IDO/TDO

抑制剂选择性比较

特异性亚型抑制剂

IDO/TDO产品

所有产品(15) IDO/TDO抑制剂(15)

目录号	产品描述	文献引用	实验数据
S8037	Necrostatin-1 Necrostatin-1 (Nec-1)是一种特异性RIP1 (RIPK1)抑制剂，抑制TNF-α诱导的细胞坏死，在293T细胞中EC50为490 nM。Necrostatin-1也可抑制 IDO、细胞自噬和凋亡。	Cell Metab, 2022, S1550-4131(22)00054-7 Bone Res, 2022, 10(1):26 Cell Death Dis, 2022, 13(2):147	Cytosolic extracts or nuclear extracts were examined by Western blot analysis using Abs against p105/p50, p100/p52 and phospho-p65. Solid arrowhead indicates a non-specific band. A nuclear marker, PARP, and cytosolic marker, b-tubulin, were used to assess the purity of each fraction.
S7111	IDO-IN-2 IDO-IN-2 (RG 6078, NLG-919 analogue, GDC-0919 analogue)是一种有效的 IDO1 通路抑制剂，IC50值 of 38 nM。	Int J Mol Sci, 2022, 23(7)3981 J Immunother Cancer, 2021, 9(7)e002840 Eur Respir J, 2020, 2000443	Inhibitor sensitivity of tryptophan 2,3-dioxygenase (TDO) in N-formylkynurenine (NFK) Green assay. Dose-response curves of INCB024360, S7111, and NTRC 0820-0 with IC50 values 67 nM and 75 nM, respectively.
S7756	Indoximod (NLG-8189） Indoximod (NLG-8189, 1-Methyl-D-tryptophan, 1-MT)，一个甲基化的色氨酸，作为 IDO (吲哚胺-(2,3)-双加氧酶) 通路抑制剂，并且能够逆转IDO介导的免疫抑制。Phase 2。	J Immunother Cancer, 2021, 9(7)e002840 Free Radic Biol Med, 2021, S0891-5849(21)00407-X Eur Respir J, 2020, 2000443
S7910	Epacadostat (INCB024360) Epacadostat (INCB024360)是一种有效的选择性吲哚胺 2,3-双加氧酶(IDO1)抑制剂，IC50为 10 nM。它对IDO1的选择性高于其他相关酶如IDO2或TDO。	Mol Cell, 2021, S1097-2765(21)00736-X Sci Adv, 2021, 7(8)eabc2331 Nat Commun, 2021, 12(1):1618	Macrophages were treated with 2 μM obatoclax, 0.1 μM SNS-032, 3 μM SaliPhe, 0.1 μM JNJ872, 1 μM gemcitabine, 1 μM epacadostat or 1 μM NLG919 or remained non-treated and infected with mock or IAV (moi 3). After 24 h cell viability was measured by CTG and results were plotted. Mean ± SD, n=3.
S8557	IDO inhibitor 1 IDO inhibitor 1是一种有效的IDO (indoleamine-(2,3)-dioxygenase)抑制剂，IC50为 3 nM。	Eur Respir J, 2020, 2000443
S8368	LM10 LM10是选择性色氨酸双加氧酶(TDO)抑制剂，抑制人源和鼠源TDO的IC50分别为0.62 μM和2 μM。	Mol Med Rep, 2021, 23(6)445 Eur J Med Chem, 2018, 160:133-145
S7587	Epacadostat (INCB024360) analogue Epacadostat (INCB024360) analogue (INCB14943) 是一个强效的竞争性IDO1 (indoleamine-(2,3)-dioxygenase)抑制剂，其IC50为67 nM。	Oncoimmunology, 2017,
S8657	PF-06840003 PF-06840003 (EOS200271)是一种高选择性的、具有生物口服活性的IDO-1抑制剂。尽管它对hIDO1仅具有中等抑制作用（IC50=0.41 μM），但它能与hIDO-1紧密结合，和hIDO-1之间形成高密度的氢键，所以PF-06840003是一个非常高效的化合物(LE 0.53, LipE 5.1)。	J Immunother Cancer, 2022, 10(3)e004414 Cell, 2020, 182(5):1252-1270.e34 Cells, 2020, 14;9(5):E1222
S8919	LY-3381916 LY-3381916 (IDO1-IN-5) 是一种有效的、选择性的 Indoleamine 2,3-dioxygenase 1 (IDO1) 脑渗透性抑制剂。LY-3381916 可表现出抗肿瘤活性。
S8957	Navoximod Navoximod (GDC-0919, NLG-919) 是一种有效的 IDO (indoleamine-(2,3)-dioxygenase) 途径的抑制剂，其Ki值为7 nM，EC50值为75 nM。	Bioorg Med Chem, 2021, 39:116160 ACS Nano, 2020, 10.1021/acsnano.0c06765 Molecules, 2020, 25(19)E4494
S8997	680C91 680C91 是一种有效的、选择性的 TDO 的抑制剂，其Ki值为51 nM。
S9137	Erianin Erianin, a natural product derived from Dendrobium chrysotoxum, has been used as an analgesic in traditional Chinese medicine and is a potential anti-tumor agent. Erianin can inhibit IDO-induced tumor angiogenesis.
S5249	Coptisine chloride Coptisine (Q-100696, NSC-119754)是一种分离自黄连的吲哚联啶生物碱，具有抗糖尿病、抗菌、抗病毒、抗肝癌和抗白血病效应。Coptisine chloride 也是一种有效的非竞争性 IDO 的抑制剂，对应的IC50值和Ki值分别为6.3 μM和5.8 μM。
S8629	Linrodostat (BMS-986205) Linrodostat (BMS-986205, ONO-7701)是IDO1的不可逆型抑制剂，IC50为1.7 nM。它能抑制犬尿氨酸的生成，在人源Hela细胞、表达人源IDO-1的HEK293细胞和表达TDO的HEK293细胞中，IC50分别为1.7、1.1和>2000 nM。	Front Oncol, 2021, 11:679517 Eur Respir J, 2020, 2000443 Br J Haematol, 2020, 190(3):361-370
S6728	IDO-IN-1 IDO-IN-1是有效的IDO抑制剂，IC50为59 nM。

目录号	产品描述	文献引用	实验数据
S8037	Necrostatin-1 Necrostatin-1 (Nec-1)是一种特异性RIP1 (RIPK1)抑制剂，抑制TNF-α诱导的细胞坏死，在293T细胞中EC50为490 nM。Necrostatin-1也可抑制 IDO、细胞自噬和凋亡。	Cell Metab,2022, S1550-4131(22)00054-7 Bone Res,2022, 10(1):26 Cell Death Dis,2022, 13(2):147	Cytosolic extracts or nuclear extracts were examined by Western blot analysis using Abs against p105/p50, p100/p52 and phospho-p65. Solid arrowhead indicates a non-specific band. A nuclear marker, PARP, and cytosolic marker, b-tubulin, were used to assess the purity of each fraction.
S7111	IDO-IN-2 IDO-IN-2 (RG 6078, NLG-919 analogue, GDC-0919 analogue)是一种有效的 IDO1 通路抑制剂，IC50值 of 38 nM。	Int J Mol Sci,2022, 23(7)3981 J Immunother Cancer,2021, 9(7)e002840 Eur Respir J,2020, 2000443	Inhibitor sensitivity of tryptophan 2,3-dioxygenase (TDO) in N-formylkynurenine (NFK) Green assay. Dose-response curves of INCB024360, S7111, and NTRC 0820-0 with IC50 values 67 nM and 75 nM, respectively.
S7756	Indoximod (NLG-8189） Indoximod (NLG-8189, 1-Methyl-D-tryptophan, 1-MT)，一个甲基化的色氨酸，作为 IDO (吲哚胺-(2,3)-双加氧酶) 通路抑制剂，并且能够逆转IDO介导的免疫抑制。Phase 2。	J Immunother Cancer,2021, 9(7)e002840 Free Radic Biol Med,2021, S0891-5849(21)00407-X Eur Respir J,2020, 2000443
S7910	Epacadostat (INCB024360) Epacadostat (INCB024360)是一种有效的选择性吲哚胺 2,3-双加氧酶(IDO1)抑制剂，IC50为 10 nM。它对IDO1的选择性高于其他相关酶如IDO2或TDO。	Mol Cell,2021, S1097-2765(21)00736-X Sci Adv,2021, 7(8)eabc2331 Nat Commun,2021, 12(1):1618	Macrophages were treated with 2 μM obatoclax, 0.1 μM SNS-032, 3 μM SaliPhe, 0.1 μM JNJ872, 1 μM gemcitabine, 1 μM epacadostat or 1 μM NLG919 or remained non-treated and infected with mock or IAV (moi 3). After 24 h cell viability was measured by CTG and results were plotted. Mean ± SD, n=3.
S8557	IDO inhibitor 1 IDO inhibitor 1是一种有效的IDO (indoleamine-(2,3)-dioxygenase)抑制剂，IC50为 3 nM。	Eur Respir J,2020, 2000443
S8368	LM10 LM10是选择性色氨酸双加氧酶(TDO)抑制剂，抑制人源和鼠源TDO的IC50分别为0.62 μM和2 μM。	Mol Med Rep,2021, 23(6)445 Eur J Med Chem,2018, 160:133-145
S7587	Epacadostat (INCB024360) analogue Epacadostat (INCB024360) analogue (INCB14943) 是一个强效的竞争性IDO1 (indoleamine-(2,3)-dioxygenase)抑制剂，其IC50为67 nM。	Oncoimmunology,2017,
S8657	PF-06840003 PF-06840003 (EOS200271)是一种高选择性的、具有生物口服活性的IDO-1抑制剂。尽管它对hIDO1仅具有中等抑制作用（IC50=0.41 μM），但它能与hIDO-1紧密结合，和hIDO-1之间形成高密度的氢键，所以PF-06840003是一个非常高效的化合物(LE 0.53, LipE 5.1)。	J Immunother Cancer,2022, 10(3)e004414 Cell,2020, 182(5):1252-1270.e34 Cells,2020, 14;9(5):E1222
S8919	LY-3381916 LY-3381916 (IDO1-IN-5) 是一种有效的、选择性的 Indoleamine 2,3-dioxygenase 1 (IDO1) 脑渗透性抑制剂。LY-3381916 可表现出抗肿瘤活性。
S8957	Navoximod Navoximod (GDC-0919, NLG-919) 是一种有效的 IDO (indoleamine-(2,3)-dioxygenase) 途径的抑制剂，其Ki值为7 nM，EC50值为75 nM。	Bioorg Med Chem,2021, 39:116160 ACS Nano,2020, 10.1021/acsnano.0c06765 Molecules,2020, 25(19)E4494
S8997	680C91 680C91 是一种有效的、选择性的 TDO 的抑制剂，其Ki值为51 nM。
S9137	Erianin Erianin, a natural product derived from Dendrobium chrysotoxum, has been used as an analgesic in traditional Chinese medicine and is a potential anti-tumor agent. Erianin can inhibit IDO-induced tumor angiogenesis.
S5249	Coptisine chloride Coptisine (Q-100696, NSC-119754)是一种分离自黄连的吲哚联啶生物碱，具有抗糖尿病、抗菌、抗病毒、抗肝癌和抗白血病效应。Coptisine chloride 也是一种有效的非竞争性 IDO 的抑制剂，对应的IC50值和Ki值分别为6.3 μM和5.8 μM。
S8629	Linrodostat (BMS-986205) Linrodostat (BMS-986205, ONO-7701)是IDO1的不可逆型抑制剂，IC50为1.7 nM。它能抑制犬尿氨酸的生成，在人源Hela细胞、表达人源IDO-1的HEK293细胞和表达TDO的HEK293细胞中，IC50分别为1.7、1.1和>2000 nM。	Front Oncol,2021, 11:679517 Eur Respir J,2020, 2000443 Br J Haematol,2020, 190(3):361-370
S6728	IDO-IN-1 IDO-IN-1是有效的IDO抑制剂，IC50为59 nM。