaminase 1 (GLS1) with a remarkable inhibition constant (IC50) of 31 nM. It does not exhibit any inhibitory activity against GLS-2. Furthermore, IPN-60090 dihydrochloride possesses outstanding physicochemical properties and pharmacokinetic characteristics in vivo. Therefore, it is a valuable compound for researching solid tumors, including lung and ovarian cancers.
T64259 GLS1 Inhibitor-5

GLS1 Inhibitor-5 (compound 24y) 是一种选择性的、口服具有活力的谷氨酰胺酶 1 (GLS1) 抑制剂 (IC50: 68 nM)。GLS1 Inhibitor-5 能够诱导细胞凋亡 (apoptosis),表现出抗肿瘤效果。
T73458 LWG-301

LWG-301是一种针对Glutaminase1(GLS1)的变构抑制剂,具有(IC50=7 nM)。通过显著阻断谷氨酰胺代谢并增加细胞内ROS,LWG-301能够诱导细胞凋亡(apoptosis)。在HCT116异种移植模型中,LWG-301展示出中等抗肿瘤活性。

化合物

Glutaminase C-IN-1
Cat.No: T3964
Synonym: Compound 968,Glutaminase Inhibitor Compound 968
Target: Glutaminase
Glutaminase-IN-3
Cat.No: T37385
Synonym:
Target: Glutaminase
Glutaminase-IN-1
Cat.No: T11421
Synonym: CB839 derivative
Target: transporter
BPTES
Cat.No: T6791
Synonym:
Target: transporter, Glutaminase
Glutaminase-IN-4
Cat.No: T63137
Synonym:
Target:
Glutaminase C Inhibitor 11
Cat.No: T83914
Synonym:
Target:
Glutaminase C-IN-2
Cat.No: T78892
Synonym:
Target: Glutaminase
GK921
Cat.No: T3968
Synonym:
Target: Glutaminase
Telaglenastat
Cat.No: T6797
Synonym: CB 839,CB839,CB-839
Target: transporter, Glutaminase, Autophagy
L-Albizziin
Cat.No: T20121
Synonym: NSC-132089,L-beta-Ureidoalanine,L-Albizziine,Albizzine,NSC 132089,Albizziin,L-脲基丙氨酸
Target: Glutaminase
Transglutaminase
Cat.No: T78362
Synonym: TG
Target:
UPGL00004
Cat.No: T17206
Synonym:
Target: Others, Glutaminase
IPN60090
Cat.No: T11412
Synonym: GLS1-IN-1
Target: Others, transporter
Telaglenastat hydrochloride
Cat.No: T39309
Synonym: CB-839 hydrochloride
Target:
JHU-083
Cat.No: T15613
Synonym:
Target: Others
THDP-17
Cat.No: T28961
Synonym: THDP 17,THDP17
Target:
GLS1 Inhibitor
Cat.No: T37222
Synonym:
Target:
IPN60090 dihydrochloride
Cat.No: T39544
Synonym: IPN60090 dihydrochloride
Target:
GLS1 Inhibitor-5
Cat.No: T64259
Synonym:
Target:
LWG-301
Cat.No: T73458
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T8373 6-Diazo-5-oxo-L-nor-Leucine

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

Influenza Virus; Glutaminase; Antibacterial; Antibiotic Microbiology/Virology; Proteases/Proteasome
6-Diazo-5-oxo-L-nor-Leucine (L-6-Diazo-5-oxonorleucine) 是一种谷氨酰胺拮抗剂,具有抗菌、抗病毒和抗癌作用,其Ki 值为 6 μM。它能降低肿瘤细胞的自我更新能力和转移能力 ,在体外表现出遗传毒性。

天然产物

6-Diazo-5-oxo-L-nor-Leucine
Cat.No: T8373
Synonym: DON,L-6-Diazo-5-oxonorleucine,6-重氮-5-氧代-L-正亮氨酸,Diazooxonorleucine
Target: Influenza Virus, Glutaminase, Antibacterial, Antibiotic
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