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33

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7181	IDO-IN-1 4-氨基-N-(3-溴-4-氟苯基)-N'-羟基-1,2,5-恶二唑-3-甲脒	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	IDO-IN-1 是吲哚胺-2,3-双加氧酶抑制剂，IC50=59 nM。
T7660	IDO inhibitor 1 4-[[2-[(氨基磺酰基)氨基]乙基]氨基]-N'-(3-溴-4-氟苯基)-N-羟基-1,2,5-恶二唑-3-甲脒	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	IDO inhibitor 1 是一种有效的吲哚胺-2,3 双加氧酶 (IDO) 抑制剂 (IC50 <100 nM)。具有潜在的免疫调节和抗肿瘤活性。
T3548	Epacadostat INCB 024360,艾卡哚司他,IDO Inhibitor 1	IDO; Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	Epacadostat (INCB 024360) 是选择性的IDO1抑制剂，IC50=71.8 nM。
T4142	PCC0208009 IDO inhibitor 1,DO-IN-2,IDO-IN-2	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	PCC0208009 (IDO-IN-2) 是一种有效的 IDO 抑制剂，其在 HeLa 细胞中的 IC50=4.52 nM。它调节 ACC 和杏仁核的突触可塑性，减少神经性疼痛和合并症。
T11623	IDO/TDO-IN-1	Others	Others
	IDO/TDO-IN-1 is an orally active dual indoleamine-2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO) inhibitor (IC50s: 9.7 and 47 nM).
T11901	IDO1-IN-5	IDO; Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	IDO1-IN-5 是可透过血脑屏障的、选择性的IDO1抑制剂，能够与缺乏血红素的 apo-IDO1 结合，但无法与成熟血红素的 IDO1 结合。
T1847	Necrostatin-1 Nec-1,Necrostatin 1	Indoleamine 2,3-Dioxygenase (IDO); Ferroptosis; Autophagy; RIP kinase	Apoptosis; Autophagy; Metabolism; NF-κB
	Necrostatin-1 (Nec-1) 是一种坏死性凋亡抑制剂和 RIP1 抑制剂，具有特异性。Necrostatin-1 抑制 TNF-α 诱导的坏死性凋亡。Necrostatin-1 也可以抑制 IDO。
T20513	IDO1-IN-1 IDO1 inhibitor 1,2 HzBTZ,2-肼基苯并噻唑,IDO1IN1,2-HzBTZ,IDO1-inhibitor-1	IDO	Metabolism
	IDO1-IN-1 (2 HzBTZ) 是一种吲哚胺 2,3-双加氧酶 1 (IDO1) 抑制剂。
T6543	Indoximod NLG-8189,Indoximod (NLG-8189）,1-Methyl-D-tryptophan,吲哚莫德	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	Indoximod (Indoximod (NLG-8189)) 是一种具有口服具有活力的吲哚胺2,3-双加氧酶(IDO) 途径抑制剂。它在调节 mTOR 中充当 Trp 模拟物。它是一种可用于癌症研究的免疫代谢佐剂。
T11624	IDO1-IN-2	IDO	Metabolism
	IDO1-IN-2 is a potent and selective IDO1 inhibitor with IC50s of 81 nM, 59 nM (mouse), and 28 nM (rat), respectively. It has anti-cancer activity.
T37329	PROTAC IDO1 Degrader-1 PROTAC IDO1 Degrader-1
	PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to CRBN E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells[1]. PROTAC IDO1 Degrader-1 (compound 2c) (10 μM; 24 hours) notably decreases IDO1 level induced by IFN-γ[1].PROTAC IDO1 Degrader-1 and IFN-γ (5 ng/mL) are incubated with HeLa cells for 24...
T11625	IDO1 and HDAC1 Inhibitor	Others	Others
	IDO1 and HDAC1 Inhibitor is a dual IDO1 and HDAC1 inhibitor (IC50s: 69.0 nM and 66.5 nM).
T12801	(S)-IDO1-IN-5	Others	Others
	(S)-IDO1-IN-5 is an active S-isomer of IDO1-IN-5. (S)-IDO1-IN-5 binds to IDOL(IC50 value less than 1.5 µΜ).
T12668	(Rac)-IDO1-IN-5	Others	Others
	(Rac)-IDO1-IN-5 is a racemate of IDO1-IN-5, a potent, selective, and brain-penetrating inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity. It specifically binds to apo-IDO1, which lacks heme, instead of mature heme-bound IDO1.
T7504	Necrostatin 2 racemate 5-[(7-氯-1H-吲哚-3-基)甲基]-3-甲基-2,4-咪唑烷二酮,Necrostatin-2 racemate	RIP kinase	Apoptosis; NF-κB
	Necrostatin 2 racemate (Necrostatin-2 racemate) 是一种特异性的RIPK1抑制剂，是一种稳定型 Nec-1。
T39888	IDO1-IN-7 IDO1-IN-7
	IDO1-IN-7, a potent and selective indoleamine-2,3-dioxygenase-1 (IDO1) inhibitor, exhibits high potency with an IC 50 of 6.1 nM in the cellular assay (SKOV3). Apart from its inhibitory properties, IDO1-IN-7 also demonstrates immunomodulatory effects, contributing to its potential applications in cancer research.
T39839	IDO1-IN-11 IDO1-IN-11
	IDO1-IN-11 is an IDO1 inhibitor with an IC 50 value of 0.6 nM.
T39946	IDO1-IN-12 IDO1-IN-12
	IDO1-IN-12 is a potent and orally available IDO1 inhibitor.
T4307	PF-06840003 EOS200271,PF 06840003	IDO; Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	PF-06840003 (EOS200271) 是口服具有活力的、选择性的IDO-1抑制剂，抑制 hIDO-1， dIDO-1和 mIDO-1 的IC50分别为 0.41 μM， 0.59 μM，和 1.5 μM。
T11616	IDO-IN-13 GS-4361	IDO; Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	IDO-IN-13 (GS-4361) 是 indoleamine 2,3-dioxygenase 1 抑制剂，EC50=17 nM。
T11619	IDO-IN-5 NLG-1489	IDO	Metabolism
	IDO-IN-5 is an indoleamine 2,3-dioxygenase (IDO) inhibitor (IC50: 1-10 μM).
T11621	IDO-IN-8 NLG-1487	IDO	Metabolism
	IDO-IN-8 is an indoleamine 2,3-dioxygenase (IDO) inhibitor (IC50: 1-10 μM).
T11618	IDO-IN-4	Others	Others
	IDO-IN-4 is an indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor.
T79189	1-Isopropyltryptophan 1-IsoPT	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	1-Isopropyltryptophan (1-IsoPT)为IDO1抑制剂，能够抑制IFN-γ刺激下IDO-1与IDO-2 mRNA的表达水平。
T39089	Acid secretion-IN-1
	Acid secretion-IN-1, a polycyclic compound, is synthesized for its application as an IDO inhibitor in synthetic experiments.
T72056	KYN-101
	KYN-101是一种高效、选择性的芳香烃受体(AHR)合成拮抗剂,在人HepG2 DRE 荧光素酶报告基因检测中IC50为22 nM,在小鼠Hepa1 Cyp-luc 检测中IC50为23 nM。KYN-101逆转IDO/TDO 介导的肿瘤进展,提高PD-1阻断B16 IDO 荷瘤小鼠和表达内源性高水平IDO 的CT26结直肠癌模型的疗效。
T74536	IDO/Tubulin-IN-2
	IDO/Tubulin-IN-2 (HT2) 是一种对TDO和微管蛋白 (tubulin)展现出高效抑制作用的化合物。该抑制剂对多种癌细胞系（包括U87、HepG2、A549、HCT-116和LO2）均表现出强抗肿瘤活性，其半抑制浓度（IC50）分别为0.43、0.036、0.041、0.095和1.04 μM，有效提升了抗肿瘤效果。
T74992	NU223612
	NU223612 是一种有效的PROTAC(PROTACs)，可降解吲哚胺 2,3-双加氧酶 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO))，Kd 为 640 nM。NU223612 通过CRBN 介导的蛋白酶体降解有效降解IDO1蛋白。NU223612 以 290 nM 的亲和力与 CRBN 结合。NU223612 可以穿过血脑屏障 (BBB)。
T76560	Imsamotide
	Imsamotide (IDO194-214) 为一种具有序列 DTLLKALLEIASCLEKALQVF 的吲哚胺 2,3-双加氧酶 (IDO) 肽。它同时作为主动免疫的免疫剂和抗肿瘤剂。
T38276	Benzomalvin C
	Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor inhibiting binding of substance P by 46% when used at 100 μg/ml in vitro. It is also a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC50 value of 130 μM for recombinant IDO. It was isolated from Penicillium and contains an epoxide group at C-19 and C-20, which is not present in benzomalvins A, B, or E.
T40211	eIF4E-IN-1 eIF4E-IN-1
	eIF4E-IN-1 (WO2021003194A1, compound Y), is a highly effective inhibitor of eIF4E, a key protein involved in immunosuppression. By targeting immune checkpoint proteins such as PD-1, PD-L1, LAG3, TIM3, and IDO, eIF4E-IN-1 functions to disrupt immune suppression and promote immune release in specific diseases such as cancer and infectious diseases.
T60266	(Rac)-Indoximod
	(Rac)-Indoximod (1-Methyl-DL-tryptophan) is a potent inhibitor of indoleamine 2,3-dioxygenase (IDO). Combined treatment with IFN-γ and (Rac)-Indoximod significantly suppresses the activity of α-SMA-expressing human cardiac myofibroblasts (hCMs) and promotes apoptosis by up-regulating the genes IRF-1, Fas, and FasL. Moreover, this co-treatment effectively improves cardiac fibrosis[1].
T11620	IDO-IN-6 NLG-1486	IDO	Metabolism
	IDO-IN-6 is an indoleamine 2,3-dioxygenase (IDO) inhibitor.

化合物

Cat.No: T7181

Synonym: 4-氨基-N-(3-溴-4-氟苯基)-N'-羟基-1,2,5-恶二唑-3-甲脒

Target: Indoleamine 2,3-Dioxygenase (IDO)

IDO inhibitor 1

Cat.No: T7660

Synonym: 4-[[2-[(氨基磺酰基)氨基]乙基]氨基]-N'-(3-溴-4-氟苯基)-N-羟基-1,2,5-恶二唑-3-甲脒

Target: Indoleamine 2,3-Dioxygenase (IDO)

Cat.No: T3548

Synonym: INCB 024360,艾卡哚司他,IDO Inhibitor 1

Target: IDO, Indoleamine 2,3-Dioxygenase (IDO)

Cat.No: T4142

Synonym: IDO inhibitor 1,DO-IN-2,IDO-IN-2

Target: Indoleamine 2,3-Dioxygenase (IDO)

Cat.No: T11623

Target: Others

Cat.No: T11901

Target: IDO, Indoleamine 2,3-Dioxygenase (IDO)

Cat.No: T1847

Synonym: Nec-1,Necrostatin 1

Target: Indoleamine 2,3-Dioxygenase (IDO), Ferroptosis, Autophagy, RIP kinase

Cat.No: T20513

Synonym: IDO1 inhibitor 1,2 HzBTZ,2-肼基苯并噻唑,IDO1IN1,2-HzBTZ,IDO1-inhibitor-1

Target: IDO

Cat.No: T6543

Synonym: NLG-8189,Indoximod (NLG-8189）,1-Methyl-D-tryptophan,吲哚莫德

Target: Indoleamine 2,3-Dioxygenase (IDO)

Cat.No: T11624

Target: IDO

PROTAC IDO1 Degrader-1

Cat.No: T37329

Synonym: PROTAC IDO1 Degrader-1

IDO1 and HDAC1 Inhibitor

Cat.No: T11625

Target: Others

(S)-IDO1-IN-5

Cat.No: T12801

Target: Others

(Rac)-IDO1-IN-5

Cat.No: T12668

Target: Others

Necrostatin 2 racemate

Cat.No: T7504

Synonym: 5-[(7-氯-1H-吲哚-3-基)甲基]-3-甲基-2,4-咪唑烷二酮,Necrostatin-2 racemate

Target: RIP kinase

Cat.No: T39888

Synonym: IDO1-IN-7

Cat.No: T39839

Synonym: IDO1-IN-11

Cat.No: T39946

Synonym: IDO1-IN-12

Cat.No: T4307

Synonym: EOS200271,PF 06840003

Target: IDO, Indoleamine 2,3-Dioxygenase (IDO)

Cat.No: T11616

Synonym: GS-4361

Target: IDO, Indoleamine 2,3-Dioxygenase (IDO)

Cat.No: T11619

Synonym: NLG-1489

Target: IDO

Cat.No: T11621

Synonym: NLG-1487

Target: IDO

Cat.No: T11618

Target: Others

1-Isopropyltryptophan

Cat.No: T79189

Synonym: 1-IsoPT

Target: Indoleamine 2,3-Dioxygenase (IDO)

Acid secretion-IN-1

Cat.No: T39089

Cat.No: T72056

IDO/Tubulin-IN-2

Cat.No: T74536

Cat.No: T74992

Cat.No: T76560

Cat.No: T38276

Cat.No: T40211

Synonym: eIF4E-IN-1

(Rac)-Indoximod

Cat.No: T60266

Cat.No: T11620

Synonym: NLG-1486

Target: IDO

Cat. No.	Product Name	Target	Signaling Pathways
T2718	Palmatine chloride	Others; Indoleamine 2,3-Dioxygenase (IDO); Aurora Kinase	Cell Cycle/Checkpoint; Chromatin/Epigenetic; Metabolism; Others
	Palmatine chloride 是口服具有活力的不可逆 IDO-1抑制剂。它能够减轻结肠损伤，预防肠道菌群失调和调节色氨酸分解代谢，并改善 DSS 诱发的结肠炎。
T5S0802	Palmatine 巴马汀,Berbericinine,Burasaine	Indoleamine 2,3-Dioxygenase (IDO); AChR; AChE; Aurora Kinase	Cell Cycle/Checkpoint; Chromatin/Epigenetic; Metabolism; Neuroscience
	Palmatine (Burasaine) 是口服具有活力的、不可逆IDO-1抑制剂。它可以减轻结肠损伤，预防肠道菌群失调和调节色氨酸分解代谢，从而改善DSS (Dextran Sulphate Sodium Salt) 诱发的结肠炎。它有用于结肠炎的研究潜力。
T4S0051	Coptisine sulfate	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	Coptisine Sulfate 是一种从黄连中分离到的生物碱，是非竞争性的IDO 抑制剂，Ki=为 5.8 μM，IC50=6.3 μM。
T5S0056	Coptisine chloride 盐酸黄连碱,氯化黄连碱,Q-100696,NSC-119754	Indoleamine 2,3-Dioxygenase (IDO); Influenza Virus; Antibacterial	Metabolism; Microbiology/Virology
	Coptisine chloride (NSC-119754) 是从黄连中分离到的一种生物碱，是一种非竞争性 IDO 抑制剂，Ki 值为 5.8 μM，IC50值为 6.3 μM。它是一种 H1N1 神经氨酸酶抑制剂，可用于甲型流感病毒感染，IC50为 104.6 μg/mL。
T5S0053	Coptisine 黄连碱,Coptisin	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	Coptisine (Coptisin) 是一种从黄连中分离到的生物碱，是非竞争性的IDO 抑制剂，Ki=为 5.8 μM，IC50=6.3 μM。
T72508	Palmatine hydroxide
	Palmatine hydroxide 是不可逆的口服活性IDO-1抑制剂，其对HEK 293-hIDO-1 和 rhIDO-1的IC50值分别为3 μM和157 μM。该化合物还能非竞争性抑制(WNV)NS2B-NS3蛋白酶，IC50值为96 μM。Palmatine hydroxide展现了抗癌、抗炎、神经保护、抗细菌和抗病毒的活性。

天然产物

Palmatine chloride

Cat.No: T2718

Target: Others, Indoleamine 2,3-Dioxygenase (IDO), Aurora Kinase

Cat.No: T5S0802

Synonym: 巴马汀,Berbericinine,Burasaine

Target: Indoleamine 2,3-Dioxygenase (IDO), AChR, AChE, Aurora Kinase

Coptisine sulfate

Cat.No: T4S0051

Target: Indoleamine 2,3-Dioxygenase (IDO)

Coptisine chloride

Cat.No: T5S0056

Synonym: 盐酸黄连碱,氯化黄连碱,Q-100696,NSC-119754

Target: Indoleamine 2,3-Dioxygenase (IDO), Influenza Virus, Antibacterial

Cat.No: T5S0053

Synonym: 黄连碱,Coptisin

Target: Indoleamine 2,3-Dioxygenase (IDO)

Palmatine hydroxide

Cat.No: T72508

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