IDO/TDO
抑制剂选择性比较
特异性亚型抑制剂
IDO/TDO产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S8037 |
Necrostatin-1Necrostatin-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。 |
![]() ![]() 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.
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S7111 |
IDO-IN-2IDO-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。 |
![]() ![]() 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. |
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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。 |
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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。 |
![]() ![]() 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.
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S8557 |
IDO inhibitor 1IDO inhibitor 1是一种有效的IDO (indoleamine-(2,3)-dioxygenase)抑制剂,IC50为 3 nM。 |
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S8368 |
LM10LM10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。 |
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S7587 |
Epacadostat (INCB024360) analogueEpacadostat (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。 |
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S8657 |
PF-06840003PF-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)。 |
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S8919 |
LY-3381916LY-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。 |
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S8957 |
NavoximodNavoximod (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。 |
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S8997 |
680C91680C91 是一种有效的、选择性的 TDO 的抑制剂,其Ki值为51 nM。 |
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S9137 |
ErianinErianin, 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. |
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S5249 |
Coptisine chlorideCoptisine (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。 |
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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。 |
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S6728 |
IDO-IN-1IDO-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-1Necrostatin-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。 |
![]() ![]() 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-2IDO-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。 |
![]() ![]() 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。 |
||
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。 |
![]() ![]() 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 1IDO inhibitor 1是一种有效的IDO (indoleamine-(2,3)-dioxygenase)抑制剂,IC50为 3 nM。 |
||
S8368 |
LM10LM10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。 |
||
S7587 |
Epacadostat (INCB024360) analogueEpacadostat (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。 |
||
S8657 |
PF-06840003PF-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)。 |
||
S8919 |
LY-3381916LY-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 |
NavoximodNavoximod (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。 |
||
S8997 |
680C91680C91 是一种有效的、选择性的 TDO 的抑制剂,其Ki值为51 nM。 |
||
S9137 |
ErianinErianin, 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 chlorideCoptisine (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。 |
||
S6728 |
IDO-IN-1IDO-IN-1是有效的IDO抑制剂,IC50为59 nM。 |