Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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。 | |||
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. |