Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6820 |
D-α-Hydroxyglutaric acid disodium
D-alpha-Hydroxyglutaric acid disodium salt,(R)-2-羟基戊二酸二钠盐,Disodium (R)-2-Hydroxyglutarate |
ATPase; Others; Reactive Oxygen Species; Endogenous Metabolite; mTOR | Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; NF-κB; Others; PI3K/Akt/mTOR signaling |
D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-Hydroxyglutarate) 是神经代谢疾病 D-2-羟基戊二酸尿症中积累的主要代谢产物,可增加活性氧的产生。它是 α-酮戊二酸 (α-KG) 的弱竞争拮抗剂,可抑制多种α-KG 依赖性双加氧酶,Ki 为 10.87 mM。 | |||
T79745 |
IDH2R140Q-IN-2
|
Dehydrogenase | Metabolism |
IDH2R140Q-IN-2 是一种具有口服活性和高效性的 IDH2R140Q 抑制剂,IC50为29 nM。IDH2R140Q-IN-2 具有潜在的抗肿瘤活性,能减少携带IDH2R140Q突变的TF-1细胞系中D2HG的生成(IC50为10 nM),抑制肿瘤组织中D2HG的水平。IDH2R140Q-IN-2适用于研究急性髓系白血病(AML)。 | |||
T63193 |
IDH2R140Q-IN-1
|
||
IDH2R140Q-IN-1 是IDH2R140Q 有效的抑制剂(IC50: 6.1 nM),能够用于急性髓细胞白血病的研究。 | |||
T1809 |
AGI-6780
|
Dehydrogenase; Isocitrate Dehydrogenase (IDH) | Metabolism |
AGI6780 能够选择性抑制肿瘤相关突变体IDH2R140Q,IC50=23±1.7 nM。它对IDH2WT 的作用效果微弱,IC50=190±8.1 nM。 | |||
T2346 |
Enasidenib
恩西地平,AG-221 |
Dehydrogenase; Isocitrate Dehydrogenase (IDH) | Metabolism |
Enasidenib (AG-221) 是口服具有活力的、可逆的、选择性IDH2突变酶抑制剂,抑制IDH2R140Q 和 IDH2R172K 的IC50分别为100 和 400 nM。 | |||
T2346L |
Enasidenib mesylate
AG221 mesylate,AG 221 mesylate,恩西地平甲磺酸盐,AG-221 mesylate |
Dehydrogenase | Metabolism |
Enasidenib mesylate (AG-221 mesylate) 是一种具有有效性和选择性的 IDH2 突变酶抑制剂,可促进白血病成髓细胞的分化,可用于治疗急性髓系白血病。 | |||
T39716 |
Mutant IDH1-IN-6
Mutant IDH1-IN-6 |
||
Mutant IDH1-IN-6 is an orally active compound that effectively inhibits mutant isocitrate dehydrogenase (IDH) enzymes. It demonstrates potency and selectivity, with IC50 values of 6.27, 3.71, 36.9, and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q, and IDH2 R172K mutants, respectively. Notably, Mutant IDH1-IN-6 exhibits lower activity in inhibiting wild-type IDH enzymes. | |||
T7307 |
Vorasidenib
PVM/MA,PVM/MA共聚物,AG-881 |
Isocitrate Dehydrogenase (IDH) | Metabolism |
Vorasidenib (PVM/MA) 是口服具有活力的、脑渗透的突变体异柠檬酸脱氢酶 1 和 2 双重抑制剂。 | |||
T63402 |
(S,R)-WT IDH1 Inhibitor 2
|
||
(S,R)-WT IDH1 Inhibitor 2 是选择性的、有效的突变型 IDH1抑制剂,能够抑制 R132G (IC50: 2.9 nM)、R132C (IC50: 3.8 nM)、R132H (IC50: 4.6 nM) 和 WT IDH1 (IC50: 46 nM),选择性比 IDH2 高出 100 倍。(S,R)-WT IDH1 Inhibitor 2 具有诱导细胞内 2-HG 减少,髓细胞分化阻滞失效的作用,并且在白血病母细胞和更不成熟的干细胞水平诱导粒细胞分化,可研究用于急性髓系白血病 (AML) 及其他癌症。 | |||
T78758 |
IHMT-IDH1-053
|
Isocitrate Dehydrogenase (IDH) | Metabolism |
IHMT-IDH1-053(compound 16)为高选择性不可逆IDH1R132H突变抑制剂,IC50值仅为4.7 nM。对IDH1wt和IDH2wt/突变体活性低。该化合物在IDH1R132H突变293T细胞中显著抑制2-羟基戊二酸(2-HG)生成,IC50为28 nM。IHMT-IDH1-053通过与IDH1R132H蛋白的Cys269残基形成共价键,结合至NADPH结合袋附近的变构袋。此外,它能够抑制携带IDH1R132突变的HT1080细胞系及原代AML细胞增殖。 |