Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11611 |
IDH1 Inhibitor 2
|
Dehydrogenase | Metabolism |
IDH1 Inhibitor 2 (compound 13) is a potent IDH1 inhibitor via direct covalent modification of His315 (IC50: 110 nM). | |||
T12128 |
Mutant IDH1-IN-2
|
Isocitrate Dehydrogenase (IDH) | Metabolism |
Mutant IDH1-IN-2是突变型异柠檬酸脱氢酶蛋白抑制剂, 在荧光生物化学检测中IC50为16.6 nM,LS-MS 生物化学检测中IC50为<22 nM,。 | |||
T63403 | WT IDH1 Inhibitor 2 | ||
WT IDH1 Inhibitor 2 是一种野生型异柠檬酸脱氢酶1 (WT IDH1) 抑制剂 (IC50: 120 nM),是突变体R132H IDH1抑制剂,是 GSK321 的异构体,具有野生型交叉反应性。 | |||
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。 | |||
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。 | |||
T3617 |
Ivosidenib
艾伏尼布,AG-120 |
Dehydrogenase; Isocitrate Dehydrogenase (IDH) | Metabolism |
Ivosidenib (AG-120) 是一种口服具有活力的异柠檬酸脱氢酶 1 的突变体酶 (mIDH1 enzyme) 抑制剂,能够使 d-2- hydroxyglutatrate (2-HG) 在体内降低。它具有良好的的安全性和临床活性,具有研究 AML 的潜力。 | |||
T15551 |
IDH889
|
Dehydrogenase | Metabolism |
IDH889 是可口服有效的,脑渗透性的,变构和突变特异性的异柠檬酸脱氢酶抑制剂,对 IDH1 R132* 突变型具有高效选择性。它高效抑制细胞内 2-HG 水平,IC50为 0.014 μM。 | |||
T62725 |
IDH1 Inhibitor 5
|
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IDH1 Inhibitor 5 (compound 2) 是一种 IDH1(异柠檬酸脱氢酶 1)的抑制剂。IDH1 Inhibitor 5 能够抑制 MOG 细胞 (IC50: 64.4 nM) 以及表达外源突变 IDH1 R132H 蛋白的野生型 IDH1 胶质瘤细胞 (IC50: 34.9 nM)。 | |||
T70890 |
ML309
|
||
ML309 is a potent inhibitor of R132H mutant IDH1 capable of reducing 2-hydroxyglutarate production in U87 MG glioblastoma cells. ML309 is capable of potent and selective inhibition of mutant IDH1 and effectively lowers cell-based production of 2-HG in a U87MG mutant glioblastoma cell line. | |||
T32009 |
GSK321
GSK 321,GSK-321 |
||
GSK321 is an effective and selective IDH1 mutation inhibitor, which can effectively inhibit the production of 2-HG in HT-1080 cells, and induce IDH1 mutant cells to differentiate into bone marrow at the level of leukemia blasts and more stem cells. | |||
T38004 |
ML-309 (hydrochloride)
|
||
ML-309 is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). It reversibly and selective inhibits IDH1R132H over wild-type IDH1 (IC50s = 96 and 36,500 nM, respectively). ML-309 reduces 2-hydroxyglutarate production in U87 MG glioblastoma cells (EC50 = 55 nM). | |||
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。 | |||
T62698 | mIDH1-IN-1 | ||
mIDH1-IN-1 (compound 43) 是一种有效的、选择性的 mIDH1 (异柠檬酸脱氢酶 1 突变体) 抑制剂 (IC50: 961.5 nM)。mIDH1-IN-1 可以有效抑制 HT1080 细胞内 2-HG (2-hydroxyglutarate) 的产生 (EC50: 208.6±8.0 nM)。mIDH1-IN-1 对 IDH1 突变体 U-87 细胞表现出明显的抗增殖效果(IC50: 41.8 nM)。mIDH1-IN-1 是一种抗肿瘤剂,能够用于研究 IDH1 突变实体瘤。 |