CAY10581是一种吲哚胺2,3-二加氧酶(IDO)酶,已参与介导与某些疾病(包括癌症)相关的病理性免疫抑制。几种萘醌可抑制细胞和体外的IDO,但效力低(μM)。重要的是,萘醌可降低野生型小鼠的肿瘤生长,但不能降低IDO缺陷小鼠的肿瘤生长。CAY10581是一种萘醌衍生物,可有效抑制IDO(IC50 = 55 nM)。与1-甲基-d-色氨酸(1MT)或环蛋白B相比,它是IDO的更有效抑制剂。CAY10581是IDO的可逆性非竞争性抑制剂,在24小时后对100μM的细胞存活率影响最小。 CAY10581 is an enzyme indoleamine 2,3-dioxygenase (IDO) has been implicated in mediating pathological immunosuppression associated with certain diseases, including cancer. Several naphthoquinones inhibit IDO in cells and in vitro, but at low (μM) potency. Importantly, naphthoquinones reduce tumor growth in wild type mice but not in IDO-deficient mice. CAY10581 is a naphthoquinone derivative that potently inhibits IDO (IC50 = 55 nM). It is a more potent inhibitor of IDO than 1-methyl-d-tryptophan (1MT) or annulin B. CAY10581 acts as a reversible uncompetitive inhibitor of IDO and demonstrates minimal impact on cell viability at 100 μM after 24 hours.
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CAY10581
CAS number:1018340-07-2 molecular formula:C22H21NO4
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Specs
| Chinese alias | - | ||
| English alias | (3R,4S)-4-(benzylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydrobenzo[g]chromene-5,10-dione | CAY 10581 | CAY-10581 | ||
| CAS number | 1018340-07-2 | molecular formula | C22H21NO4 |
| molecular weight | 363.41 g/mol | Exact mass | ≥97% |
| PSA | 75.600 Ų | logp | 2.3 |
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