Ivaltinostat (CG-200745) 是一种有效的泛 HDAC 抑制剂，具有异羟肟酸部分，可在催化袋底部结合锌。Ivaltinostat 抑制组蛋白 H3 和微管蛋白的脱乙酰作用。Ivaltinostat 诱导 p53 的积累，促进 p53 依赖性反式激活，并增强 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。Ivaltinostat 可增强 Gemcitabine 耐药细胞对 Gemcitabine (HY-16138) 和 5-Fluorouracil (5-FU; HY-90006) 的敏感性。Ivaltinostat 诱导凋亡并具有抗肿瘤作用。 Ivaltinostat (CG-200745) is an active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat inhibits deacetylation of histone H3 and tubulin. Ivaltinostat induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat induces apoptosis and has anti-tumour effects.
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CG200745
CAS number：936221-33-9 molecular formula：C24H33N3O4
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| Chinese alias | CG-2 | CG-200745 | HDCG-0745 | ||
| English alias | CG 2 (HDAC INHIBITOR) | HY-16138 | (E)-N-(3-(Dimethylamino)propyl)-N'-hydroxy-2-((1-naphthyloxy)methyl)-2-octenediamide | CG200745 | CG-200745 | IVALTINOSTAT [INN] | (E)-N-[3-(dimethylamino)propyl]-N'-hydroxy-2-(naphthalen-1-yloxymethyl)oct-2-enediamide | | ||
| CAS number | 936221-33-9 | molecular formula | C24H33N3O4 |
| molecular weight | 427.54 g/mol | Exact mass | - |
| PSA | 90.900 Ų | logp | 3.000 |
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