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Cat. No. Product Name Target Signaling Pathways
T2043 Mutant IDH1-IN-1

IDH1-IN-1

Dehydrogenase; Isocitrate Dehydrogenase (IDH) Metabolism
Mutant IDH1-IN-1IDH1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)。
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,。
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。
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.
T12129 Mutant IDH1-IN-4

Others Others
Mutant IDH1-IN-4 is an mutant Isocitrate dehydrogenase 1 (IDH 1) inhibitor.
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。
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).
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-1IDH1 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。
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。

化合物

Mutant IDH1-IN-1
Cat.No: T2043
Synonym: IDH1-IN-1
Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)
Mutant IDH1-IN-2
Cat.No: T12128
Synonym:
Target: Isocitrate Dehydrogenase (IDH)
Mutant IDH1 inhibitor
Cat.No: T16161
Synonym:
Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)
Mutant IDH1-IN-6
Cat.No: T39716
Synonym: Mutant IDH1-IN-6
Target:
Mutant IDH1-IN-4
Cat.No: T12129
Synonym:
Target: Others
Olutasidenib
Cat.No: T16384
Synonym: FT-2102
Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)
ML-309 (hydrochloride)
Cat.No: T38004
Synonym:
Target:
mIDH1-IN-1
Cat.No: T62698
Synonym:
Target:
IHMT-IDH1-053
Cat.No: T78758
Synonym:
Target: Isocitrate Dehydrogenase (IDH)
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