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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。
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | 询价 | 期货 | |
50 mg | 询价 | 期货 |
产品描述 | IHMT-IDH1-053 (compound 16) is an irreversible inhibitor exhibiting high selectivity for the IDH1 R132H mutant, achieving an IC50 of 4.7 nM. It preferentially targets IDH1 mutants over wild-type IDH1 and IDH2, both wild-type and mutants. In 293T cells transfected with the IDH1 R132H mutant, IHMT-IDH1-053 reduces 2-hydroxyglutarate (2-HG) production with an IC50 value of 28 nM. The compound engages with the R132H protein at an allosteric site near the NAPDH binding region, forming a covalent linkage with Cys269. Additionally, IHMT-IDH1-053 impedes the growth of both the HT1080 cell line and primary acute myeloid leukemia (AML) cells harboring IDH1 R132 mutations [1]. |
靶点活性 | R132H IDH1:4.7 μM |
分子量 | 532.63 |
分子式 | C25H33FN6O4S |
存储 | Shipping with blue ice. |
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