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31

抑制剂 & 化合物

2

天然产物

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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-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)。
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。
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,。
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.
T11611	IDH1 Inhibitor 2	Dehydrogenase	Metabolism
	IDH1 Inhibitor 2 (compound 13) is a potent IDH1 inhibitor via direct covalent modification of His315 (IC50: 110 nM).
T11612	IDH1 Inhibitor 3	Others	Others
	IDH1 Inhibitor 3 is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor (IC50: 45 nM for IDH1R132H).
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).
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)。
T72705	IDH1 Inhibitor 7
	IDH1 Inhibitor7 是一种 IDH1抑制剂，IC50小于100 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。
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。
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。
T6820	D-α-Hydroxyglutaric acid disodium D-alpha-Hydroxyglutaric acid disodium salt,(R)-2-羟基戊二酸二钠盐,Disodium (R)-2-Hydroxyglutarate	ATPase; Others; Reactive Oxygen Species; Endogenous Metabolite; mTOR	Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; NF-κB; Others; PI3K/Akt/mTOR signaling
	D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-Hydroxyglutarate) 是神经代谢疾病 D-2-羟基戊二酸尿症中积累的主要代谢产物，可增加活性氧的产生。它是 α-酮戊二酸 (α-KG) 的弱竞争拮抗剂，可抑制多种α-KG 依赖性双加氧酶，Ki 为 10.87 mM。
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。
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))。
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。
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。
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。
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。
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。
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。
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).
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。
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.
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.
T26898	BRD2879 BRD 2879,BRD-2879
	BRD2879 is a potent and cell-active inhibitor of IDH1-R132H (IC50 = 50 nM).
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).
T32013	GSK990 GSK-990,GSK 990
	GSK990 is similar to GSK864 but is inactive as an IDH1 inhibitor, may be used as a native control to GSK864.
T25006	AGI-14100 AGI 14100	Dehydrogenase	Metabolism
	AGI-14100 是一种新型且可口服的 mIDH1 抑制剂。AGI-14100 用于治疗原发性人类髓性白血病。

化合物

Mutant IDH1-IN-1

Cat.No: T2043

Synonym: IDH1-IN-1

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Mutant IDH1 inhibitor

Cat.No: T16161

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Mutant IDH1-IN-2

Cat.No: T12128

Target: Isocitrate Dehydrogenase (IDH)

Mutant IDH1-IN-6

Cat.No: T39716

Synonym: Mutant IDH1-IN-6

IDH1 Inhibitor 2

Cat.No: T11611

Target: Dehydrogenase

IDH1 Inhibitor 3

Cat.No: T11612

Target: Others

IDH1 Inhibitor 1

Cat.No: T11613

Target: Others

Mutant IDH1-IN-4

Cat.No: T12129

Target: Others

IDH1 Inhibitor 5

Cat.No: T62725

IDH1 Inhibitor 7

Cat.No: T72705

WT IDH1 Inhibitor 2

Cat.No: T63403

IHMT-IDH1-053

Cat.No: T78758

Target: Isocitrate Dehydrogenase (IDH)

(S,R)-WT IDH1 Inhibitor 2

Cat.No: T63402

D-α-Hydroxyglutaric acid disodium

Cat.No: T6820

Synonym: D-alpha-Hydroxyglutaric acid disodium salt,(R)-2-羟基戊二酸二钠盐,Disodium (R)-2-Hydroxyglutarate

Target: ATPase, Others, Reactive Oxygen Species, Endogenous Metabolite, mTOR

Cat.No: T62698

Cat.No: T15550

Target: Dehydrogenase

Cat.No: T16384

Synonym: FT-2102

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Cat.No: T15551

Target: Dehydrogenase

Cat.No: T2104

Synonym: IDH-C35

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Cat.No: T3617

Synonym: 艾伏尼布,AG-120

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

AG-120 (racemic)

Cat.No: T22253

Synonym: 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

Target: Dehydrogenase

Cat.No: TQ0042

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Cat.No: T15442

Target: Others

Cat.No: T7307

Synonym: PVM/MA,PVM/MA共聚物,AG-881

Target: Isocitrate Dehydrogenase (IDH)

Cat.No: T63778

Cat.No: T32009

Synonym: GSK 321,GSK-321

Cat.No: T70890

Cat.No: T26898

Synonym: BRD 2879,BRD-2879

ML-309 (hydrochloride)

Cat.No: T38004

Cat.No: T32013

Synonym: GSK-990,GSK 990

Cat.No: T25006

Synonym: AGI 14100

Target: Dehydrogenase

Cat. No.	Product Name	Target	Signaling Pathways
T1717	alpha-Mangostin α-倒捻子素,α-Mangostin,Mangostin	Apoptosis; Virus Protease; Dehydrogenase; Reactive Oxygen Species; Antibacterial; Antifungal	Apoptosis; Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB
	alpha-Mangostin (Mangostin) 是有多种生物活性的膳食呫吨酮。它是一种IDH1突变体的抑制剂，Ki 值为 2.85 μM。
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

alpha-Mangostin

Cat.No: T1717

Synonym: α-倒捻子素,α-Mangostin,Mangostin

Target: Apoptosis, Virus Protease, Dehydrogenase, Reactive Oxygen Species, Antibacterial, Antifungal

Alternaphenol B2

Cat.No: T83133

Target: Isocitrate Dehydrogenase (IDH)

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