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41

抑制剂 & 化合物

3

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。
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。
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).
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.
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。
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。
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.
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.
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...
T82082	IDO1-IN-23	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	IDO1-IN-23（化合物41）是一种有效的人类IDO1抑制剂，具备13 μM的IC50值。
T78687	IDO1-IN-21	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	IDO1-IN-21（化合物10m）为IDO1抑制剂，其IC50值为0.64 μM。该化合物在小鼠体内可有效抑制肿瘤生长。
T61944	IDO1-IN-15
	IDO1-IN-15 是有效的IDO1抑制剂，IC50为127 nM。IDO1-IN-15与Epacadostat 在体外对抗 IDO1 酶的效力相当。
T61789	IDO1-IN-14
	IDO1-IN-14 (compound 4a) is a highly effective inhibitor of the IDO1 enzyme, exhibiting an IC50 value of 396.9 nM. Additionally, IDO1-IN-14 demonstrates excellent suppression of cellular IDO1 activity, as observed in HeLa cells with an EC50 value of 3393 nM [1].
T74507	IDO1-IN-20
	IDO1-IN-20是一种催化色氨酸氧化代谢的酶，能在肿瘤微环境中对肿瘤进行免疫抑制。
T63814	IDO2-IN-1
	IDO2-IN-1 是一种口服活性的强效IDO2抑制剂，其IC50为112 nM。该化合物适用于炎症性自身免疫研究。
T63034	IDO1-IN-13
	IDO1-IN-13 (compound 27a) 是一种 IDO1 的有效抑制剂 (IC50: 61.6 nM)。IDO1-IN-13 能够抑制细胞 IDO1，对 HeLa 的 EC50 值为 30 nM。在 SK-OV-3 异种移植肿瘤组织中，IDO1-IN-13 减少了 51% 的 kyn/trp 比率。
T73111	IDO1-IN-17
	IDO1-IN-17 (I-4) 是IDO1的抑制剂，其在 hela 细胞中的IC50值为 0.44 μM。
T63082	IDO1-IN-19
	IDO1-IN-19 (Compound 17) 是一种 IDO1 的有效抑制剂，具有潜力进行癌症疾病的研究。
T63780	IDO1-IN-16
	IDO1-IN-16 (I-1) 是一种 IDO1 抑制剂，能够靶向holo-IDO1 (IC50: 127 nM)。
T78975	IDO1-IN-22	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	IDO1-IN-22（Compound 3）是一种效能显著的IDO1抑制剂，具备低纳摩尔级生化活性（hIDO1 IC50：67.4 nM）以及显著的细胞内抑制效果（HeLa细胞中hIDO1 IC50：17.6 nM）。在小鼠LLC异种移植模型中表现出卓越的抗肿瘤效果，并表现出有利的药代动力学（PK）特性。
T62638	IDO1-IN-18
	IDO1-IN-18 (Compound 14) 是一种 IDO1 的有效抑制剂。IDO1-IN-18 具有潜力进行癌症疾病的研究。
T61385	IDO1/TDO-IN-1
	IDO1/TDO-IN-1 (30) is a highly effective inhibitor that targets both IDO1 and TDO enzymes with uncompetitive (Ki = 0.23 μM) and competitive (Ki = 0.73 μM) mechanisms, respectively. This compound, IDO1/TDO-IN-1 (30), exhibits a significant capacity to induce cell apoptosis via the potential mitochondria-mediated Bcl-2/Bax pathway [1].
T63222	IDO1/2-IN-1
	IDO1/2-IN-1 是一个有效的、口服具有活力的 IDO1/IDO2 双重抑制剂，对 IDO1 和 IDO2 的IC50分别为 28 nM 和 144 nM，表现出抗肿瘤作用。
T78795	IDO1/TDO-IN-6	Indoleamine 2,3-Dioxygenase (IDO)	Metabolism
	IDO1/TDO-IN-6（compound 11）为IDO1/TDO双重抑制剂，其IC50值分别为2.25 μM和2.89 μM。在抑制IDO1和TDO方面，其Ki值分别为1.9 μM和3.1 μM。IDO1/TDO-IN-6适用于癌症与免疫学领域的研究。
T63651	IDO1/2-IN-1 hydrochloride
	IDO1/2-IN-1 hydrochloride 是一个有效的 IDO1 (IC50: 28 nM) 和 IDO2 (IC50: 144 nM) 双重抑制剂，口服具有活力。IDO1/2-IN-1 hydrochloride 表现出抗肿瘤作用。
T60499	IDO1/TDO-IN-2
	IDO1/TDO-IN-2 (Compound 1) 是有效的IDO1/TDO 双重抑制剂，IC50s 分别为 0.1 和 0.07 μM，具有癌症研究的潜力。
T61140	IDO1/TDO-IN-3
	IDO1/TDO-IN-3 is a powerful inhibitor targeting IDO1 and TDO enzymes. It displays noteworthy effectiveness against IDO1 (IC50: 0.005 μM) and TDO (IC50: 0.004 μM). Additionally, IDO1/TDO-IN-3 demonstrates considerable in vivo anti-tumor properties while exhibiting no apparent toxicity [1].
T60318	IDO1/TDO-IN-4
	IDO1/TDO-IN-4 显示出对 IDO1 (IC50 = 3.53 μM) 和 TDO (IC50 = 1.15 μM) 的有效抑制作用，并且具有可接受的安全性和药代动力学特性。IDO1/TDO-IN-4 可与 IDO1 形成氢键，与 TDO 产生 π-π 堆积相互作用。 IDO1/TDO-IN-4 可用于抑郁症以及炎症引起的抑郁症的研究。
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).
T11618	IDO-IN-4	Others	Others
	IDO-IN-4 is an indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor.
T11621	IDO-IN-8 NLG-1487	IDO	Metabolism
	IDO-IN-8 is an indoleamine 2,3-dioxygenase (IDO) inhibitor (IC50: 1-10 μM).
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。
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.

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)

Cat.No: T11901

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: T39888

Synonym: IDO1-IN-7

Cat.No: T39839

Synonym: IDO1-IN-11

Cat.No: T39946

Synonym: IDO1-IN-12

Cat.No: T20513

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

Target: 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: T11624

Target: IDO

(S)-IDO1-IN-5

Cat.No: T12801

Target: Others

(Rac)-IDO1-IN-5

Cat.No: T12668

Target: Others

PROTAC IDO1 Degrader-1

Cat.No: T37329

Synonym: PROTAC IDO1 Degrader-1

Cat.No: T82082

Target: Indoleamine 2,3-Dioxygenase (IDO)

Cat.No: T78687

Target: Indoleamine 2,3-Dioxygenase (IDO)

Cat.No: T61944

Cat.No: T61789

Cat.No: T74507

Cat.No: T63814

Cat.No: T63034

Cat.No: T73111

Cat.No: T63082

Cat.No: T63780

Cat.No: T78975

Target: Indoleamine 2,3-Dioxygenase (IDO)

Cat.No: T62638

IDO1/TDO-IN-1

Cat.No: T61385

Cat.No: T63222

IDO1/TDO-IN-6

Cat.No: T78795

Target: Indoleamine 2,3-Dioxygenase (IDO)

IDO1/2-IN-1 hydrochloride

Cat.No: T63651

IDO1/TDO-IN-2

Cat.No: T60499

IDO1/TDO-IN-3

Cat.No: T61140

IDO1/TDO-IN-4

Cat.No: T60318

Cat.No: T11616

Synonym: GS-4361

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

Cat.No: T11619

Synonym: NLG-1489

Target: IDO

Cat.No: T11618

Target: Others

Cat.No: T11621

Synonym: NLG-1487

Target: IDO

Acid secretion-IN-1

Cat.No: T39089

Cat.No: T72056

IDO/Tubulin-IN-2

Cat.No: T74536

Cat.No: T38276

Cat.No: T40211

Synonym: eIF4E-IN-1

Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
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。

天然产物

Coptisine sulfate

Cat.No: T4S0051

Target: Indoleamine 2,3-Dioxygenase (IDO)

Cat.No: T5S0802

Synonym: 巴马汀,Berbericinine,Burasaine

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

Cat.No: T5S0053

Synonym: 黄连碱,Coptisin

Target: Indoleamine 2,3-Dioxygenase (IDO)

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