kga

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。

KGA-2727是选择性，高亲和力和口服有效的 SGLT1抑制剂，对人和大鼠 SGLT1的 Ki 分别为 97.4 nM 和 43.5 nM，对 SGLT1的选择性比人SGLT2 高 140 倍 ，大鼠SGLT2高390 倍。KGA-2727具有抗糖尿病活性。

Patidegip, laos known as Saridegib and IPI-926, is an orally bioavailable, cyclopamine-derived (for structure comparison see Fig 1) inhibitor of the Hedgehog (Hh) pathway with potential antineoplastic activity. Specifically, Hedgehog pathway inhibitor IPI-926 binds to and inhibits the cell membrane-spanning G-protein coupled receptor SMO, which may result in the suppression of Hh pathway signaling and a decrease in tumor cell proliferation and survival. SMO is activated upon binding of Hh ligand to the cell surface receptor Patched (PTCH); inappropriate activation of Hh signaling and uncontrolled cellular proliferation may be associated with SMO mutations.

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。

Mizagliflozin 是口服有效的、选择性的 SGLT1抑制剂，对人 SGLT1 的 Ki 值为 27 nM。Mizagliflozin 对 SGLT1 的选择性是 SGLT2的303 倍。Mizagliflozin 是抗糖尿病药物，可以改善餐后血糖波动并有可能有改善慢性便秘的潜力。

BPTES 是一种特异性 GlutamiN Ase GLS1 (KGA) 抑制剂，IC50=0.16 μM。

GSNKGAIIGLM(131602-53-4(free base)) (Amyloid beta-peptide(25-35)) 是阿尔茨海默病淀粉样蛋白 β-肽的片段 Aβ(25-35)。

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.