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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T76174 |
Isocitrate dehydrogenase
|
||
Isocitrate dehydrogenase(ICDH) 异柠檬酸脱氢酶是一种柠檬酸或三羧酸循环酶,常用于生化研究。Isocitrate dehydrogenase 催化异柠檬酸氧化脱羧生成 α-酮戊二酸,并将 NAD(P)+还原为 NAD(P)H,在细胞代谢中起重要作用。 | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
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))。 | |||
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。 | |||
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,。 | |||
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。 | |||
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。 | |||
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。 | |||
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)。 | |||
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。 | |||
T22253 |
AG-120 (racemic)
1-(4-氰基-2-吡啶基)-5-氧代-L-脯氨酰-2-(2-氯苯基)-N-(3,3-二氟环丁基)-N2-(5-氟-3-吡啶基)甘氨酰胺 |
Dehydrogenase | Metabolism |
AG-120 (racemic) 是 AG-120 的外消旋混合物,是一种可口服的异柠檬酸脱氢酶 1 型 (IDH1) 抑制剂,具有潜在的抗肿瘤活性。 | |||
T28932 | TC-E 5008 | ||
TC-E 5008 is a selective inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1). | |||
T12129 | Mutant IDH1-IN-4 | Others | Others |
Mutant IDH1-IN-4 is an mutant Isocitrate dehydrogenase 1 (IDH 1) inhibitor. | |||
T15442 |
GSK864
|
Others | Others |
GSK864 is an inhibitor of isocitrate dehydrogenase 1 (IDH1) mutant. GSK864 inhibits IDH1 mutants R132C, R132H, and R132G (IC50: 8.8, 15.2, and 16.6 nM). | |||
T70315 |
AGI-16903
|
||
AGI-16903 is a metabolite of enasidenib -- an isocitrate dehydrogenase-2 inhibitor that has been shown to inhibit human nucleoside transporters and uptake of azacitidine in oocytes. | |||
T23945 |
DA-11004
DA11004,UNII-48M66E9ER2 |
||
DA-11004 is a potent NADP-dependent isocitrate dehydrogenase inhibitor (IC50: 1.49 μM for IDPc). DA-11004 inhibited fatty acid synthesis in adipose tissues via IDPc inhibition. It also decreased the plasma glucose levels and FFA in HF diet-induced obesity | |||
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). | |||
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。 | |||
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. | |||
T62725 |
IDH1 Inhibitor 5
|
||
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)。 | |||
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。 | |||
T35520 |
Aflatoxin G1-13C17
Aflatoxin G1-13C17 |
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Aflatoxin G1-13C17is intended for use as an internal standard for the quantification of aflatoxin G1by GC- or LC-MS. Aflatoxin G1is a mycotoxin that has been found inA. terricola.1In vivo, aflatoxin G1is lethal to ducklings (LD50= 1.18 mg/kg).2It induces hepatocellular carcinoma tumor formation and lethality in rats when administered at doses of 1.4 and 3 mg/animal, respectively. Aflatoxin G1also inhibits liver and kidney succinate dehydrogenase and fumarase, as well as kidney cytochrome oxidase... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T83133 |
Alternaphenol B2
|
Isocitrate Dehydrogenase (IDH) | Metabolism |
IDH1 Inhibitor 是一种化学化合物,其通过选择性抑制异柠檬酸脱氢酶1 (IDH1) 酶的活性来起作用。这种抑制剂对R132突变的IDH1酶特别有效,因此在某些类型的癌症治疗中具有潜在的应用价值。IDH1 Inhibitor能够阻断异常的代谢途径和纠正肿瘤细胞增殖的代谢异常。在药物研发和临床试验中,研究人员评估其对特定肿瘤生长的抑制效果及其安全性和耐受性。 |