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Search Results for " mutant idh1 inhibitor "

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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
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)。
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,。
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))。
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。
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。
T11612	IDH1 Inhibitor 3	Others	Others
	IDH1 Inhibitor 3 is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor (IC50: 45 nM for IDH1R132H).
T12129	Mutant IDH1-IN-4	Others	Others
	Mutant IDH1-IN-4 is an mutant Isocitrate dehydrogenase 1 (IDH 1) inhibitor.
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)。
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.
T11613	IDH1 Inhibitor 1	Others	Others
	IDH1 Inhibitor 1 is an orally bioavailable, brain-penetrant, and selective mutant IDH1 inhibitor (IC50s: 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT).
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).
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。
T63778	Safusidenib
	Safusidenib 是选择性的、口服具有活力的 IDH1 突变型抑制剂，对突变型 IDH1 具有显著抑制作用，但不能抑制野生型 IDH1，能够抑制软骨肉瘤中的肿瘤活性。Safusidenib 对IDH1R132H 和 IDH1R132C 具有活性，在没有预孵育的情况下，IC50 值分别为 15 和 130 nM。
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).
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。
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。
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 inhibitor

Cat.No: T16161

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Mutant IDH1-IN-1

Cat.No: T2043

Synonym: IDH1-IN-1

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Mutant IDH1-IN-2

Cat.No: T12128

Target: Isocitrate Dehydrogenase (IDH)

Cat.No: T15551

Target: Dehydrogenase

Cat.No: T15550

Target: Dehydrogenase

Cat.No: TQ0042

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Cat.No: T16384

Synonym: FT-2102

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

IDH1 Inhibitor 3

Cat.No: T11612

Target: Others

Mutant IDH1-IN-4

Cat.No: T12129

Target: Others

IDH1 Inhibitor 5

Cat.No: T62725

Cat.No: T70890

IDH1 Inhibitor 1

Cat.No: T11613

Target: Others

Cat.No: T15442

Target: Others

WT IDH1 Inhibitor 2

Cat.No: T63403

Cat.No: T63778

Cat.No: T32009

Synonym: GSK 321,GSK-321

ML-309 (hydrochloride)

Cat.No: T38004

(S,R)-WT IDH1 Inhibitor 2

Cat.No: T63402

Cat.No: T62698

IHMT-IDH1-053

Cat.No: T78758

Target: Isocitrate Dehydrogenase (IDH)

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。

天然产物

Alternaphenol B2

Cat.No: T83133

Target: Isocitrate Dehydrogenase (IDH)

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