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Targets Recommended: Isocitrate Dehydrogenase (IDH) Dehydrogenase

27

抑制剂 & 化合物

2

天然产物

1

化合物库

2

重组蛋白

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Cat. No.	Product Name
L2130	抗癌细胞代谢库		1268 compounds
	1268 种癌细胞代谢相关的生物活性小分子化合物的特有集合，用于肿瘤相关的研究以及抗肿瘤药物的筛选，用于高通量、高内涵筛选；

化合物库

抗癌细胞代谢库

Cat.No: L2130

Compounds: 1268

Cat. No.	Product Name	Target	Signaling Pathways
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))。
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。
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,。
T63380	IDH-C227
	IDH-C227 是选择性的、有效的 IDH1R132H 抑制剂，表现出抗癌活性。
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。
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。
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。
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.
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。
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。
T79745	IDH2R140Q-IN-2	Dehydrogenase	Metabolism
	IDH2R140Q-IN-2 是一种具有口服活性和高效性的 IDH2R140Q 抑制剂，IC50为29 nM。IDH2R140Q-IN-2 具有潜在的抗肿瘤活性，能减少携带IDH2R140Q突变的TF-1细胞系中D2HG的生成（IC50为10 nM），抑制肿瘤组织中D2HG的水平。IDH2R140Q-IN-2适用于研究急性髓系白血病（AML）。
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。
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.
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。
T72705	IDH1 Inhibitor 7
	IDH1 Inhibitor7 是一种 IDH1抑制剂，IC50小于100 nM。
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)。
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。
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。
T63193	IDH2R140Q-IN-1
	IDH2R140Q-IN-1 是IDH2R140Q 有效的抑制剂(IC50: 6.1 nM)，能够用于急性髓细胞白血病的研究。
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。

化合物

Cat.No: T15550

Target: Dehydrogenase

Cat.No: T15551

Target: Dehydrogenase

Cat.No: T2104

Synonym: IDH-C35

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

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: T63380

Cat.No: T7741

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Cat.No: T2346

Synonym: 恩西地平,AG-221

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Cat.No: TQ0042

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Cat.No: T1809

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Mutant IDH1-IN-6

Cat.No: T39716

Synonym: Mutant IDH1-IN-6

Cat.No: T16384

Synonym: FT-2102

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Cat.No: T3617

Synonym: 艾伏尼布,AG-120

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

IDH2R140Q-IN-2

Cat.No: T79745

Target: Dehydrogenase

Cat.No: T7307

Synonym: PVM/MA,PVM/MA共聚物,AG-881

Target: Isocitrate Dehydrogenase (IDH)

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

IHMT-IDH1-053

Cat.No: T78758

Target: Isocitrate Dehydrogenase (IDH)

IDH1 Inhibitor 7

Cat.No: T72705

IDH1 Inhibitor 5

Cat.No: T62725

WT IDH1 Inhibitor 2

Cat.No: T63403

(S,R)-WT IDH1 Inhibitor 2

Cat.No: T63402

IDH2R140Q-IN-1

Cat.No: T63193

Cat.No: T62698

Cat. No.	Product Name	Target	Signaling Pathways
T74193	(R)-IDHP
	(R)-IDHP为IDHP异构体，属于丹参代谢物。该化合物能通过抑制血管平滑肌细胞电压依赖性钙通道与受体操作钙通道的Ca2+释放和Ca2+内流，发挥血管松弛作用，适用于心脑血管疾病研究。
T3682	(-)-Catechin gallate (-)-Catechin 3-O-gallate,儿茶素没食子酸酯,几茶素没食子酸酯,(-)-Catechin 3-gallate	Others; COX	Immunology/Inflammation; Neuroscience; Others
	(-)-Catechin gallate ((-)-Catechin 3-O-gallate) 是绿茶儿茶素中的微量组分，可抑制COX-1和COX-2活性。它抑制人 Beta-secretase，对氯喹敏感的恶性疟原虫 NF54 和耐氯喹的恶性疟原虫 K1 具有抗疟原虫活性。

天然产物

Cat.No: T74193

(-)-Catechin gallate

Cat.No: T3682

Synonym: (-)-Catechin 3-O-gallate,儿茶素没食子酸酯,几茶素没食子酸酯,(-)-Catechin 3-gallate

Target: Others, COX

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPY-02413	Isocitrate dehydrogenase/IDH1 Protein, Human, Recombinant (His) HEL-S-26,HEL-216,IDP,IDCD,PICD,IDH,isocitrate dehyd...	Human	E. coli
	Isocitrate dehydrogenase/IDH1 Protein, Human, Recombinant (His) is expressed in E. coli expression system with His tag. The predicted molecular weight is 48 kDa and the accession number is O75874.
TMPJ-01009	BLVRA Protein, Human, Recombinant (His) Biliverdin reductase A,BVR,BVR A,BLVR,BLVRA,Biliverdin-IX α-...	Human	E. coli
	Human Biliverdin reductase A (BLVRA) is belonged to the Gfo/Idh/MocA family and Biliverdin reductase subfamily. BLVRA is an enzyme that in humans is encoded by the BLVRA gene. BLVRA plays an important role in reducing the gamma-methene bridge of the open tetrapyrrole, biliverdin IX alpha, to bilirubin with the concomitant oxidation of a NADH or NADPH cofactor. BLVRA acts on biliverdin by reducing its double-bond between the pyrrole rings into a single-bond. It accomplishes this using NADPH + H+ ...

重组蛋白

Isocitrate dehydrogenase/IDH1 Protein, Human, Recombinant (His)

Cat.No: TMPY-02413

Species: Human

Expression System: E. coli

BLVRA Protein, Human, Recombinant (His)

Cat.No: TMPJ-01009

Species: Human

Expression System: E. coli

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