15
1
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T15550 |
IDH-305
|
Dehydrogenase | Metabolism |
IDH-305 是突变选择性的、口服性的、脑渗透性的 IDH1抑制剂,靶向 IDH1 (R132) 突变。它对突变体 IDH1 亚型的选择性比野生型高 200 倍 (IC50= 27 nM (IDH1R132H), 28 nM (IDH1R132C), 6.14 µM (IDH1WT))。 | |||
T2104 |
AGI-5198
IDH-C35 |
Dehydrogenase; Isocitrate Dehydrogenase (IDH) | Metabolism |
AGI-5198 (IDH-C35) 是一种选择性的突变体 IDH1R132H 抑制剂,IC50=0.07 μM。 | |||
T16161 |
Mutant IDH1 inhibitor
|
Dehydrogenase; Isocitrate Dehydrogenase (IDH) | Metabolism |
Mutant IDH1 inhibitor 是一种突变型IDH1 R132H 的抑制剂,IC50<72 nM。 | |||
T7741 |
DS-1001b
|
Dehydrogenase; Isocitrate Dehydrogenase (IDH) | Metabolism |
DS-1001b 是IDH-1(异柠檬酸脱氢酶-1) 突变体抑制剂。 | |||
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,。 | |||
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。 | |||
TQ0042 |
BAY-1436032
|
Dehydrogenase; Isocitrate Dehydrogenase (IDH) | Metabolism |
BAY-1436032 是一种选择性泛突变异柠檬酸脱氢酶 1 新型口服抑制剂。 | |||
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。 | |||
T2043 |
Mutant IDH1-IN-1
IDH1-IN-1 |
Dehydrogenase; Isocitrate Dehydrogenase (IDH) | Metabolism |
Mutant IDH1-IN-1 是 IDH1突变体的选择性抑制剂,能够作用于突变体 IDH1 R132C/R132C (IC50:4 nM) ,IDH1 R132H/R132H (IC50:42 nM) ,IDH1 R132H/WT (IC50:80 nM) 和野生型 IDH1 (IC50:143 nM)。 | |||
T16384 |
Olutasidenib
FT-2102 |
Dehydrogenase; Isocitrate Dehydrogenase (IDH) | Metabolism |
Olutasidenib (FT-2102) 是一种可透过血脑屏障的、具有口服活性的、突变型异柠檬酸脱氢酶(IDH)1的选择性有效抑制剂,对IDH1- R132H 和 IDH1- R132C 的IC50分别为 21.2 nM 和 114 nM,可用于急性髓性白血病或骨髓增生异常综合征的研究。 | |||
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。 | |||
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。 | |||
T12129 | Mutant IDH1-IN-4 | Others | Others |
Mutant IDH1-IN-4 is an mutant Isocitrate dehydrogenase 1 (IDH 1) inhibitor. | |||
T39716 |
Mutant IDH1-IN-6
Mutant IDH1-IN-6 |
Others | Others |
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. |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-02413 |
Isocitrate dehydrogenase/IDH1 Protein, Human, Recombinant (His)
HEL-S-26,HEL-216,IDP,IDCD,PICD,IDH,isocitrate |
Human | E. coli |
Isocitrate dehydrogenase/IDH1 Protein, Human, Recombinant (His) is expressed in E. coli expression system with His tag. The predicted molecular weight is 48 kDa and the accession number is O75874. |